Search results for: anti-diabetic

Authors: Fatima Doganc, Hakan Goker

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Benzimidazole moiety is an important pharmacophore and privileged structure for the medicinal chemists, since it exhibits various important biological activities. Some clinically used drugs have benzimidazole moiety, such as omeprazole, astemizole, albendazole and domperidone. 2-(4-tert-Butylphenyl)benzimidazole, is a PGC-1α transcriptional regulator shown to have beneficial effects in diabetic mice. We planned to modify the structure of this compound for developing new antidiabetic drug candidates. Hence, a series of guanidino or amidino, benzo/pyrido/pyrimidino-imidazole derivatives were freshly prepared. Mass, 1H-NMR, 13C-NMR, 2D-NMR spectroscopy techniques were used for the new derivatives to clarify their structures and their purity was controlled through the elemental analysis. Antidiabetic activity studies of the synthesized compounds are under the investigation.

Keywords: antidiabetic agents, benzimidazole, imidazopyridine, imidazopyrimidine

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Authors: Rayah Asiri, Anna Robinson-Barella, Adam Todd, Andy Husband

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Introduction: A high prevalence of diabetes and diabetes-related complications in ethnic minority communities is of significant concern. Several studies have indicated low adherence rates to antidiabetic medications in ethnic minorities. Poor adherence to antidiabetic medications leads to a higher risk of complications and mortality. This review aims to explore the barriers to and facilitators of adherence to antidiabetic medication among ethnic minority groups in high-income countries. Methods: A comprehensive search of MEDLINE, Embase, CINAHL, and PsycINFO databases for qualitative studies exploring the barriers to or facilitators of adherence to antidiabetic medication in ethnic minority groups were conducted from database inception to March 2022 (PROSPERO CRD42022320681). A quality assessment of the studies was conducted using the Critical Appraisal Skills Programme (CASP) tool. Key concepts and themes from relevant studies were synthesised using a meta-ethnographic approach. Result: A total of 18 studies were included in the review, and three major themes were developed: 1) cultural underpinnings, 2) communication and building relationships, and 3) managing diabetes during holidays. Conclusion: Multiple barriers and facilitators of adherence to antidiabetic medication among ethnic minority people in high-income countries have been identified. A medication adherence intervention focusing on identified barriers to adherence to antidiabetic medication in ethnic minorities may help in improving diabetes outcomes in these groups.

Keywords: medication adherence, diabetes, ethnic minority, barriers, facilitators

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Authors: Iram Batool, Aamer Saeed, Irfan Zia Qureshi, Ayesha Razzaq, Saima Kalsoom

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Heterocyclic compounds analogues and their derivatives have attracted strong interest in medicinal chemistry due to their biological and pharmacological properties. A series of new thiazolopyrimidine carboxylates were conveniently synthesized by one-pot three-component reaction of ethyl acetoacetate, 2-aminothiazole and benzaldehyde substituted with electron-donating and electron-withdrawing groups in order to find some more potent antidiabetic and antibacterial drugs. The structures of synthesized compounds were characterized by elemental analysis, IR, 1H NMR, 13C NMR spectroscopy. An in vitro antidiabetic effect was evaluated in adult male BALB/c mice and antibacterial activities were tested against Micrococcus luteus, Salmonella typhimurium, Bacillus subtilis, Bordetella bronchiseptica and Escherichia coli. Some of the tested compounds proved to possess good to excellent activities more than the reference drugs. An in silico molecular docking was also performed on synthesized compounds. The current study is expected to provide useful insights into the design of antidiabetic and antibacterial drugs and understanding the mechanism by which such drugs interact with RNA and diabetes target and exert their biochemical action.

Keywords: antidiabetic, antibacterial, MOE docking, thiazolopyrimidine

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Authors: Kinjal H. Shah, Piyush M. Patel

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Diabetes mellitus is considered to be a serious endocrine syndrome. Synthetic hypoglycemic agents can produce serious side effects including hematological effects, coma, and disturbances of the liver and kidney. In addition, they are not suitable for use during pregnancy. In recent years, there have been relatively few reports of short-term side effects or toxicity due to sulphonylureas. Published figures and frequency of side effects in large series of patient range from about 1 to 5%, with symptoms severe enough to lead to the withdrawal of the drug in less than 1 to 2%. Adverse effects, in general, have been of the following type: allergic skin reactions, gastrointestinal disturbances, blood dyscrasias, hepatic dysfunction, and hypoglycemia. The associated disadvantages with insulin and oral hypoglycemic agents have led to stimulation in the research for locating natural resources showing antidiabetic activity and to explore the possibilities of using traditional medicines with proper chemical and pharmacological profiles. Literature survey reveals that the inhabitants of Abbottabad district of Pakistan use the dried leaf powder along with table salt and water orally for treating diabetes, skin allergy, wounds and as a blood purifier, where they pronounced the plant locally as ‘Nem.' The detailed phytochemical investigation of the Cedrela toona Roxb. leaves for antidiabetic activity has not been documented. Hence, there is a need for phytochemical investigation of the leaves for antidiabetic activity. The collection of fresh leaves and authentification followed by successive extraction, phytochemical screening, and testing of antidiabetic activity. The blood glucose level was reduced maximum in ethanol extract at 5th and 7th h after treatment. Blood glucose was depressed by 8.2% and 10.06% in alloxan – induced diabetic rats after treatment which was comparable to the standard drug, Glibenclamide. This may be due to the activation of the existing pancreatic cells in diabetic rats by the ethanolic extract.

Keywords: antidiabetic, Cedrela toona Roxb., phytochemical screening, blood glucose

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Authors: Sunil Kumar

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Background: The present study was performed to investigate the antidiabetic effect of the constituents isolated from Sarca asoca by enzyme inhibitory activity. Methods: The dried leaves of Sarca asoca were defatted with petroleum ether and further the same amount plant materials were extracted with methanol. The dried methanol extract was subjected to fractionation and chromatographic separation, which led to the isolation of kaemferol, β-sitosterol and quercetin stigmasterol. Their structures were elucidated on the basis of spectroscopic studies as well as by comparison with the data available in the literature. The compounds were evaluated for in vitro enzyme inhibition effect. Results: The isolated compounds kaemferol, β-sitosterol and stigmasterol showed 45.32, 40.5 and 41.23% α-amylase inhibition respectively and 43.45, 39.29 and 32.43% α-glucosidase inhibition respectively at the conc. of 50 µg/kg. Conclusion: The compounds isolated from Sarca asoca showed in vitro and in vivo antidiabetic activity. So, Euphorbia hirta is a beneficial plant for management of diabetic disorders.

Keywords: diabetes, quercetin, sitosterol, stigmasterol

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Authors: Yohannes Kelifa, Gomathi Periasamy, Aman Karim

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Introduction: Diabetes mellitus has become a major public health and economical problem across the globe. Modern antidiabetic drugs have a number of limitations, and scientific investigation of traditional herbal remedies used for diabetes may provide novel leads for the development of new antidiabetic drugs that can be used as alternative or complementary to available antidiabetic allopathic medications. Though Myrica salicifolia Hochst. ex A. Rich. is used for the management of diabetes in Ethiopian traditional medicine, there was no previous scientific evidence about its antidiabetic effect to the authors’ knowledge. This study was undertaken to evaluate the antidiabetic activity the root extracts of Myrica salicifolia in streptozotocin (STZ)-induced diabetic mice. Methods: Experimental diabetes was induced by intraperitoneal administration of STZ (150 mg/kg) in male mice. Diabetic mice were treated with oral doses of M. salicifolia root extracts at 200, 400 and 600 mg/kg, and its fractions (chloroform, ethyl acetate, n-butanol and aqueous) at a dose of 400 mg/kg daily for 15 days. Fasting blood glucose level (BGL) was measured at 0, 5th,10th, and 15th day. The free radical scavenging activity of the crude extract was determined using in vitro by DPPH assay. The statistical significance was assessed by one-way ANOVA, followed by Tukey’s multiple comparison tests. Results were considered significant when p < 0.05. Results: Daily administration of the M. salicifolia 80% methanol root extracts (at three different doses (200, 400 and 600 mg/kg) significantly (p < 0.05, p < 0.01 and p < 0.001) reduced fasting BGL compared with diabetic control. The aqueous and butanol fractions at a dose of 400 mg/kg resulted in maximum reduction of fasting BGL by 42.39%, and 52.13%, respectively at the 15th day in STZ-induced diabetic mice. Free radical scavenging activity of the 80% methanol extract of M. salicifolia was comparable to ascorbic acid. The IC50 values of the crude extract and ascorbic acid (a reference compound) were found to be 4.54 μg/ml and 4.39 μg/ml, respectively. Conclusion: These findings demonstrated that the methanolic extracts of M. salicifolia root and its fractions (n-butanol and aqueous) exhibit a significant antihyperglycemic activity in STZ-induced diabetic mice. Furthermore, the result of the present study indicates that M. salicifolia root extract is a potential source of natural antioxidants.

Keywords: antidiabetic, diabetes mellitus, DPPH, mice, Myrica salicifolia, streptozotocin

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Authors: E. Chiam, E. Koh, W. Teh, M. Prabhakaran

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Fruits and vegetables (F&V) are widely eaten for their nutritional value and associated health benefits being an immense source of bioactive compounds. However, F&V peels are often discarded, and it accounts for a higher proportion of food waste. Incorporation of F&V peels as functional ingredients can add more value to food due to the higher amounts of phytochemicals present in them. In this research, methanolic extracts of different F&V peels, namely apple, orange, kiwi, grapefruit, dragon fruit, pomelo, and pumpkin are investigated for their total phenolic content (TPC) by Folin-Ciocalteau (FC) assay and the antioxidant capacity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and phosphomolybdenum assay using UV-Vis spectroscopy. Evaluation of the α-glucosidase inhibitory assay was carried out during this study to determine the antidiabetic potential of F&V peels. Results of our study showed that grapefruit peels contained the highest total phenolic content of 477.81 ± 0.01 mg gallic acid equivalent per gram dry weight of the sample, and kiwi peel had the highest antioxidant capacity (90.51 ± 0.10 % inhibition of DPPH radical) among the different F&V peels studied. Fruit peels exhibited high α-glucosidase inhibitory activity. Comparing fruit peels with vegetable peels, it was found that fruit peels had high total phenolic content, antioxidant capacity and anti-diabetic potential compared to vegetable peels.

Keywords: polyphenolics, fruit peels, antioxidant, antidiabetic

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Authors: S. N. T. I. Sampath, J. M. S. Jayasinghe, A. P. Attanayake, V. Karunaratne

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Diabetes mellitus is one of the major public health posers throughout the world today that incidence and associated with increasing mortality. Insufficient regulation of the blood glucose level might be serious effects for health and its necessity to identify new therapeutics that have ability to reduce hyperglycaemic condition in the human body. Even though synthetic antidiabetic drugs are more effective to control diabetes mellitus, there are considerable side effects have been reported. Thus, there is an increasing demand for searching new natural products having high antidiabetic activity with lesser side effects. The purposes of the present study were to evaluate different physical parameters and in-vitro and in-vivo antidiabetic potential of the selected combined medicinal plant extracts mixture composed of leaves of Murraya koenigii, cloves of Allium sativum, fruits of Garcinia queasita and seeds of Piper nigrum. The selected plants parts were mixed and ground together and extracted sequentially into the hexane, ethyl acetate and methanol. Solvents were evaporated and they were further dried by freeze-drying to obtain a fine powder of each extract. Various physical parameters such as moisture, total ash, acid insoluble ash and water soluble ash were evaluated using standard test procedures. In-vitro antidiabetic activity of combined plant extracts mixture was screened using enzyme assays such as α-amylase inhibition assay and α-glucosidase inhibition assay. The acute anti-hyperglycaemic activity was performed using oral glucose tolerance test for the streptozotocin induced diabetic Wistar rats to find out in-vivo antidiabetic activity of combined plant extracts mixture and it was assessed through total oral glucose tolerance curve (TAUC) values. The percentage of moisture content, total ash content, acid insoluble ash content and water soluble ash content were ranged of 7.6-17.8, 8.1-11.78, 0.019-0.134 and 6.2-9.2 respectively for the plant extracts and those values were less than standard values except the methanol extract. The hexane and ethyl acetate extracts exhibited highest α-amylase (IC50 = 25.7 ±0.6; 27.1 ±1.2 ppm) and α-glucosidase (IC50 = 22.4 ±0.1; 33.7 ±0.2 ppm) inhibitory activities than methanol extract (IC50 = 360.2 ±0.6; 179.6 ±0.9 ppm) when compared with the acarbose positive control (IC50 = 5.7 ±0.4; 17.1 ±0.6 ppm). The TAUC values for hexane, ethyl acetate, and methanol extracts and glibenclamide (positive control) treated rats were 8.01 ±0.66; 8.05 ±1.07; 8.40±0.50; 5.87 ±0.93 mmol/L.h respectively, whereas in diabetic control rats the TAUC value was 13.22 ±1.07 mmol/L.h. Administration of plant extracts treated rats significantly suppressed (p<0.05) the rise in plasma blood glucose levels compared to control rats but less significant than glibenclamide. The obtained results from in-vivo and in-vitro antidiabetic study showed that the hexane and ethyl acetate extracts of selected combined plant mixture might be considered as a potential source to isolate natural antidiabetic agents and physical parameters of hexane and ethyl acetate extracts will helpful to develop antidiabetic drug with further standardize properties.

Keywords: diabetes mellitus, in-vitro antidiabetic assays, medicinal plants, standardization

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Authors: Ikram Mohamed Eltayeb, Ustina Saeed Barsoumbolice

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Cinnamomum zeylanicum belong to the family Lauraceae and Artemisia absinthium belong to the family Asteraceae. Both were traditionally used as antiemetic, anti-inflammatory and antidiabetic. In Sudan, the mixtures of the two plants were traditionally used for the treatment of diabetes. Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia. It is mainly classified into two major groups, type-1 and type-2. Type-2 is a combination of resistance to insulin action and an inadequate compensatory insulin secretory response. The treatment of type-2 diabetes mellitus (DM) with synthetic drugs have many side effects so many researches were conducted to overcome or reduce this side effects by using alternative medicine. The objective of this study is to investigate and compare the anti-diabetic activity of C. zeylanicum and A. absinthium and their combination with difference ratio. C. zeylanicum and A. absinthium were extracted by 96% ethanol using Soxhlet apparatus. Thirty-two rats were divided into eight groups; each group contains four rats. 1st group was administered with distilled water at dose of 10ml/kg, 2nd group had received glucose only at dose of 2g/kg intraperitoneal, the standard group (3rd group) had received Glibenclamide orally at dose of 0.45mg/kg, 4th group received 100 mg C. zeylanicum + 300 mg A. absinthium with a ratio of (25:75), 5th group received 300 mg C. zeylanicum + 100 mg A. absinthium with a ratio of (75:25), 6th group received 200 mg C. zeylanicum + 200 mg A. absinthiumwith a ratio of (50:50), 7th group received 400 mg of A. absinthium, 8th group received 400 mg of C. zeylanicum. Then the blood samples were taken Retro-orbitally at 0, 1, 2 and 4 hours and the glucose level was measured. Each plant alone and their combination with different ratios shows antidiabetic effect. The significant activity was shown by A. absinthium extract (400 mg/kg), combination of ratio of (75:25) A. absinthium: C. zeylanicum(400mg/kg) and then C. zeylanicum(400mg/kg) with p-value 0.001, 0.022, 0.030 respectively, the activity was found to be increased with time. The other combinations showed less activity with p-value > 0.05. The result concludes that the good antidiabetic activity was performed by A. absinthium alone and its activity decreased by increase combination ratio with C. zeylanicum. Which maybe explains by the antagonistic effect between the compounds of C. zeylanicum and A. absinthium.

Keywords: antidiabetic, Artemisia absinthium , cinnamomum zeylanicum, combination

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Authors: Parminder Nain, Jaspreet kaur, Vipin Saini, Sunil Sharma

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Jasminum humile commonly known as yellow Jasmine or Pili chameli, is a medicinal plant used in Ayurveda for treating various diseases, one of which is diabetes mellitus. The current study aimed to establish the antidiabetic and antioxidant properties of aqueous extract of Jasminum humile leaves (AEJHL) in nicotinamide/streptozotocin induced type 2 diabetic rats. Phytochemical screening, HPLC analysis, and acute toxicity study of AEJHL were carried out. Male albino wistar rats (n=42) were divided into seven equal groups. Rats with moderate diabetes having hyperglycemia (blood glucose 250-400 mg/dl) were taken for the experiment. Various concentrations of aqueous extract of Jasminum humile leaves (50, 100, 200 and 300 mg/kg, p.o.), and glibenclamide (1mg/kg, p.o.) were orally administered to diabetic rats for 45 days. The effect of AEJHL on blood glucose, plasma insulin and biochemical parameters such as hemoglobin, total protein, serum creatinine, serum urea, alkaline phosphate, Glutamic-oxalacetic transaminase (SGOT) and glutamic-pyruvic transaminase (SGPT), as well as total cholesterol, triglycerides, and high-density lipoprotein (HDL) were also studied. The antioxidant effect of AEJHL was determined by analyzing hepatic and renal antioxidant markers, like superoxide dismutase (SOD), catalase (CAT), reduced Glutathione (GSH), Glutathione peroxidase (GPx), and lipid peroxidation (LPO) in diabetic rats. After 45-days oral administration of aqueous extract of Jasminum humile leaves significantly (p<0.05) reduced blood sugar and increase plasma insulin level and also reverse all above biochemical parameters and antioxidant enzyme level at dose dependent manner. These findings provide in vivo evidence that the aqueous extract of Jasminum humile leaves possess significant antidiabetic and antioxidant potential in nicotinamide/streptozotocin-induced type-2 diabetes mellitus in rats.

Keywords: antidiabetic, antioxidant, jasminum humile, nicotinamide/streptozotocin, type-2 diabetic

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Authors: Khalil Abdullah Ahmed Khalil, Elsadig Mohamed Ahmed

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Extracts of various plants material capable of decreasing blood sugar have been tested in experimental animal models and their effects confirmed. Neem or Margose (Azadirachta Indica) is an indigenous plant believed to have antiviral, antifungal, antidiabetic and many other properties. This paper deals with a comparative study of the effect of aqueous Neem leaves extract alone or in combination with glibenclamide on alloxan diabetic rabbits. Administration of crude aqueous Neem extract (CANE) alone (1.5 ml/kg/day), as well as the combination of CANE (1.5 ml/kg/day) with glibenclamide (0.25 mg/kg/day) significantly, decreased (P<0.05) the concentrations of serum lipids, blood glucose and lipoprotein VLDL(very low-density lipoproteins) and LDL(low-density lipoproteins) but significantly increased (P<0.05) the concentration of HDL(high-density lipoprotein). The change was observed significantly greater when the treatment was given in combination of CANE and glibenclamid than with CANE alone.

Keywords: neem, hypoglycemic, hypolipidemic, cholesterol

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Authors: Hairin Taha, Aditya Arya, M. A. Hapipah, A. M. Mustafa

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Plants have been an important source of medicine since ancient times. Pseuduvaria monticola is a rare montane forest species from the Annonaceae family. Traditionally, the plant was used to cure symptoms of fever, inflammation, stomach-ache and also to reduce the elevated levels of blood glucose. Scientifically, we have evaluated the antidiabetic potential of the Pseuduvaria monticola bark methanolic extract on certain in vitro cell based assays, followed by in vivo study. Results from in vitro models displayed PMm upregulated glucose uptake and insulin secretion in mouse pancreatic β-cells. In vivo study demonstrated the PMm down-regulated hyperglycaemia, oxidative stress and elevated levels of pro-inflammatory cytokines in type 2 diabetic rat models. Altogether, the study revealed that Pseuduvaria monticola might be used as a potential candidate for the management of type 2 diabetes and its related complications.

Keywords: type 2 diabetes, Pseuduvaria monticola, insulin secretion, glucose uptake

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Authors: Bhupendra Kumar Poudel, Sadhana Amatya, Tirtha Maiya Shrestha, Bharatmani Pokhrel, Mohan Prasad Amatya

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Background: H. salicifolia is a dense, branched, multipurpose, deciduous, nitrogen fixing, thorny willow-like small to moderate tree, restricted to the Himalaya. Among the two species of Nepal (Hippophae salicifolia and H. tibetana), it has been traditionally used as food additive, anticancer (bark), and treating toothache, tooth inflammation (anti-inflammatory) and radiation injury; while people of Western Nepal have largely undermined its veiled treasure by using it for fuel, wood and soil stabilization only. Therefore, the main objective of this study was to explore biological properties (analgesic, antidiabetic, cytotoxic and anti-inflammatory properties of this plant. Methodology: The transverse section of leaves and stems were viewed under microscope. Extracts obtained from soxhlation subjected to tests for phytochemical and biological studies. Rats (used to study antidiabetic and anti-inflammatory properties) and mice (used to study analgesic, CNS depressant, muscle relaxant and locomotor properties) were assumed to be normally distributed; then ANOVA and post hoc tukey test was used to find significance. The data obtained were analyzed by SPSS 17 and Excel 2007. Results and Conclusion: Pharmacognostical analysis revealed the presence of long stellate trichomes, double layered vascular bundle 5-6 in number and double layered compact sclerenchyma. The preliminary phytochemical screening of the extracts was found to exhibit the positive reaction tests for glycoside, steroid, tannin, flavonoid, saponin, coumarin and reducing sugar. The brine shrimp lethality bioassay tested in 1000, 100 and 10 ppm revealed cytotoxic activity inherent in methanol, water, chloroform and ethyl acetate extracts with LC50 (μg/ml) values of 61.42, 99.77, 292.72 and 277.84 respectively. The cytotoxic activity may be due to presence of tannins in the constituents. Antimicrobial screening of the extracts by cup diffusion method using Staphylococcus aereus, Escherichia coli and Pseudomonas aeruginosa against standard antibiotics (oxacillin, gentamycin and amikacin respectively) portrayed no activity against the microorganisms tested. The methanol extract of the stems and leaves showed various pharmacological properties: and antidiabetic, anti-inflammatory, analgesic [chemical writhing method], CNS depressant, muscle relaxant and locomotor activities in a dose-dependent fashion, indicating the possibility of the presence of different constituents in the stems and leaves responsible for these biological activities. All the effects when analyzed by post hoc tukey test were found to be significant at 95% confidence level. The antidiabetic activity was presumed to be due to flavonoids present in extract. Therefore, it can be concluded that this plant’s secondary metabolites possessed strong antidiabetic, anti-inflammatory and cytotoxic activity which could be isolated for further investigation.

Keywords: Hippophae salicifolia, constituents, antidiabetic, inflammatory, brine shrimp

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Authors: Rajnish Gupta, R. S. Gupta

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Present research was aimed to investigate antidiabetic and antioxidant status of Lupeol in streptozotocin induced diabetes. Rats were divided into following groups mainly: control, diabetic, normal group as well as diabetic treated with Lupeol at 25 and 35 mg/kg b.wt./day for 21 days, diabetic group treated with glibenclamide. Tissue (pancreas, kidney and liver) as well as serum biochemical parameters were analysed for any abnormal behavior. Lupeol administration reduced diabetes onset with significant improvement in serum insulin level also strengthened by increase in β-Cell counts. A significant decrease was observed in serum glucose level. Furthermore, Lupeol treatment increased the antioxidant enzymes, glycolytic enzymes and also protein levels with a decrease in the level of thiobarbituric acid-reactive oxygen species and gluconeogenic enzymes. Present study proves that Lupeol administration significantly reinstated serum and tissue biochemical parameters and thus strengthening its antidiabetic potential.

Keywords: oxidative stress, pterostilbene, thiobarbituric acid, reactive oxygen species

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Authors: Devarakonda Ramadevi, Dasari Rambabu, K. Suresh Babu, Battu Ganga Rao, Lakshmi Sirisha Kotikalapudi

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The phytochemical and biological evaluation of the whole plant of Derris scandens is belonging to the family fabaceae. The dried plant of D.scandens was procured from the tirumala. The completely dried powder of the whole plant was taken and ground to a coarse powder which was then subjected to Soxhlet extraction with hexane and chloroform successively for 36 hrs. Chloroform extract was filtered and concentrated by using rotary evaporator an about 100g extract was obtained. The chloroform extract was subjected to column chromatographed over silicagel. From the column chromatography seven compounds were isolated named as osajin, scandinone, scandenone, 4,5,7-tri hydroxy biprenyl isoflavone, derris isoflavone-A, scandenin and isoscandinone. D.scandens resulting in the isolation of seven compounds in the plant was confirmed by spectral data (1H NMR, 13C NMR, ESI-MS and FTIR). The isolated compounds were screened for antioxidant activity, antidiabetic activity, α-glucosidase (inhibitory activity) and anti-bacterial activity. The isolated seven compounds were tested for α-glucosidase inhibitory activity and antioxidant activity. All the seven compounds showed good α-glucosidase inhibitory activity and moderate antioxidant activity.

Keywords: Derris scandens, phytochemical, antioxident, antidiabetic, antibacterial activity

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Authors: Dawit Chankaye

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Background: Azadirachta indica is the most versatile medicinal plant known as “the village pharmacy”. The plant is known for its broad spectrum of biological activity in India and various countries throughout history by many different human cultures. The present study was undertaken to determine the antimalarial and antidiabetic properties of the leaf extracts of A. indica grown in Ethiopia when treated in vivo. This work has also been concerned with determining essential oil composition and the antimicrobial activity of the plant in vitro. Methods: Leaf extracts were prepared using three different selected solvents. Standard and clinical isolates were treated with extracts of the leaves of A. indica using the agar well diffusion method. The antimalarial and antidiabetic tests were conducted in vivo in mice. Phytochemical screening was done using various chemical tests, and the volatile oil constituents were determined using gas chromatography-mass spectrometry (GC/MS). Results: In vivo antimalarial activity studies showed 85.23%, 69.01%, and 81.54% suppression of parasitemia for 70% ethanol, acetone, and water extracts, respectively. The extracts collected from the leaves also showed reduced blood sugar levels in alloxan-induced diabetic mice. In addition, the solvent extracts were shown to have an inhibitory effect on the growth of microorganisms under the study. The minimum inhibitory concentration (MIC) ranged from 850 to 1050 µg/ml. Notably, the phytochemical investigation of the ethanol extracts showed the presence of secondary metabolites. Seventeen compounds (mainly sesquiterpenes) that represent 75.45% of the essential oil were characterized by GC/MS analysis. Conclusion: Extracts examined in this study indicated that the leaf of A. indica grown in Ethiopia retained the biological activities demonstrating the extent equivalent to when it was grown in its natural habitat. In addition, phytochemical investigation and GC/MS analysis of volatile oil constituents showed comparable results to those presented in India and elsewhere.

Keywords: Azadirachta indica, vivo, antimalarial activity, antidiabetic activity, alloxan, mice, phytochemical

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Authors: John Lyndon C. Lunnay

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This study discerns to evaluate the antidiabetic efficacy of pig bile on alloxan-induced BALB/c mice. The experimental animals were divided and selected using RCBD into 5 groups (n= 4): T1 (negative control), T2 (1ml/kg), T3 (2ml/kg), T4 (3ml/kg) and T5 (Glibenclamide). Hyperglycemia was induced by injecting 1% alloxan monohydrate intraperitoneally. A glucose tolerance test was performed using a 2g/kg glucose solution, and blood glucose levels were measured at different time intervals. 14 days of monitoring was also done to ensure effectivity and efficacy of the different treatments. Bodyweight was also determined. Results show that administration of treatments on test animals significantly reverted the blood glucose levels of mice in 60 minutes and 120 minutes using an oral glucose tolerance test. After 14 days of monitoring, normal blood glucose levels were seen significantly on T2 (1ml/kg), T3 (2ml/kg), T4 (3ml/kg), and T5 (Glibenclamide), which only suggests the efficacy of pig bile on lowering glucose levels on alloxan-induced diabetic mice. Bodyweight analysis shows no significant difference. Duncan’s multiple range test (DMRT) shows comparable efficacy and effectivity between T4 (3ml/kg) and T5 (Glibenclamide) on lowering BGL at different day and time intervals.

Keywords: pig bile, BALB/c mice, blood glucose, Gllibenclamide

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Authors: Sourabh Jain, Vikas Jain, Dharmendar Kumar

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The present study investigated the antidiabetic potential of Cedrus deodara heart wood aqueous extract. Aqueous extract of Cedrus deodara was found to reduce blood sugar level in alloxan induced diabetic rats. Reduction in blood sugar could be seen from 5th day after continuous administration of the extract and on 21st day sugar levels were found to be reduced by 40.20%. Oxidative stress produced by alloxan was found to be significantly lowered by the administration of Cedrus deodara aqueous extract (500 mg/kg). This was evident from a significant decrease in lipid per oxidation level in liver induced by alloxan. The level of Glutathione, Catalase, Superoxide dismutase and Glutathione-S-Transferase in liver, kidney and pancreas tissue were found to be increased significantly after drug administration. The results obtained in the present study suggest that the Cedrus deodara aqueous extract effectively and significantly reduced the oxidative stress induced by alloxan and produced a reduction in blood sugar level.

Keywords: Cedrus deodara, heartwood, antioxidant, anti-diabetic, anti-inflammatory

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Authors: Manjusha Choudhary

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Objective: Cassia occidentalis Linn. belongs to Family Caesalpiniaceae is a common weed scattered from the foothills of Himalayas to West Bengal, South India, Burma, and Sri Lanka. It is used widely in folklore medicine in India as laxative, expectorant, analgesic, anti-malarial, hepatoprotective, relaxant, anti-inflammatory and antidiabetic. The present study was carried out to investigate the hypoglycaemic and hypolipidemic activities of ethanolic extract of Cassia occidentalis stem bark. Methods: Stem bark extract of Cassia occidentalis (SBCO) was administered orally at 250 and 500 mg/kg doses to normal and streptozotocin (STZ) induced type-2 diabetic mice. Various parameters like fasting blood glucose (FBG) level, serum cholesterol, high density lipoprotein (HDL) cholesterol, triglycerides (TG), total protein, urea, creatinine, serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) levels and physical parameters like change in body weight, food intake, water intake were performed for the evaluation of antidiabetic effects. Results: Both the doses of extract caused a marked decrease in FBG levels in STZ induced type 2 diabetic mice. Administration of SBCO led to the decrease in the blood glucose, food intake, water intake, organ weight, SGOT, SGPT levels with significant value and increased the levels of TG, HDL cholesterol, creatinine, cholesterol, total protein with a significant value (p < 0.05-0.01). The decrease in body weight induced by STZ was restored to normal with a significant value (p < 0.01) at both doses. Conclusion: Present study reveals that SBCO possess potent hypoglycaemic and hypolipidemic activities and supports the folklore use of the stem bark of plant as antidiabetic agent.

Keywords: Cassia occidentalis, diabetes, folklore, herbs, hypoglycemia, streptozotocin

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Authors: Nawel Ouennoughi, Kamel Daoud

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During recent years, new pharmaceutical dosage forms were developed in the research laboratories and which consists of encapsulating one or more active molecules in a polymeric envelope. Several techniques of encapsulation allow obtaining the microparticles or the nanoparticles containing one or several polymers. In the industry, microencapsulation is implemented to fill the following objectives: to ensure protection, the compatibility and the stabilization of an active matter in a formulation, to carry out an adapted working, to improve the presentation of a product, to mask a taste or an odor, to modify and control the profile of release of an active matter to obtain, for example, prolonged or started effect. To this end, we focus ourselves on the encapsulation of the antidiabetic. It is an oral hypoglycemic agent belonging to the second generation of sulfonylurea’s commonly employed in the treatment of type II non-insulin-dependent diabetes in order to improve profile them dissolution. Our choice was made on the technique of encapsulation by complex coacervation with two types of polymers (gelatin and the gum Arabic) which is a physicochemical process. Several parameters were studied at the time of the formulation of the microparticles and the nanoparticles: temperature, pH, ratio of polymers etc. The microparticles and the nanoparticles obtained were characterized by microscopy, laser granulometry, FTIR and UV-visible spectrophotometry. The profile of dissolution obtained for the microparticles showed an improvement of the kinetics of dissolution compared to that obtained for the active ingredient.

Keywords: coacervation, gum Arabic, microencapsulation, gelatin

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Authors: Satria B. Mahathma, Asri Hendrawati

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Background: Diabetes mellitus (DM) is a metabolic disorder syndrome characterized by chronic hyperglycemia. The number of people with diabetes rose from 108 million in 1980 to 422 million in 2014. In general, almost 90% of the prevalence of DM is type 2 DM which marked by insulin resistance and decreased receptor sensitivity. Aside from conventional antidiabetic therapy, the utilization of medicinal plants as alternative medicine has beneficial effects in diabetic patients. Flavonoid contents in radish leaves such as quercetin, pelargonidin, and kaempferol are thought to have antidiabetic activity on decreasing blood glucose levels by tricyclic nucleotide modulation of pancreatic beta cells and ameliorating insulin resistance. This study aimed to determine the effect of variant concentration of radish leaves ethanol extract on blood glucose levels in diabetic rats. Method: This study used pretest-posttest control group design by using 16 male Wistar rats which were induced type-2 diabetic by streptozotocin 60 mg/kg BW-nicotinamide 120 mg/kg BW intraperitoneally. Rats who had developed type-2 DM later divided randomly into 4 groups; negative control received placebo, positive control received glibenclamide 5 mg/kg BW/day, rats intervention I and intervention II received 100% and 50% of radish leaves ethanol extract, respectively. Treatments were administered orally for four weeks. The blood glucose levels were measured using the Enzymatic Colorimetric Test “GOD-PAP”. Data were analyzed by the dependent t-test for pretest-posttest intervention difference and one-way ANOVA followed by post hoc test to determine the significant difference of each treatment to obtain the significant data. Result: The result revealed that intervention group had lower blood glucose levels mean than control group which the lowest was intervention II group (negative control: 540,9 ± 191,7 mg/dl, positive control: 494, 97 ± 64,91 mg/dl, intervention I: 301,92 ± 165,70 mg/dl, and intervention II group: 276,1 ± 139,02 mg/dl. Intervention II group had the highest antidiabetic activity, followed by the intervention I group with the amount of decrease in blood glucose levels were -151,85 ± 77,43 mg/dl and -11,08 ± 186,62 mg/dl, however negative and positive control group didn’t have antidiabetic activity. The dependent t-test result showed there is a significant difference in decreasing blood glucose levels in the intervention II pretest-posttest intervention (p=0,03) while the other group didn’t. Data analyzed by one-way ANOVA also revealed the intervention II group significantly declined blood glucose levels compared to the negative and positive control group (p = 0,033 and p=0,032, respectively). Conclusion: There is a significant effect of radish leaves ethanol extract on blood glucose levels in streptozotocin-nicotinamide-induced diabetic rats with the optimal therapeutic effect at a concentration of 50%.

Keywords: blood glucose levels, medicinal plant, radish leaves, type-2 diabetes mellitus

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Authors: Sourabh Jain, Vikas Jain, Dharmendra Kumnar

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The present study investigated the antidiabetic potential of Cedrus deodara heart wood aqueous extract and its relationship in alloxan-induced diabetic rats. Aqueous extract of Cedrus deodara was found to reduce blood sugar level in alloxan induced diabetic rats. Reduction in blood sugar could be seen from 5th day after continuous administration of the extract and on 21st day sugar levels were found to be reduced by 40.20%. Oxidative stress produced by alloxan was found to be significantly lowered by the administration of Cedrus deodara aqueous extract (500 mg/kg). This was evident from a significant decrease in lipid per oxidation level in liver induced by alloxan. The level of Glutathione, Catalase, Superoxide dismutase and Glutathione-S-Transferase in liver, kidney and pancreas tissue were found to be increased significantly after drug administration. The results obtained in the present study suggest that the Cedrus deodara aqueous extract effectively and significantly reduced the oxidative stress induced by alloxan and produced a reduction in blood sugar level.

Keywords: Cedrus deodara, heartwood, antioxidant, anti-diabetic, anti-inflammatory

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Authors: T. Wresdiyati, S. Sa’diah, A. Winarto

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Diabetes mellitus (DM) is a metabolic disease that can be indicated by the high level of blood glucose. The objective of this study was to observe the antidiabetic properties of ethanolic extract of Indonesian Swietenia mahagoni Jacq. seed on the profile of pancreatic superoxide dismutase and β-cells in the alloxan- experimental diabetic rats. The Swietenia mahagoni seed was obtained from Leuwiliang-Bogor, Indonesia. Extraction of Swietenia mahagoni was done by using ethanol with maceration methods. A total of 25 male Sprague dawley rats were divided into five groups; (a) negative control group, (b) positive control group (DM), (c) DM group that was treated with Swietenia mahagoni seed extract, (d) DM group that was treated with acarbose, and (e) non-DM group that was treated with Swietenia mahagoni seed extract. The DM groups were induced by alloxan (110 mg/kgBW). The extract was orally administrated to diabetic rats 500 mg/kg/BW/day for 28 days. The extract showed hypoglycemic effect, increased body weight, increased the content of superoxide dismutase in the pancreatic tissue, and delayed the rate of β-cells damage of experimental diabetic rats. These results suggested that the ethanolic extract of Indonesian Swietenia mahagoni Jacq. seed could be proposed as a potential anti-diabetic agent.

Keywords: beta cells, diabetes, hypoglycemic, rat, Swietenia mahagoni

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Authors: Ravisinh Solanki, Ravi Patel, Chhaganbhai Patel

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Purpose: The purpose of this study is to develop a methodology for the risk assessment and evaluation of nitrosamine impurities in Glipizide antidiabetic formulations. Nitroso compounds, including nitrosamines, have emerged as significant concerns in drug products, as highlighted by the ICH M7 guidelines. This study aims to identify known and potential sources of nitrosamine impurities that may contaminate Glipizide formulations and assess their presence. By determining observed or predicted levels of these impurities and comparing them with regulatory guidance, this research will contribute to ensuring the safety and quality of combination antidiabetic drug products on the market. Factors contributing to the presence of genotoxic nitrosamine contaminants in glipizide medications, such as secondary and tertiary amines, and nitroso group-complex forming molecules, will be investigated. Additionally, conditions necessary for nitrosamine formation, including the presence of nitrosating agents, and acidic environments, will be examined to enhance understanding and mitigation strategies. Method: The methodology for the study involves the implementation of the N-Nitroso Acid Precursor (NAP) test, as recommended by the WHO in 1978 and detailed in the 1980 International Agency for Research on Cancer monograph. Individual glass vials containing equivalent to 10mM quantities of Glipizide is prepared. These compounds are dissolved in an acidic environment and supplemented with 40 mM NaNO2. The resulting solutions are maintained at a temperature of 37°C for a duration of 4 hours. For the analysis of the samples, an HPLC method is employed for fit-for-purpose separation. LC resolution is achieved using a step gradient on an Agilent Eclipse Plus C18 column (4.6 X 100 mm, 3.5µ). Mobile phases A and B consist of 0.1% v/v formic acid in water and acetonitrile, respectively, following a gradient mode program. The flow rate is set at 0.6 mL/min, and the column compartment temperature is maintained at 35°C. Detection is performed using a PDA detector within the wavelength range of 190-400 nm. To determine the exact mass of formed nitrosamine drug substance related impurities (NDSRIs), the HPLC method is transferred to LC-TQ-MS/MS with the same mobile phase composition and gradient program. The injection volume is set at 5 µL, and MS analysis is conducted in Electrospray Ionization (ESI) mode within the mass range of 100−1000 Daltons. Results: The samples of NAP test were prepared according to the protocol. The samples were analyzed using HPLC and LC-TQ-MS/MS identify possible NDSRIs generated in different formulations of glipizide. It was found that the NAP test generated a various NDSRIs. The new finding, which has not been reported yet, discovered contamination of Glipizide. These NDSRIs are categorised based on the predicted carcinogenic potency and recommended its acceptable intact in medicines. The analytical method was found specific and reproducible.

Keywords: NDSRI, nitrosamine impurities, antidiabetic, glipizide, LC-MS/MS

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Authors: Priyanka Mokashi, Aparna Khanna, Nancy Pandita

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Diabetes mellitus is a chronic metabolic disorder which will be the 7th leading cause of death by 2030. The current line of treatment for the diabetes mellitus is oral antidiabetic drugs (biguanides, sulfonylureas, meglitinides, thiazolidinediones and alpha-glycosidase inhibitors) and insulin therapy depending upon the type 1 or type 2 diabetes mellitus. But, these treatments have their disadvantages, ranging from the developing of resistance to the drugs and adverse effects caused by them. Alternative to these synthetic agents, natural products provides a new insight for the development of more efficient and safe drugs due to their therapeutic values. Enicostema littorale blume (A. Raynal) is a traditional Indian plant belongs to the Gentianaceae family. It is widely distributed in Asia, Africa, and South America. There are few reports on Swrtiamarin, major component of this plant for its antidiabetic activity. However, the antidiabetic activity of flavonoids from E. littorale and their mechanism of action have not yet been elucidated. Flavonoids have a positive relationship with disease prevention and can act on various molecular targets and regulate different signaling pathways in pancreatic β-cells, adipocytes, hepatocytes and skeletal myofibers. They may exert beneficial effects in diabetes by (i) improving hyperglycemia through regulation of glucose metabolism in hepatocytes; (ii) enhancing insulin secretion and reducing apoptosis and promoting proliferation of pancreatic β-cells; (iii) increasing glucose uptake in hepatocytes, skeletal muscle and white adipose tissue (iv) reducing insulin resistance, inflammation and oxidative stress. Therefore, we have isolated four flavonoid rich fractions, Fraction A (FA), Fraction B (FB), Fraction C (FC), Fraction D (FD) from crude alcoholic hot (AH) extract from E. littorale, identified by LC/MS. Total eight flavonoids were identified on the basis of fragmentation pattern. Flavonoid FA showed the presence of swertisin, isovitexin, and saponarin; FB showed genkwanin, quercetin, isovitexin, FC showed apigenin, swertisin, quercetin, 5-O-glucosylswertisin and 5-O-glucosylisoswertisin whereas FD showed the presence of swertisin. Further, these fractions were assessed for their antidiabetic activity on stimulating glucose uptake in insulin-resistant HepG2 cell line model (IR/HepG2). The results showed that FD containing C-glycoside Swertisin has significantly increased the glucose uptake rate of IR/HepG2 cells at the concentration of 10 µg/ml as compared to positive control Metformin (0.5mM) which was determined by glucose oxidase- peroxidase method. It has been reported that enhancement of glucose uptake of cells occurs due the translocation of Glut4 vesicles to cell membrane through IR/IRS1/AKT pathway. Therefore, we have studied expressions of three genes IRS1, AKT and Glut4 by real-time PCR to evaluate whether they follow the same pathway or not. It was seen that the glucose uptake rate has increased in FD treated IR/HepG2 cells due to the activation of insulin receptor substrate-1 (IRS1) followed by protein kinase B (AKT) through phosphoinositide 3-kinase (PI3K) leading to translocation of Glut 4 vesicles to cell membrane, thereby enhancing glucose uptake and insulin sensitivity of insulin resistant HepG2 cells. Hence, the up-regulation indicated the mechanism of action through which FD (Swertisin) acts as antidiabetic candidate in the treatment of type 2 diabetes mellitus.

Keywords: E. littorale, glucose transporter, glucose uptake rate, insulin resistance

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Authors: Meliani Samiha, Hassaine Sarah

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Figs are so much consumed in the Mediterranean region; they present a high nutritional value and also multiple therapeutic virtues. Our work contributes to the study of the antidiabetic activity of the common fig of the region of El Amra (AinDefla) Algeria. To do this, 20 Wistar rats female, divided into 4 lots, were used: Lot 1: 5 normal controls; Lot 2: 5 normal controls treated with dry fig juice at 20%; Lot 3: 5 diabetic controls; Lot 4: 5 diabetic controls treated with dry fig juice at 20%. The rats are rendered diabetic by intra-peritoneal injection of a streptozotocin solution. The blood glucose is measured after 1 hour, 2 hours, 3 hours and after 4 hours of the administration of the fig juice; it’s measured also on the 5th day, 8th day and 9th day of the beginning of the experiment. The determination of cholesterol and triglycerides blood is carried out at the beginning and the end of the study. On the 9th day, we recorded a very significant decrease of the blood sugar level of diabetic rats treated with dry fig juice. This blood glucose level normalized for 3 rats/5rats, we also recorded a decrease, but not significant, of cholesterol and triglycerides blood levels. In the short term (for 4 hours), an increase of blood sugar level, one hour after administration, for normal and diabetic rats. This increase is probably due to the high level of sugar content in the preparation. The blood glucose level is then corrected, four hours later. This may be the result of anti hyperglycemic effect of the active ingredients contained in the figs.

Keywords: antidiabetic, figs, hypoglycemia, streptozotocin

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Authors: Nondumiso Lushozi, Busisani Lembede, Eliton Chivandi

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Consumption of fructose increases the risk of obesity, nonalcoholic fatty liver disease (NAFLD) and metabolic syndrome in children. Zingerone which is found in ginger has antidiabetic and antiobesogenic properties. Therefore, the aim of the study was to investigate the potential of orally administered zingerone to protect growing Sprague-Dawley rats (mimicking growing children) against high-fructose diet-induced metabolic derangements. Forty, 21-day old female Sprague-Dawley rats were randomly allocated and administered the following four treatments for 12 weeks: group I: standard rat chow (SR) + plain water (PW) + plain gelatine cube (PC). group II: SR + 20% (w/v) fructose solution (FS) + PC. group III: SR + FS + 100 mg/kg/day of fenofibrate in gelatine cube. group IV: SR+ FS + 20 mg/kg/day of zingerone in gelatine cube. The rats’ triglyceride, cholesterol, insulin & adiponectin concentration, visceral fat liver lipid content, homoeostasis model assessment of insulin resistance (HOMA-IR) and ability to handle glucose were determined. Oral administration of zingerone significantly increased (P<0.001) visceral fat and liver lipid content (P<0.001), respectively. Results from the study revealed that administration of 20% fructose solution did not induce metabolic dysfunction, however the zingerone treatment increased visceral fat and liver lipid content, all these lipid abnormalities are typical features of the metabolic syndrome, therefore the current study suggests that zingerone has no effect on metabolic dysfunction in adolescent females.

Keywords: antidiabetic, metabolic syndrome, zingerone, antiobesogenic

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Authors: M. A. Munteanu, A. M. Lungu, A. I. Chivescu, V. Teodorescu, E. Tufanoiu, C. Nicolae, T. I. Nanea

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Introduction: Sodium-glucose co-transporter 2 inhibitors (SGLT2i), which were first developed as antidiabetic medications, have demonstrated numerous positive benefits on the cardiovascular system, especially in the prevention of heart failure (HF). HF is a challenging, multifaceted disease that needs all-encompassing therapy. It should not be viewed as a limited form of heart illness but rather as a systemic disease that leads to multiple organ failure and death. SGLT2i is an extremely effective tool for treating HF by using its pleiotropic effects. In addition to its use in patients with diabetes mellitus who are at high cardiovascular risk or who have already experienced a cardiovascular event, SGLT2i administration has been shown to have positive effects on a variety of HF manifestations and stages, regardless of the patient's presence of diabetes mellitus. Material and Methods: According to the guide, 110 patients (83 males and 27 females) with heart failure with mildly reduced ejection fraction (HFmrEF), with T2D and neoplasia, were enrolled in the prospective study. The structural and functional state of the left ventricle myocardium and ejection fraction was assessed through echocardiography. Patients were randomized to receive once-daily dapagliflozin 10 mg. Results: Patients with HFmrEF were divided into 3 subgroups according to age. 7% (8) patients aged < 45 years, 35% (28) patients aged between 46-59 years, and 58% (74) patients aged> 60 years. The most prevalent comorbidities were hypertension (43.1%), coronary heart disease (40%), and obesity (33.2%). Study drug discontinuation and serious adverse events were not frequent in the subgroups, in either men or women, until now. Conclusions: SGLT-2 inhibitors are a novel class of antidiabetic agents that have demonstrated positive efficacy and safety outcomes in the setting of HFmrEF. Until now, in our study, dapagliflozin was safe and well-tolerated irrespective of sex.

Keywords: diabetes mellitus type 2, Sodium-glucose co-transporters-2 inhibitors, heart failure, neoplasia

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Authors: P. Gayathri, G. P. Jeyanthi

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The bark of Polyalthia longifolia is used in ayurvedic system of medicine for the manangement of various ailments including diabetes mellitus. The bark of P. longifolia extracts was extracted using various polar and non-polar solvents and tested for inhibition of alpha-amylase and alpha-glucosidase among which the ethanolic extracts were found to be more potent. The ethanolic extracts of the bark were tested for the in vitro inhibition of alpha-amylase using starch as substrate and alpha-glucosidase using p-nitro phenyl alpha-D-gluco pyranoside as substrate to establish its in vitro antidiabetic effect. The mechanism of inhibition was determined by Dixon plot and Cornish-Bowden plot. The cytotoxic effect of the extract was tested on L6 and Vero cell-lines. The extract was partially purified by TLC. The individual effect of the ethanolic extract, TLC fractions and its combinatorial effect with insulin and glibenclamide on glucose uptake by rat hemi-diaphragm were studied.Results revealed that the ethanolic extracts of Polyalthia longifolia bark exhibited competitive inhibition of alpha-amylase and alpha-glucosidase. The extracts were also found not to be cytotoxic at the highest dose of 1 mg/mL. Glucose uptake study revealed that the extract alone and when combined with insulin, decreased the glucose uptake when compared to insulin control, however the purified TLC fractions exhibited significantly higher (p<0.05) glucose uptake by the rat hemi-diaphragm when compared to insulin. The study shows various possible mechanism of in vitro antidiabetic effect of the P. longifolia bark.

Keywords: alpha-amylase, alpha-glucosidase, dixon, cornish-bowden, L6 , Vero cell-lines, glucose uptake, polyalthia longifolia bark, ethanolic extract, TLC fractions

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Authors: Aditya Arya, Hairin Taha, Ataul Karim Khan, Nayiar Shahid, Hapipah Mohd Ali, Mustafa Ali Mohd

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This study has investigated the antidiabetic and antioxidant potential of Pseudovaria macrophylla bark extract on streptozotocin–nicotinamide induced type 2 diabetic rats. LCMS-QTOF and NMR experiments were done to determine the chemical composition in the methanolic bark extract. For in vivo experiments, the STZ (60 mg/kg/b.w, 15 min after 120 mg/kg/1 nicotinamide, i.p.) induced diabetic rats were treated with methanolic extract of Pseuduvaria macrophylla (200 and 400 mg/kg∙bw) and glibenclamide (2.5 mg/kg) as positive control respectively. Biochemical parameters were assayed in the blood samples of all groups of rats. The pro-inflammatory cytokines, antioxidant status and plasma transforming growth factor βeta-1 (TGF-β1) were evaluated. The histological study of the pancreas was examined and its expression level of insulin was observed by immunohistochemistry. In addition, the expression of glucose transporters (GLUT 1, 2 and 4) were assessed in pancreas tissue by western blot analysis. The outcomes of the study displayed that the bark methanol extract of Pseuduvaria macrophylla has potentially normalized the elevated blood glucose levels and improved serum insulin and C-peptide levels with significant increase in the antioxidant enzyme, reduced glutathione (GSH) and decrease in the level of lipid peroxidation (LPO). Additionally, the extract has markedly decreased the levels of serum pro-inflammatory cytokines and transforming growth factor beta-1 (TGF-β1). Histopathology analysis demonstrated that Pseuduvaria macrophylla has the potential to protect the pancreas of diabetic rats against peroxidation damage by downregulating oxidative stress and elevated hyperglycaemia. Furthermore, the expression of insulin protein, GLUT-1, GLUT-2 and GLUT-4 in pancreatic cells was enhanced. The findings of this study support the anti-diabetic claims of Pseudovaria macrophylla bark.

Keywords: diabetes mellitus, Pseuduvaria macrophylla, alkaloids, caffeic acid

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