Search results for: in vitro antileishmanial activity

Authors: Kriyapa lairungruang, Arunporn Itharat

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Limonia acidissima L. (LA) (Common name: wood apple, Thai name: ma-khwit) is a medicinal plant which has long been used in Thai traditional medicine. Its bark is used for treatment of diarrhea, abscess, wound healing and inflammation and it is also used in oral cancer. Thus, this research aimed to investigate antioxidant and cytotoxic activities of the LA bark extracts produced by various extraction methods. Different extraction procedures were used to extract LA bark for biological activity testing: boiling in water, maceration with 95% ethanol, maceration with 50% ethanol and water boiling of each the 95% and the 50% ethanolic residues. All extracts were tested for antioxidant activity using DPPH radical scavenging assay, cytotoxic activity against human laryngeal epidermoid carcinoma (HEp-2) cells and human oral epidermoid carcinoma (KB) cells using sulforhodamine B (SRB) assay. The results found that the 95% ethanolic extract of LA bark showed the highest antioxidant activity with EC50 values of 29.76±1.88 µg/ml. For cytotoxic activity, the 50% ethanolic extract showed the best cytotoxic activity against HEp-2 and KB cells with IC50 values of 9.55±1.68 and 18.90±0.86 µg/ml, respectively. This study demonstrated that the 95% ethanolic extract of LA bark showed moderate antioxidant activity and the 50% ethanolic extract provided potent cytotoxic activity against HEp-2 and KB cells. These results confirm the traditional use of LA for the treatment of oral cancer and laryngeal cancer, and also support its ongoing use.

Keywords: antioxidant activity, cytotoxic activity, Laryngeal epidermoid carcinoma, Limonia acidissima L., oral epidermoid carcinoma

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Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

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Oxadiazoles and their derivatives with thioether functionalities represent a new and exciting class of physiologically active heterocyclic compounds. Several molecules with these moieties play a vital role in pharmaceuticals because of their diverse biological activities. This paper describes a new class of 1,3,4- oxadiazole-2-thioethers with acetophenone, coumarin, and N-phenyl acetamide residues (S-alkylation), with the hope that the addition of various biologically active molecules will have a synergistic effect on anticancer activity. The structure of the synthesized title compounds was determined by the combined methods of IR, proton-NMR, carbon-13-NMR, and mass spectrometry. Further, all the newly prepared molecules were assessed against their antioxidant activity. Furthermore, four compounds were assessed for their molecular docking interactions and cytotoxicity activity. The synthesized derivatives have shown moderate antioxidant activity compared to the standard BHA. The IC50 of the tilted molecules (11b, 11c, 13b, and 14b) observed for in vitro anti-cancer activities were 11.20, 15.73, 59.61, and 27.66 g/ml at 72-hour treatment time against the A549 cell lines, respectively. The tested compounds' biological evaluation showed that 11b is the most effective molecule in the series.

Keywords: antioxidant activity, cytotoxicity activity, molecular docking, 1, 3, 4-Oxadiazole-2 thioether derivatives

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Authors: Isaac Samuel

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A study was conducted to determine the in-vitro degradation of selected Nigerian browse plants consumed by small ruminants on free range in northern guinea savannah region of Nigeria using in vitro gas production, proximate composition, fibre components, methane gas production and dry matter degradation as tools. The leaves samples of the selected browse plants were collected, processed and incubated using in vitro gas dry matter degradation techniques. Results obtained showed variation in the rate of degradation. The result obtained from chemical analysis showed that the CP content of A. occidentale (26.49%) was higher than F. thonningi (23.58%), M. indica (20.58%) and T. catappa (18.61%). Both ADF and NDF of A. occidentale (40.00 and 50.00) were as well higher than F. thonningi (20.00 and 40.00), M. indica (20.00 and 40.00) and T.catappa (20.00 and 42.00). Results from in vitro gas production however showed that T. catappa (23.67ml/DM) has a significantly higher (p<0.05) value than F.thonningi (20.67ml/DM), A. occidentale (16.67ml/DM), and M. indica(14.00ml/DM) at 72 hours of incubation. Methane gas production and in vitro gas production can be used to predict dry matter degradation and nutritive value of feedstuff for small ruminants. A. occidentale with the least methane gas production and highest crude protein (CP) content might have the most nutritive value among the browse plants investigated.

Keywords: in vitro, degradation, browse, gas production

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Authors: Karima Oldyerou, B. Meddah, A. Tirtouil

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The food borne infections have a significant impact on public health. Salmonella is the first bacterial cause, especially because of its general availability in the intestinal tract of poultry, pigs and cattle. This bacteria and essential oil of Laurus nobilis subject in this article. In vitro evaluation of the antibacterial activity shows a sensitivity of Salmonella spp. with a MIC of 2.5 mg.ml -1 in vivo after infection of wistar rats and administered orally this essential oil, microbiological results fecal material shows the antibacterial effect of this oil on Salmonella spp.

Keywords: Laurus nobilis, essential oil, salmonella, antibacterial activity, fecal matte

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Authors: John Carlo Combista, Jimbert Tan

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The orchid, Vanda tessellata was chosen by the researchers because of the presence of the constituents in the family Orchidaceae such as alkaloids, flavonoids and glycosides that might give an inhibition activity of the carbonic anhydrase enzyme. This study aimed to determine the in vitro inhibition of carbonic anhydrase of Vanda tessellata flower extract. With the use of modified colorimetric Maren T.H. (1960) method, the time in seconds each test solution changed its color after the rate of CO2 hydration were recorded. Two solvents were used: the semi-polar, 95% ethanol and the non-polar, dichloromethane solvents. The percent inhibition activity of carbonic anhydrase of the different concentrations of solvents ethanol (1%, 25% and 50%) and dichloromethane (1% and 10%) test solutions were determined. Results showed that the ethanol-based extract of Vanda tessellata in different concentrations showed an inhibitory effect while the dichloromethane-based extract of Vanda tessellata showed no inhibitory effect of carbonic anhydrase activity. For ethanol extract, the concentration with the highest activity was 50% followed by 25% which changed its color from red to yellow with an average time of 13.11 seconds and 11.57 seconds but 1% with an average time of 7.56 seconds did not exhibit an effect. The researchers recommend the isolation of the specific active constituents of Vanda tessellata that is responsible for the inhibitory effect of carbonic anhydrase enzyme. It is also recommended to utilize different blood types to observe different reactions to the inhibition of the carbonic anhydrase.

Keywords: carbonic anhydrase, inhibition, modified colorimetric Maren TH method, Vanda orchid

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Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

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Triazoles are basic five-membered ring heterocycles with an unsaturated, six-delocalized electron ring system. Since the dawn of click chemistry, triazoles have represented a functional heterocyclic core that has been the foundation of medicinal chemistry. The compounds with 1,2,3-triazole rings can be used in several fields, including medicine, organic synthesis, polymer chemistry, fluorescent imaging, horticulture, and industries, to name a few. Besides that, they found it to have health applications in the prevention and reduction of the risk of diseases, such as anti-cancer, antimicrobial, antiviral, and anti-inflammatory properties. Here, we present the synthesis of twelve 1,2,3-triazolyl chalcone derivatives (4a–l), which were produced in high yields by coupling substituted aldehydes and triazolyl acetophenone (3a–d) in ethanol. The title products were characterized by physicochemical, infrared, nuclear magnetic resonance, and mass spectral methods. The in vitro tests were used to evaluate the antioxidant and antimicrobial activity of each of the prepared molecules. The preliminary assessment and 2,2-diphenyl-1-picrylhydrazyl activity of the title compounds showed significantly higher antibacterial activity and moderate-to-good antifungal and antioxidant activities compared to their standards. This work presents the synthesis of triazolyl chalcone derivatives and their biological activity. Based on the findings, these compounds could be used as lead compounds in antimicrobial and antioxidant research in the future.

Keywords: antibacterial activity, antifungal activity, antioxidant activity, chalcone, 1, 2, 3-triazole

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Authors: Djebbar Atmani, Aghiles Karim Aissat, Nadjet Debbache-Benaida, Nassima Chaher-Bazizi, Dina Atmani-Kilani, Meriem Rahmani-Berboucha, Naima Saidene, Malika Benloukil, Lila Azib

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Medicinal plants are believed to be an important source for the discovery of potential antioxidant, anti-inflammatory and anti-diabetic substances. The present study was designed to investigate the neuroprotective, anti-inflammatory, anti-diabetic and anti-hyperuricemic potential of Pistacia lentiscus, as well as the identification of active compounds. The antioxidant potential of plant extracts against known radicals was measured using various standard in vitro methods. Anti-inflammatory activity was determined using the paw edema model in mice and by measuring the secretion of the pro-inflammatory cytokine, whereas the anti-diabetic effect was assessed in vivo on streptozotocin-induced diabetic rats and in vitro by inhibition of alpha-amylase. The anti-hyperuricemic activity was evaluated using the xanthine oxidase assay, whereas neuroprotective activity was investigated using an Aluminum-induced toxicity test. Pistacia lentiscus extracts and fractions exhibited high scavenging capacity against DPPH, NO. and ABTS+ radicals in a dose-dependent manner and restored blood glucose levels, in vivo, to normal values, in agreement with the in vitro anti-diabetic effect. Oral administration of plant extracts significantly decreased carrageenan-induced mice paw oedema, similar to the standard drug, diclofenac, was effective in reducing IL-1β levels in cell culture and induced a significant increase in urinary volume in mice, associated to a promising anti-hyperuricemic activity. Plant extracts showed good neuroprotection and restoration of cognitive functions in mice. HPLC-MS and NMR analyses allowed the identification of known and new phenolic compounds that could be responsible for the observed activities. Therefore, Pistacia lentiscus could be beneficial in the treatment of inflammatory conditions and diabetes complications and the enhancement of cognitive functions.

Keywords: Pistacia lentiscus, anti-inflammatory, antidiabetic, flavanols, neuroprotective

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Authors: M. G. Shehata, S. A. El Sohaimy, Marwa M. Abu-Serie, Nourhan M. Abd El-Aziz

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Probiotic strains can potentially be used as bio-preservatives and functional food supplement. Eight lactic acid bacteria strains (LAB) Lactobacillus brevis NRRL B-4527; Streptococcus thermophilus BLM 58; Pediococcusacidilactici ATCC 8042; Lactobacillus rhamnosus CCUG 1452; Lactobacillus curvatus ATCC 51436; Lactococcuslactis sub sp. lactisDSM 20481; Lactobacillus plantarum DMSZ 20079 and Lactobacillus plantarumTF103 were selected to screen the antioxidant, anticancer potential and probiotic properties. LAB strains exhibited good probiotic, antioxidant properties and showed antagonistic activity against food-borne pathogenic (Bacillus subtilis DB 100 host; Candida albicans ATCCMYA-2876; Clostridium botulinum ATCC 3584; Escherichia coli BA 12296; Klebsiellapneumoniae ATCC12296; Salmonella senftenberg ATCC 8400 and Staphylococcus aureus NCTC 10788). Further, in vitro probiotic properties of eight strains displayed excellent acid tolerance, bile tolerance, simulated gastrointestinal juice tolerance, in vitro adhesion ability for HT-29 cell line. The antioxidant effect of intracellular and cell-free extract of lactic acid bacteria strains was evaluated by various antioxidant assays, namely, resistance to hydrogen peroxide, DPPH radical scavenging, ABTS radical scavenging, and hydroxyl radical scavenging (HRS). The results showed that intracellular and cell-free supernatant of S. Thermophilus BLM 58, L. lactissubsp.lactis DSM 20481, P. acidilactici ATCC 8042, L. brevis NRRL B-4527 strains possess excellent antioxidant capacity. The intracellular of S. Thermophilus BLM 58 and P. acidilactici ATCC 8042 also showed excellent anticancer activity against Caco-2, MCF-7, HepG-2, and PC-3. Antioxidative property of selected lactic acid bacteria strains would be useful in the functional food manufacturing industry. They could beneficially affect the consumer by providing dietary source of antioxidants.

Keywords: anticancer activity, antioxidant activity, functional food, lactic acid bacteria, probiotic

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Authors: Eric Beyegue, Boris Azantza, Judith Laure Ngondi, Julius E. Oben

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Background: It is clearly that phytochemical constituents of plants in relation exhibit free radical scavenging, antioxidant and glycosylation properties. This study investigated the in vitro antioxidant and free radical scavenging, inhibited activities against α-amylase and invertase enzymes of stem bark extracts C. edulis (Olacaceae). Methods: Four extracts (hexane, dichloromethane, ethanol and aqueous) from the barks of C. edulis were used in this study. Colorimetric in vitro methods were using for evaluate free radical scavenging activity DPPH, ABTS, NO, OH, antioxidant capacity, glycosylation activity, inhibition of α-amylase and invertase activities, phenolic, flavonoid and alkaloid contents. Results: C. edulis extracts (CEE) had a higher scavenging potential on the 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (OH), nitrite oxide (NO), 2, 2-azinobis (3-ethylbenzthiazoline)-6-sulfonic acid (ABTS) radicals and glucose scavenging with the IC50 varied between 41.95 and 36694.43 µg/ml depending on the solvent of extraction. The ethanol extract of C. edulis stem bark (CE EtOH) showed the highest polyphenolic (289.10 + 30.32), flavonoid (1.12 + 0.09) and alkaloids (18.47 + 0.16) content. All the tested extracts demonstrated a relative high inhibition potential against α-amylase and invertase digestive enzymes activities. Conclusion: This study suggests that CEE exhibited higher antioxidant potential and significant inhibition potential against digestive enzymes.

Keywords: Coula edulis, antioxidant, scavenging activity, amylase, invertase

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Authors: Zelikha Labbani

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The in vitro isolated microspore culture is the most powerful androgenic pathway to produce doubled haploid plants in the short time. To deviate a microspore toward embryogenesis, a number of factors, different for each species, must concur at the same time and place. Once induced, the microspore undergoes numerous changes at different levels, from overall morphology to gene expression. Induction of microspore embryogenesis not only implies the expression of an embryogenic program, but also a stress-related cellular response and a repression of the gametophytic program to revert the microspore to a totipotent status. As haploid single cells, microspore became a strategy to achieve various objectives particularly in genetic engineering. In this communication we would show the most recent advances in the producing haploid embryos via in vitro isolated microspore culture.

Keywords: in vitro isolated microspore culture, success, haploid cells, bioinformatics, biomedicine

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Authors: H. Kadi, A. Moussaoui, A. Medah, N. Benayahia, Nahal Bouderba

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For thousands of years, Punica granatum L. has been used in traditional medicine all over the world and predate the introduction of antibacterial drugs. The aim of the present study was to investigate the antibacterial activity of aqueous and ethanolic extracts of Punica granatum L. bark obtained by decoction and maceration. The different extracts of Punica granatum L. (Lythraceae) bark have been tested for antibacterial activity against Gram-positive bacteria (Staphylococcus aureus, Bacillus stearothermophilus) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) by disc diffusion method. The ethanolic macerate extract showed the strong in vitro antibacterial activity against Pseudomonas aeruginosa with zone inhibition of 24.4 mm. However, the results tests by disc diffusion method revealed the effectiveness of ethanolic decoctate against Gram-positive bacteria (Staphylococcus aureus and Bacillus stearothermophilus) with diameter zone of inhibition varying with 21.1mm and 23.75 mm respectively.

Keywords: Punica granatum L. bark, antibacterial activity, maceration, decoction

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Authors: Amir Khaleghipour, Amirhossein Moghanian, Elhamalsadat Ghaffari

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Modified bioactive glass has been considered as a promising multifunctional candidate in bone repair and regeneration due to its attractive properties. The present study mainly aims to evaluate how the individual substitution of lithium (L-BG) and magnesium (M-BG) for calcium can affect the in vitro bioactivity of sol-gel derived substituted 58S bioactive glass (BG); and to present one composition in both of the 60SiO₂–(36-x)CaO–4P₂O₅–(x)Li₂O and 60SiO₂–(36-x)CaO–4P₂O₅–(x)MgO quaternary systems (where x= 0, 5, 10 mol.%) with improved biocompatibility, enhanced alkaline phosphatase (ALP) activity, and the most efficient antibacterial activity against methicillin-resistant Staphylococcus aureus bacteria. To address these aims, and study the effect of CaO/Li₂O and CaO/MgO substitution up to 10 mol % in 58S-BGs, the samples were characterized by X-ray diffraction, Fourier transform infrared spectroscopy, inductively coupled plasma atomic emission spectrometry and scanning electron microscopy after immersion in simulated body fluid up to 14 days. Results indicated that substitution of either CaO/ Li₂O and CaO/ MgO had a retarding effect on in vitro hydroxyapatite (HA) formation due to the lower supersaturation degree for nucleation of HA compared with 58s-BG. Meanwhile, magnesium had a more pronounced effect. The 3-(4, 5dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and alkaline phosphatase (ALP) assays showed that both substitutions of CaO/ Li₂O and CaO/ MgO up to 5mol % in 58s-BGs led to increased biocompatibility and stimulated proliferation of the pre-osteoblast MC3T3 cells with respect to the control. On the other hand, substitution of either Li or Mg for Ca in the 58s BG composition resulted in improved bactericidal efficiency against MRSA bacteria. Taken together, sample 58s-BG with 5 mol % CaO/Li₂O substitution (BG-5L) was considered as a multifunctional biomaterial in bone repair/regeneration with improved biocompatibility, enhanced ALP activity as well enhanced antibacterial efficiency against methicillin-resistant Staphylococcus aureus (MRSA) bacteria among all of the synthesized L-BGs and M-BGs.

Keywords: alkaline, alkaline earth, bioactivity, biomedical applications, sol-gel processes

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Authors: Yamani Amal, Lazaae Jamila, Elachouri Mostafa

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Plants and their active agents – especially polyphenols – may have a principal role in the treatment of diseases that result from the defect of physiological antioxidant mechanisms. Bryonia dioica is well known in Moroccan traditional medicine for alleviatin pain and traiting many diseases. We have focused on plant belonging to Cucurbitaceae Family from around the world to understand their therapeutic uses and their potential antioxidant activities Although several biological activities and Chemical composition of Bryonia dioica are well characterized, no direct, in vitro study, of this natural product examined the antioxydant effect of the extract from the roots of Bryonia dioica. The aim of this study was to determine in vitro antioxidant activity of the B.dioica root, using antioxidant analysis methods based on determination of Hydroxyradical Scavenging, 1,1-diphenyl-2-picrylhydrazine (DPPH) radical scavenging, Hydrogenperoxide Scavenging and Nitric Oxide Scavenging. In this study, it was demonstrated, that, B. dioica root extract showed excellent antioxidant properties. This investigation showed that the roots of this plant contain potent natural scavengers R. It may represent an interesting source of antioxidant phenolics that may favour the extension of their cultivation as new source of natural antioxidants in addition to containing high quality proteins for human or animal nutrition. Therefore, there is need for all stakeholders on the Morocco to strive towards taking advantage of our enormous biodiversity resources to free our people from diseases, abject poverty and stagnation.

Keywords: Morocco, bryoniadioica, in vitro, antioxydant

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Authors: Suhair Saleh, Ahmad Aljaberi

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Cationic lipid-mediated delivery of nucleic acids represents an exciting approach for developing therapeutically realistic gene medicines. Elucidation of the molecular and formulation requirements for efficient lipofection is a prerequisite to enhance the biological activity of such delivery systems. To this end, the in vitro lipofection activity of the ionizable asymmetric 1,2-dialkoylamidopropane-based derivatives bearing single primary amine group as the cationic head group was evaluated. The electrostatic interactions of these cationic lipids with plasmid DNA in physiologically relevant medium were investigated by means of gel electrophoresis retardation and Eth-Br quenching assays. The effect of the presence of the helper lipid on these interactions was evaluated. The physicochemical properties of these lipids in terms of bilayer fluidity and extent of ionization were investigated using fluorescence anisotropy and surface potential techniques, respectively. The results showed that only the active lipid, 1,2lmp[5], existed in a liquid crystalline state at physiological temperature. Moreover, the extent of ionization of this lipid in assemblies was significantly higher that it's saturated analogues. Inclusion of the helper lipid DOPE improved the encapsulation and association between 1,2lmp[5] and plasmid DNA, which was reflected by the significant boost of lipofection activity of the 1,2lmp[5]/DOPE formulation as compared to the lipid alone. In conclusion, membrane fluidity and sufficient protonation of ionizable cationic lipid are required for efficient association and encapsulation of plasmid DNA and promoting improved in vitro lipofection activity.

Keywords: cationic lipids, gene delivery, lipofection, membrane fluidity, helper lipids, surface potential

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Authors: Nattawit Thiapairat

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Multiple diseases have been linked to excessive levels of free radicals, which cause tissue or cell damage as a result of oxidative stress. Many plants are sources of high antioxidant activity. Derris scandens has a high amount of phenolic and flavonoid contents which demonstrated good biological activities. This study focused on the antioxidant activity of polyphenols extracted from D. scandens. This study performs total flavonoids content and various antioxidant assays, which were 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The total flavonoid content of D. scandens extract was determined and expressed as quercetin equivalents (QE)/g measured by the aluminum chloride colorimetric method. The antioxidant activity of D. scandens extract was also determined by DPPH and ABTS assays. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. The half-maximal inhibitory concentration (IC50) values for D. scandens extract from DPPH and ABTS assays were 41.79 μg/mL ± 0.783 and 29.42 μg/mL ± 0.890, respectively, in the DPPH assay. To conclude, D. scandens extract consists of a high amount of total phenolic content, which exhibits a significant antioxidant activity. However, further investigation regarding antioxidant activity such as SOD, ROS, and RNS scavenging assays and in vivo experiments should be performed.

Keywords: ABTS assay, antioxidant activity, Derris scandens, DPPH assays, total flavonoid content

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Authors: Nacera Baali, Zahia Belloum, Souad Ameddah, Fadila Benayache, Samir Benayache, Chantal Wrutniak-Cabello

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Allurement of herbs as health beneficial foods and as a source material for the development of new drugs, has led to greater furtherance in the study of herbal medicines during recent years. In the present study, in vitro antioxidant, free radical scavenging capacity, and hepatoprotective activity of butanolic extract from Genista quadriflora Munby (G.quadriflora) were evaluated using established in vitro models such as DPPH radical and hydrogen peroxide radical scavenging activities and antilipidperoxidation ability. Interestingly, the extract showed considerable in vitro antioxidant and free radical scavenging activities in a dose-dependent manner when compared to the standard antioxidant which verified the presence of antioxidant compound in extract tested. The hepatoprotective potential of G.quadriflora extract was also evaluated in male Wistar rats against paracetamol (APAP) induced liver damage. Therapy of G.quadriflora showed the liver protective effect on biochemical and histopathological alterations. Moreover, histological studies also supported the biochemical finding, that is, the maximum improvement in the histoarchitecture of the liver. Results revealed that G.quadriflora extract could protect the liver against APAP-induced oxidative damage by possibly increasing the antioxidant protection mechanism in rats. These findings are of great importance in view of the availability of the plant and its observed possible diverse applications in medicine and nutrition.

Keywords: genista quadriflora munby, antioxidant, liver, paracetamol, oxidative stress

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Authors: Khayra Zerrouki, Noureddine Djebli, Esra Eroglu, Afife Mat, Ozhan Gul

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Neurodegenerative diseases of the human brain comprise a variety of disorders that affect an increasing percentage of the population. Alzheimer’s disease (AD) is a complex, multifactorial, heterogeneous mental illness, which is characterized by an age-dependent loss of memory and an impairment of multiple cognitive functions, but this 10 last years it concerns the population most and most young. Hypericum perforatum has traditionally been used as an external anti-inflammatory and healing remedy for the treatment of swellings, wounds and burns, diseases of the alimentary tract and psychological disorders. It is currently of great interest due to new and important therapeutic applications. In this study, the chemical composition of methanolic extract of Hypericum perforatum (HPM) was analysed by using high performance liquid chromatography – diode array detector (HPLC-DAD). The in vitro antioxidant activity of HPM was evaluated by using several antioxidant tests. HSM exhibits inhibitory capacity against posphatidylcholine liposome peroxidation, induced with iron and ascorbic acid, scavenge DPPH and superoxide radicals and act as reductants. The cytotoxic activity of HSM was also determined by using MTT cell viability assay on HeLa and NRK-52E cell lines. The in vivo activity studies in Swiss mice were determined by using behavioral, memory tests and histological study. According to tests results HPM that may be relevant to the treatment of cognitive disorders. The results of chemical analysis showed a hight level of hyperforin and quercitin that had an important antioxidant activity proved in vitro with the DPPH, anti LPO and SOD; this antioxidant activity was confirmed in vivo after the non-toxic results by means of improvement in behavioral and memory than the reducing shrunken in pyramidal cells of mice brains.

Keywords: AlCl3, alzheimer, mice, neuroprotective, neurotoxicity, phytotherapy

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Authors: Ibrahim M. Labouta, Marwa H. El-Wakil, Hayam M. Ashour, Ahmed M. Hassan, Manal N. Saudi

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The receptor tyrosine kinase c-Met is an attractive target for therapeutic treatment of cancers nowadays. Among the wide variety of heterocycles that have been explored for developing c-Met kinase inhibitors, the 1,2,4-triazines have been rarely investigated, although they are well known in the literature to possess antitumor activities. Herein we describe the design and synthesis of a novel series of 1,2,4-triazine derivatives possessing N-acylarylhydrazone moiety and another series combining the 1,2,4-triazine scaffold to the well-known anticancer drug 6-MP in order to explore their “double-drug” effect. The synthesized compounds were evaluated for their in vitro antitumor activity against three c-Met addicted cancer cell lines (A549, HT-29 and MKN-45). Most compounds showed moderate to excellent antiproliferative activity and four compounds showed potent inhibitory activity more than the reference drug Foretinib against one or more cancer cell lines. The obtained results revealed that the potent compounds are highly selective to A549 (lung adenocarcinoma) cancer cell line. The c-Met kinase inhibitory activity of the potent derivatives is still under investigation. The present study clearly demonstrates that the 1,2,4-triazine core ring exhibits promising antitumor activity with potential c-Met kinase inhibitory activity.

Keywords: 1, 2, 4-triazine, antitumor, c-Met inhibitor, double-drug

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Authors: Chanasit Chaocharoenphat

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Hibiscus sabdariffa is a herbal plant that is commonly used for home remedies in Thailand. This study aims to determine the antioxidant activity of polyphenols, as oxidative stress plays a vital role in the development of cancer, and H. sabdariffa was used in this study. The total flavonoids content was determined using the aluminium chloride colourimetric method and expressed as quercetin equivalents (QE)/g and the antioxidant capacity of the flavonoids using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The IC50 values of H. sabdariffa extract were 167.14 μg/mL ± 0.843 and 77.59 μg/mL ± 0.798, respectively. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. To summarise, H. sabdariffa extract contains a high concentration of total flavonoids and exhibits potent antioxidant activity. However, additional antioxidant activity assays such as superoxide dismutase (SOD), reactive oxygen species (ROS), and reactive nitrogen species (RNS) scavenging assays and in vitro antioxidant experiments should be carried out to investigate the molecular mechanism of the compound.

Keywords: ABTS assay, antioxidant activity, Gracilaria fisheri, DPPH assays, total flavonoid content

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Authors: Friday A. Ogori, Ojotu M. Eke, Oneh J. Abu, Abraham T. Girgih

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B.aeqygtiaca del (Balanites aegyptiaca del) seed protein concentrate (APC) was hydrolyzed using different enzymes such as pepsin+pancreatin (PP), Alcalase (Alca), and Flavourzyme (Flav). The Alca has higher yield (100%) when compared to PP (83.23%) and Flav (62.90%). The hydrophobic amino acid and Sulphur containing amino acid (40.19%, 7.04%) in PP hydrolysate were higher compared to Alcalase (38.92%, 6.69%), Flavourenzyme (37.43%,6.35%), and APC (39.97%, 6.95%) samples. The PP has stronger DPPH, Hydroxyl radical quenching, Ferric reducing activity, and linoleic acid peroxidation activity, followed by the protein concentrate (APC) and Alcalase (Alca), while Flavourenzyme (Flav) derived hydrolysate was least in scavenging and inhibiting radical peroxidation properties. Flavourenzyme derived hydrolysate had stronger Ferric reducing antioxidant potential and metal chelating property. The result showed that the Alcalase hydrolysate has promising peptide yield, and PP hydrolysate had excellent amino acid residues and good in-vitro antioxidant potentials and could be a preferred ingredients in the nutraceutical and functional food emerging industries.

Keywords: balanites aegyptiaca del, protein concentrate, protein hydrolysates, enzymatic hydrolysis, antioxidants

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Authors: Mohammed Auwal Ibrahim, Aminu Mohammed

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Stigmasterol has previously been reported to possess antitrypanosomal activity using in vitro and in vivo models. However, the mechanism of antitrypanosomal activity is yet to be elucidated. In the present study, molecular docking was used to decipher the mode of interaction and binding affinity of stigmasterol to three known antitrypanosomal drug targets viz; adenosine kinase, ornithine decarboxylase and triose phosphate isomerase. Stigmasterol was found to bind to the selected trypanosomal enzymes with minimum binding energy of -4.2, -6.5 and -6.6 kcal/mol for adenosine kinase, ornithine decarboxylase, and triose phosphate isomerase respectively. However, hydrogen bond was not involved in the interaction of stigmasterol with all the three enzymes, but hydrophobic interaction seemed to play a vital role in the binding phenomenon which was predicted to be non-competitive like type of inhibition. It was concluded that binding to the three selected enzymes, especially triose phosphate isomerase, might be involved in the antitrypanosomal activity of stigmasterol but not mediated via a hydrogen bond interaction.

Keywords: antitrypanosomal, in silico, molecular docking, stigmasterol

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Authors: Ireneusz Majsterek, Dariusz Pytel, J. Alan Diehl

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PKR-like ER kinase (PERK) is serine/threonie endoplasmic reticulum (ER) transmembrane kinase activated during ER-stress. PERK can activate signaling pathways known as unfolded protein response (UPR). Attenuation of translation is mediated by PERK via phosphorylation of eukaryotic initiation factor 2α (eIF2α), which is necessary for translation initiation. PERK activation also directly contributes to activation of Nrf2 which regulates expression of anti-oxidant enzymes. An increased phosphorylation of eIF2α has been reported in Alzheimer disease (AD) patient hippocampus, indicating that PERK is activated in this disease. Recent data have revealed activation of PERK signaling in non-Hodgkins lymphomas. Results also revealed that loss of PERK limits mammary tumor cell growth in vitro and in vivo. Consistent with these observations, activation of UPR in vitro increases levels of the amyloid precursor protein (APP), the peptide from which beta-amyloid plaques (AB) fragments are derived. Finally, proteolytic processing of APP, including the cleavages that produce AB, largely occurs in the ER, and localization coincident with PERK activity. Thus, we expect that PERK-dependent signaling is critical for progression of many types of diseases (human cancer, neurodegenerative disease and other). Therefore, modulation of PERK activity may be a useful therapeutic target in the treatment of different diseases that fail to respond to traditional chemotherapeutic strategies, including Alzheimer’s disease. Our goal will be to developed therapeutic modalities targeting PERK activity.

Keywords: PERK kinase, small molecule inhibitor, neurodegenerative disease, Alzheimer’s disease

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Authors: Sarunpron Khruengsai, Patcharee Pripdeevech

Abstract:

This study aimed to investigate the fumigation activities of the volatile compounds produced by Trichoderma spp. against Fusarium oxysporum and F. proliferatum fungi that cause significant rot in fresh chilies. Two Trichoderma spp. were isolated from the leaves of Schefflera leucantha grown in Thailand and later identified as T. afroharzianum MFLUCC19-0090 and T. afroharzianum MFLUCC19-0091. Both in vitro and in vivo dual culture volatile assays were used to study the effects of the produced volatile compounds on mycelial growth. In vitro results showed that the volatile compounds produced by T. afroharzianum MFLUCC19-0090 significantly inhibited the growth of F. oxysporum, while the volatile compounds produced by T. afroharzianum MFLUCC19-0091 significantly inhibited the growth of F. proliferatum. The effectiveness of Trichoderma-derived volatile compounds in inhibiting the mycelial growth of the selected pathogens in the inoculated, fresh chili samples was further demonstrated in vivo. The volatile profiles of both Trichoderma spp. were characterized using gas chromatography-mass spectrometry. Seventy-three volatile compounds were detected from both strains. Among the major volatile compounds detected, phenyl ethyl alcohol was found to possess the strongest antifungal activity against both pathogens. The results support the possibility of using volatile compounds produced by T. afroharzianum MFLUCC19-0090 and T. afroharzianum MFLUCC19-0091 as alternative fumigants for preventing Fusarium rot of fresh chilies during the post-harvest period.

Keywords: antifungal activity, biocontrol, endophytic fungi, post-harvest

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Authors: Babak Qasemi-Panahi, Gholamali Moghaddam, Seyed-Abbas Rafat, Hossein Daghigh Kia, Mansoureh Movahedin, Reza Hadavi

Abstract:

The objective of this study was to determine the effects of IGF-I on ovine oocytes maturation and subsequent development of embryos derived from in vitro fertilization (IVF). In vitro maturation (IVM) of oocytes and in vitro culture (IVC) of embryos was conducted with or without 100 ng/mL IGF-1. In the IGF-I treated group, mean percentage of oocyte maturation was significantly higher than the control group (57.67 ± 3.04 versus 49.81 ± 3.04%, respectively, P < 0.05). However, in comparison with control group, there was no significant effect of IGF-1 on rates of cleavage, morula, and blastocyst formation (85% versus 84%; 63% versus 65%, and 40% to 39%, respectively). These data demonstrate that IGF-I has a positive effect on ovine oocyte maturation rate, but it has not the significant outcome on embryo development.

Keywords: ovine, IGF-I, IVM, ICSI

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Authors: M. Das, B. P. Sarma, G. Ahmed

Abstract:

Human diet can be a major source of antioxidants. Poly¬phenols, which are organic compounds present in the regular human diet, have good antioxidant property. Most of the diseases are detected too late and that cause irre¬versible damage to the body. Therefore food that forms the natural source of antioxidants can prevent free radi¬cals from damaging our body tissues. Dillenia indica and Garcinia penducalata are two major fruits, easily available in Assam, North eastern Indian state. In the present study, the in vitro antioxi¬dant properties of the fruits of these plants are compared as the decoction of these fruits form a major part of Assamese cuisine. DPPH free radical scavenging activity of the methanol, petroleum ether and water extracts of G. penducalata and D. indica fruits were carried out by the methods of Cotelle A et al. (1996). Different concentrations ranging from 10–110 ug/ml of the extracts were added to 100 uM of DPPH (2,2, Diphenyl-2-picryl hydrazyl) and the absor¬bance was read at 517 nm after incubation. Ascorbic acid was used as the standard. Different concentrations of the methanol, petroleum ether and water extracts of G. penducalata and D. indica fruits were mixed with sodium nitroprusside and incubated. Griess reagent was added to the mixtures and their optical density was read at 546 nm following the method of Marcocci et al. (1994). Ascorbic acid was used as the standard. In order to find the scavenging activity of the extracts against hydroxyl radicals, the method of Kunchandy & Ohkawa (1990) was followed.The superoxide scavenging activity of the methanol, petroleum ether and water extracts of the fruits was deter¬mined by the method of Robak & Gryglewski (1998).Six replicates were maintained in each of the experiments and their SEM was evaluated based on which, non linear regres¬sion (curve fit), exponential growth were derived to calculate the IC50 values of the SAWE and standard compounds. All the statistical analyses were done by using paired t test. The hydroxyl radical scavenging activity of the various extracts of D. indica exhibited IC50 values < 110 ug/ml concentration, the scavenging activity of the extracts of G. penducalata was surprisingly>110 ug/ml.Similarly the oxygen free radical scavenging activity of the different extracts of D. indica exhibited an IC50 value of <110 ug/ml but the methanolic extract of the same exhib¬ited a better free radical scavenging activity compared to that of vitamin C. The methanolic extract of D. indica exhibited an IC50 value better than that of vitamin C. The DPPH scavenging activities of the various extracts of D. indica and G. penducalata were <110 ug/ml but the methanolic extract of D. indica exhibited an IC50 value bet¬ter than that of vitaminc C.The higher amounts of phenolic content in the methanolic extract of D. indica might be one of the major causes for its enhanced in vitro antioxidant activity.The present study concludes that Dillenia indica and Garcinia penducalata both possesses anti oxidant activi¬ties. The anti oxidant activity of Dillenia indica is superior to that of Garcinia penducalata due to its higher phenolic content

Keywords: antioxidants, free radicals, phenolic, scavenging

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Authors: Maryam Nejat Dehkordi, Per Lincoln, Hassan Momtaz

Abstract:

Interaction of Schiff base complexes of iron and manganese (iron [N, N’ Bis (5-(triphenyl phosphonium methyl) salicylidene) -1, 2 ethanediamine) chloride, [Fe Salen]Cl, manganese [N, N’ Bis (5-(triphenyl phosphonium methyl) salicylidene) -1, 2 ethanediamine) acetate) with DNA were investigated by spectroscopic and isothermal titration calorimetry techniques (ITC). The absorbance spectra of complexes have shown hyper and hypochromism in the presence of DNA that is indication of interaction of complexes with DNA. The linear dichroism (LD) measurements confirmed the bending of DNA in the presence of complexes. Furthermore, isothermal titration calorimetry experiments approved that complexes bound to DNA on the base of both electrostatic and hydrophobic interactions. Furthermore, ITC profile exhibits the existence of two binding phases for the complex. Antibacterial activity of ligand and complexes were tested in vitro to evaluate their activity against the gram positive and negative bacteria.

Keywords: Schiff base complexes, ct-DNA, linear dichroism (LD), isothermal titration calorimetry (ITC), antibacterial activity

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Authors: Abdelkrim Cheriti, Mebarka Belboukhari, Nasser Belboukhari

Abstract:

Launaea Cass. is a small genus of the family Asteraceae (tribe Lactuceae, subtribe Sonchinae), consisting of 54 species, of which 9 are presented in the flora of Algeria and is mainly distributed in the South Mediterranean, Africa and SW Asia. Plants in the Launaea genus have been used ethnobotanically as bitter stomachic, for treating diarrhea, gastrointestinal tracts, as anti-inflammatory, for skin diseases, treatment of infected wounds, hepatic pains, children fever, as soporific, lactagogue, diuretic and as insecticidal. Antioxidants are vital substances, which possess the ability to protect the body from damages caused by free radical induced oxidative stress. A variety of free radical scavenging antioxidants is found in a number of dietary sources. The main objective of this study focused on the screening of antioxidant activity of Launaea nudicaulis (Asteraceae) extracts. The in vitro antioxidant activity was investigated with DPPH radical scavenging assay. The quantitative evaluation of DPPH scavenging activity showed that n-BuOH and EtOAc extracts are the most active extracts with a percentage of antiradical activity of 89,62% and 71,57% respectively.

Keywords: Launaea, phytochemical, South Algeria, Sahara, endemic specie

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Authors: Mthokozisi B. C. Simelane

Abstract:

Despite the various efforts by governmental and non-governmental organizations aimed at eradicating the disease, malaria is said to kill a child every 30 seconds. Traditional healers use different concoctions prepared from medicinal plants to treat malaria. In the quest to bio-prospect plant-derived triterpenes for anti-malaria activity, we report here the in vivo antiplasmodial activity of ursolic acid acetate (ursolic acid isolated from dichloromethane extract of Mimusops caffra was chemically modified to its acetate derivative). The transdermal administration of ursolic acid acetate (UAA) dose dependently showed complete inhibition of the parasites’ growth at the highest concentration of 400 mg/kg after 15 days of Plasmodium berghei infection. UAA prevented the in vitro aggregation of MDH but did not prevent the expression of PfHsp 70 in E. coli XL1 blue cells. It, however, enhanced PfHsp70 ATPase activity with the specific activity of 65 units (amount of phosphate released 73.83 nmolPi/min.mg). Ursolic acid acetate prevented the formation of hemozoin (60 ± 0.02% at 6 mg/ml). The results suggest that Ursolic acid acetate possesses potential anti-malaria properties.

Keywords: Mimusops caffra, ursolic acid acetate, hemozoin, Malaria

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Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

Abstract:

Pyrazole is an aromatic five-membered heterocycle with two nitrogen and three carbon atoms in its ring structure. According to the literature, pyrazoline, pyrazole, and thiazole-containing moieties are found in various drug structures and are responsible for nearly all pharmacological effects. The pyrazoline linked to pyrazole moiety carbothioamides was synthesized via the reaction of pyrazole-bearing chalcones (3-(5-chloro-3-methyl-¹-phenyl-1H-pyrazol-4-yl)-¹-(substituted aryl) prop-2-ene-¹-one derivatives) with a nucleophile thiosemicarbohyrazide by heating in ethanol using fused sodium acetate as a catalyst. Then the carbothioamide derivatives were converted into the pyrazoline hybrid to pyrazole and thiazole derivatives by condensing with substituted phenacyl bromide in alcohol in a basic medium. Next, the chemical structure of the newly synthesized molecules was confirmed by IR, 1H-NMR, and mass spectral data. Further, they were screened for their in vitro antioxidant activity. Compared to butylated hydroxy anisole (BHA)., the antioxidant data showed that the synthesized compounds had good to moderate activity.

Keywords: pyrazoline-pyrazole carbothioamide derivatives, pyrazoline-pyrazole-thiazole derivatives, spectral studies, antioxidant activity

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Authors: Zelikha Labbani

Abstract:

The In Vitro isolated micro spore culture is the most powerful androgenic pathway to produce doubled haploid plants in the short time. To deviate a micro spore toward embryogenesis, a number of factors, different for each species, must concur at the same time and place. Once induced, the micro spore undergoes numerous changes at different levels, from overall morphology to gene expression. Induction of micro spore embryogenesis not only implies the expression of an embryogenic program, but also a stress-related cellular response and a repression of the gametophytic program to revert the microspore to a totipotent status. As haploid single cells, micro spore became a strategy to achieve various objectives particularly in genetic engineering. In this study we would show the most recent advances in the producing haploid embryos via In Vitro isolated micro spore culture.

Keywords: haploid cells, In Vitro isolated microspore culture, success

Procedia PDF Downloads 586