Search results for: alkaloid

Authors: Ana C. Ramos Valdivia, Ileana Vera-Reyes, Ariana A. Huerta-Heredia

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The conditions of biotic and abiotic stress in plants can lead to the generation of high amounts of reactive oxygen species (ROS), which leads through a signaling cascade and second messengers to different antioxidant defense responses including the production of secondary metabolites. A limited number of species of plants like Uncaria tomentosa (cat claw) typical of the Amazon region produce monoterpenoid oxindole alkaloids (MOA) such as isopteropodine, mitraphylline, rhynchophylline and its isomers. Moreover, in cultivated roots, the glucoindole alkaloid 3α-dihydrocadambine (DHC) is also accumulated. Several studies have demonstrated that MAO has antioxidant properties and possess important pharmacological activities such as antitumor and immunostimulant while DHC, has hypotensive and hypolipidemic effects. In order the study the regulatory concerns operating in MAO production, the links between oxidative stress and antioxidant alkaloid production in U. tomentosa root cultures were examined. Different amount of hydrogen peroxide between 0.2 -1.0 mM was added to 12 days old roots cultures showing that, this substance had a differential effect on the production of DHC and MOA whereas the viability remained in 80% after six days. Addition of 0.2 mM hydrogen peroxide increased approximately 65% MAO and DHC production (0,540 ± 0.018 and 0.618 ± 0.029 mg per g dry weight, respectively) relative to the control. On contrast, after the addition of 0.6 mM and 1 mM hydrogen peroxide, DHC accumulation into the roots gradually decreased to 53% and 93% respectively, without changes in MAO concentration, which was in relation to a twice increase of the intracellular hydrogen peroxide content. On the other hand, concentrations of DHC (0.1, 0.5 and 1.0 mM in methanol) demonstrated free-radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. The calculated IC50 for all tested concentrations was 0.180 mg per ml (0.33 mM) while the calculated TE50 was 276 minutes. Our results suggest that U. tomentosa root cultures both MAO and DHC have antioxidant capacities and respond to oxidative stress with a stimulation of their production; however, in presence of a higher concentration of ROS into the roots, DHC could be oxidized.

Keywords: monoterpenoid indole alkaloid, oxidative stress, root cultures, uncaria tomentosa

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Authors: Rajesh A. Rane, Shital S. Naphade, Rajshekhar Karpoormath

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Thiozolidin-4-one, a mimic of thiazolobenzimidazole (TBZ) has drawn many attentions due to its potent and selective inhibition against the HIV-1 and low toxicity by binding to the allosteric site of the reverse transcriptase (RT) as a non-nucleoside RT inhibitor (NNRTI). Similarly, marine bromopyrrole alkaloids are well known for their diverse array of anti-infective properties. Hence, we have reported synthesis and in vitro HIV-1 RT inhibitory activity of a series of 4-thiazolidinone-bromopyrrole alkaloid hybrids tethered with amide linker. The results of in vitro HIV-1 RT kit assay showed that some of the compounds, such as 4c, 4d, and 4i could effectively inhibit RT activity. Among them, compounds 4c having 4-chlorophenyl substituted 4-thiazolidione ring was the best one with the IC50 value of 0.26 µM. The sturdy emerges with key structure-activity relationship that pyrrole-NH-free core benefited inhibition against HIV-1 RT inhibition. This study identified conjugate 4c with potent activity and selectivity as promising compound for further drug development to HIV.

Keywords: antiviral drugs, bromopyrrole alkaloids, HIV-1 RT inhibition, 4-thiazolidinone

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Authors: Kakali Bhadra

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Binding of small molecules to DNA and recently to RNA, continues to attract considerable attention for developing effective therapeutic agents for control of gene expression. This work focuses towards understanding interaction of harmalol, a dihydro beta-carboline alkaloid, with different nucleic acid motifs viz. double stranded CT DNA, single stranded A-form poly(A), double-stranded A-form of poly(C)·poly(G) and clover leaf tRNAphe by different spectroscopic, calorimetric and molecular modeling techniques. Results of this study converge to suggest that (i) binding constant varied in the order of CT DNA > poly(C)·poly(G) > tRNAphe > poly(A), (ii) non-cooperative binding of harmalol to poly(C)·poly(G) and poly(A) and cooperative binding with CT DNA and tRNAphe, (iii) significant structural changes of CT DNA, poly(C)·poly(G) and tRNAphe with concomitant induction of optical activity in the bound achiral alkaloid molecules, while with poly(A) no intrinsic CD perturbation was observed, (iv) the binding was predominantly exothermic, enthalpy driven, entropy favoured with CT DNA and poly(C)·poly(G) while it was entropy driven with tRNAphe and poly(A), (v) a hydrophobic contribution and comparatively large role of non-polyelectrolytic forces to Gibbs energy changes with CT DNA, poly(C)·poly(G) and tRNAphe, and (vi) intercalated state of harmalol with CT DNA and poly(C)·poly(G) structure as revealed from molecular docking and supported by the viscometric data. Furthermore, with competition dialysis assay it was shown that harmalol prefers hetero GC sequences. All these findings unequivocally pointed out that harmalol prefers binding with ds CT DNA followed by ds poly(C)·poly(G), clover leaf tRNAphe and least with ss poly(A). The results highlight the importance of structural elements in these natural beta-carboline alkaloids in stabilizing different DNA and RNA of various motifs for developing nucleic acid based better therapeutic agents.

Keywords: calorimetry, docking, DNA/RNA-alkaloid interaction, harmalol, spectroscopy

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Authors: Venoos Iman, Suzita Mohd Noor, Syam Mohan, Mohamad Ibrahim Noordin

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Girinimbine, a carbazole alkaloid was isolated from the stem bark and root of Murraya koenigii and its structure and purity was identified by HPLC and LC-MS. Here we report that Girinimbine strongly inhibit angiogenesis activity both in vitro and in vivo. MTT result showed that girinimbine inhibits cell proliferation of the HUVECS cell line in vitro. Result of endothelial cell invasion, migration, tube formation and wound healing assays also demonstrated significant time and does dependent inhibition by girinimbine. Moreover, girinibine mediates its anti-angiogenic activity through up- and down-regulation of angiogenic and anti-aniogenic proteins. Furthermore, anti-angiogenic potential of girinimbine was evidenced in vivo on zebrafish model. Girinimbine inhibited neo-vessels formation in zebrafish embryos during 24 hours exposure time. Together, these results demonstrated for the first time that girinimbine could effectively suppress angiogenesis and strongly suggest that it might be a novel angiogenesis inhibitor.

Keywords: anti-angiogenic, carbazole alkaloid, girinimbine, zebrafish

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Authors: Tiah Rachmatiah, Subaryanti

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Plants of Lauraceae family are known to contain many chemical compounds which have potential bioactivity such as alkaloids, flavonoids, lactones, terpenes, etc. Actinodaphne macrophylla and Nectandra angustifolia are two species from Lauraceae. A previous study on the crude alkaloidal extract from the bark of Act. macrophylla and n-hexane extract from the bark of N. angustifolia showed antiplasmodial activity against Plasmodium falciparum. The study was continued to find antiplasmodial active compounds from the two extracts. The materials were obtained from Bogor Botanical Garden, West Java, Indonesia. Crude alkaloidal extract of Act. macrophylla was prepared by maceration in dichloromethane after moistened with NH4OH 25% and n-hexane extract of N. angustifolia was prepared by maceration in n-hexane. A major compound was isolated by column chromatography using silica gel and a mixture of CH2Cl2 and methanol as a gradient solvent system for the alkaloidal extract and mixture of n-hexane and ethyl acetate for n-hexane extract. Fine white needle crystals were obtained from the alkaloidal extract and rod crystals from n-hexane extract. Molecular structure of the compounds was determined by analysis of spectra of NMR, IR, MS and compared by references. In vitro bioactivity test of the compound was performed against Plasmodium falciparum. The results showed that the bark of Act. macrophylla contained an aporphine alkaloid, actinodaphnine, that had activity against P. falciparum with IC50 value of 0.095 µg/mL and the bark of N. angustifolia contained a lignan compound, sesamine, with IC50 of 0.122 µg/mL.

Keywords: actinodaphne macrophylla, alkaloid, antiplasmodial, lauraceae, lignan, nectandra angustifolia

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Authors: Leonardo Parra, Daniel Martínez, Jorge Pizarro, Fernando Ortega, Manuel Chacón-Fuentes, Andrés Quiroz

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Control of Dalaca pallens or blackworms, one of the most important hypogeous pest in grassland in southern Chile, is based on the use of broad-spectrum insecticides such as organophosphates and pyrethroids. However, the rapid development of insecticide resistance in field populations of this insect and public concern over the environmental impact of these insecticides has resulted in the search for other control methods. Specifically, the use of endophyte fungi for controlling pest has emerged as an interesting and promising strategy. Endophytes from ryegrass (Lolium perenne), establish a biotrophic relationship with the host, defined as mutualistic symbiosis. The plant-fungi association produces alkaloids where peramine is the main toxic substance against Listronotus bonariensis, the most important epigean pest of ryegrass. Nevertheless, the effect of peramina on others pest insects, such as D. pallens, to our knowledge has not been studied, and also its possible metabolization in the body of the larvae. Therefore, we addressed the following research question: Do larvae of D. pallens store peramine after consumption of ryegrass endophyte infected (E+)? For this, specimens of blackworms were fed with ryegrass plant of seven experimental lines and one commercial cultivar endophyte free (E-) sown at the Instituto de Investigaciones Agropecuarias Carillanca (Vilcún, Chile). Once the feeding period was over, ten larvae of each treatment were examined. Individuals were dissected, and their gut was removed to exclude any influence of remaining material. The rest of the larva's body was dried at 60°C by 24-48 h and ground into a fine powder using a mortar. 25 mg of dry powder was transferred to a microcentrifuge tube and extracted in 1 mL of a mixture of methanol:water:formic acid. Then, the samples were centrifuged at 16,000 rpm for 3 min, and the supernatant was colected and injected in the liquid chromatography of high resolution (HPLC). The results confirmed the presence of peramine in the larva's body of D. pallens. The insects that fed the experimental lines LQE-2 and LQE-6 were those where peramine was present in high proportion (0.205 and 0.199 ppm, respectively); while LQE-7 and LQE-3 obtained the lowest concentrations of the alkaloid (0.047 and 0.053 ppm, respectively). Peramine was not detected in the insects when the control cultivar Jumbo (E-) was tested. These results evidenced the storage and metabolism of peramine during consumption of the larvae. However, the effect of this alkaloid present in 'future ryegrass cultivars' (LQE-2 and LQE-6) on the performance and survival of blackworms must be studied and confirmed experimentally.

Keywords: blackworms, HPLC, alkaloid, pest

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Authors: Rozalina Keremedchieva, Ivan Svinyarov, Milen G. Bogdanov

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In continuation of a research project on the application of ionic liquids (ILs) as an alternative to the conventional organic solvents used in the recovery of value added chemicals of industrial interest1-3 we developed a procedure for back extraction and isolation in pure form of the biologically active alkaloid glaucine from IL-based aqueous solutions. One of the approaches applied was the formation of two-phase systems (IL-ATPS) by the addition of kosmotropic salts to the plant extract. The ability of the salts (Na2CO3, MgSO4, (NH4)2SO4, NaH2PO4) to induce the formation of two-phase systems and the influence of pH value on the partition coefficients of glaucine was comprehensively studied. As a result, it was found that the target alkaloid is preferably partitioned into the IL-rich phase regardless of the pH value of the medium and thus shows the inapplicability of the approach used for the isolation of the target compound from the ionic liquid. However, the results obtained can be used as a platform for the development of an analytical method for the quantitative determination of low concentrations of glaucine in biological samples. We further examined the ability of a series of organic solvents such as diethyl ether, Tert-butylmethyl ether, ethyl acetate, butyl acetate, toluene, chloroform, dichloromethane to recover glaucine form raw IL-based aqueous extracts. Optimal conditions for quantitative extraction of glaucine into chloroform were found from which, after removal of the solvent and subsequent recrystallization from ethanol, the target compound was isolated in a high purity as a hydrobromide salt – The form in which it entrance as an active ingredient in various medicines.

Keywords: natural products, ionic liquids, solid-liquid extraction, liquid-liquid extraction

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Authors: Thaís T. Valério Caetano, Lívia de Carvalho Ferreira, João Máximo De Siqueira, Carlos Alexandre Carollo, Arthur Ladeira Macedo, Vanessa C. Stein

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Nicotiana glauca, commonly known as wild tobacco or tobacco bush, belongs to the Solanaceae family. It is native to South America but has become naturalized in various regions, including Australia, California, Africa, and the Mediterranean. N. glauca is listed in the Global Invasive Species Database (GISD) and the Invasive Species Compendium (CABI). It is known for producing pyridine alkaloids, including anabasine, which is highly toxic. Anabasine is predominantly found in the leaves and can cause severe health issues such as neuromuscular blockade, respiratory arrest, and cardiovascular problems when ingested. Mistaken identity with edible plants like spinach has resulted in food poisoning cases in Israel and Brazil. Anabasine, a minor alkaloid constituent of tobacco, may contribute to tobacco addiction by mimicking or enhancing the effects of nicotine. Therefore, it is essential to investigate the production pattern of anabasine and its relationship to the developmental stages of the plant. This study aimed to establish the relationship between the phenological plant age, cultivation place, and the increase in anabasine concentration, which can lead to human intoxication cases. In this study, N. glauca plants were collected from three different rural areas in Brazil during a year to examine leaves at various stages of development. Samples were also obtained from cultivated plants in Marilândia, Minas Gerais, Brazil, as well as from Divinópolis, Minas Gerais, Brazil, and Arraial do Cabo, Rio de Janeiro, Brazil. In vitro cultivated plants on MS medium were included in the study. The collected leaves were dried, powdered, and stored. Alkaloid extraction was performed using a methanol and water mixture, followed by liquid-liquid extraction with chloroform. The anabasine content was determined using HPLC-DAD analysis with nicotine as a standard. The results indicated that anabasine production increases with the plant's development, peaking in adult leaves during the reproduction phase and declining afterward. In vitro, plants showed similar anabasine production to young leaves. The successful adaptation of N. glauca in new environments poses a global problem, and the correlation between anabasine production and the plant's developmental stages has been understudied. The presence of substances produced by the plant can pose a risk to other species, especially when mistaken for edible plants. The findings from this study shed light on the pattern of anabasine production and its association with plant development, contributing to a better understanding of the potential risks associated with N. glauca and the importance of accurate identification.

Keywords: alkaloid production, invasive species, nicotiana glauca, plant phenology

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Authors: Ewon Kaliyadasa, U. L. B. Jayasinghe, S. E. Peiris

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Ashwagandha (Withania sominifera Duanal) is an important medicinal herb belongs to family Solanaceae. This plant has raised its popularity after discovering anti stress and sex stimulating properties that mainly due to the presence of biologically active alkaloid compounds. Therefore it is vital to adapt to a proper agro technological package that ensure optimum growth of ashwagandha to obtain the finest quality without degrading pharmacologically active constituents. Organic and inorganic fertilizer mixtures were combined with direct seeding and transplanting as four different treatments in this study. Tuber fresh and dry weights were recorded up to twelve months starting from two months after sowing (MAS) while shoot height, root length, number of leaves, shoot fresh and dry weights and root: shoot ratio up to 6MAS. Results revealed that growth of ashwagandha was not affected significantly by method of planting or type of fertilizer or its combinations during most of the harvests. However, tubers harvested at 6MAS recorded the highest dry tuber weight per plant in all four treatments compared to early harvests where two direct seeded treatments are the best. Chemical comparison of these two treatments, direct seeding coupled with organic and inorganic fertilizer shown that direct seeding with organic treatment recorded the highest values for alkaloid and withaferine A content with lower percentage of fiber. Further these values are in concurring with the values of commercially available tuber samples. Having considered all facts, 6MAS can be recommended as the best harvesting stage to obtain high quality tubers of ashwagandha under local conditions.

Keywords: alkaloids, direct seeding, dry tuber weight, inorganic fertilizer, organic fertilizer, transplanting, withaferine a

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Authors: João Pedro Zanella, Michel J. O. Fagundes

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Introduction: Drug use has been practised by humans universally for millennia, not excluding any population from these habits, however, the rampant drug use is a global concern due to the harm that affects the health of the world population. In this sense, it is observed the reduction of lasting and effective public policies for the resolution, increasing the demand for treatment services. With this comes ibogaine, an alkaloid derived from the root of an African bush (Tabernanthe Iboga), found mostly in Gabon and used widely by the native Bwiti population in rituals, and also other social groups, which demonstrates efficacy against chemical dependence, psychic and emotional disorders, opioid withdrawal was first confirmed by a study in rats done by Michailo Dzoljic and associates in 1988 and again in 1994. Methods: A brief description of the plant, its neurohumoral potential and the effects caused by ingested doses, in a simplified and objective way, will be discussed in the course of this abstract. Results: Ibogaine is not registered or passed by Anvisa, regarding safety and efficacy, and cannot be sold in Brazil. Its illegal trade reaches R$ 5 thousand for a session with the proceeds of the root, and its effect can last up to 72 hours, attributing Iboga's psychoactive effects to the alkaloid called ibogaine. The shrub where Ibogaine is located has pink and yellow flowers, and its fruit produced does not have psychoactive substances, but its root bark contains 6 to 7% indolic alkaloids. Besides extraction from the iboga plant, ibogaine hydrochloride can be semisynthesized from voacangine, another plant alkaloid that acts as a precursor. Its potential has the ability to perform multiple interactions with the neurotransmitter system, which are closely associated with addiction, including nicotinic, opioid and serotoninergic systems. Studies carried out by Edwards found that the doses administered of Iboga should be determined by a health professional when its purpose is to treat individuals for dependence on other drugs. Its use in small doses may cause an increase in sensibility, impaired vision and motor alterations; in moderate quantities, hallucinations, motor and neurological alterations and impaired vision; in high quantities it may cause hallucinations with personal events at a deeper level lasting up to 24 hours or more, followed by motor and visual alterations. Conclusion: The product extracted from the Iboga plant is of great importance in controlling addiction, reducing the need for the use of narcotics by patients, thus gaining a space of extreme importance in the treatment of users of psychoactive substances. It is remarkable the progress of the latest’s research about the usefulness of Ibogaine, and its benefits for certain treatments, even with the restriction of its sale in Brazil. Besides this, Ibogaine has an additional benefit of helping the patient to gain self-control over their destructive behaviours.

Keywords: alkaloids, dependence, Gabon, ibogaine

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Authors: Hesti Ghassani, Tessa Septiadi

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In the world we live on today, young generation highly influences the future of a nation. We have to concern that the condition of the country in 20 years later depending by the character of young adults these days. Therefore, it is important that we have to support and control the teenagers especially in one of developing countries in which I live in: Indonesia. Indonesia is a home to 240 million people. It diverse in languages, cultures, as well as attitudes. The differences among each individual lead us to think that there is something we have to take care of. It is necessary to pay attention to the nutrition consumed by the nation. We initiate to control the food consumed by young generation as early as a primary students. Nutrition affects the immune of the body, neuron system, and, most importantly brain. One of the nutrition that has to be fulfilled is milk. However, most of the population in Indonesia isn’t aware of the importance of consuming milk as their daily basis. We’ve formed an innovation called the Brilliant Candy which is affordable and rich in nutrition. So that is why the paper made by literature study to solve the problem with effective ways using available resources, practice and cheap. Brilliant Candy consists of Centella asiatica extract mixed with Soy milk. Centella asiatica contains of alkaloid which give the energy to brain and circulate oxygen. Based on the research of Sathya and Ganga, Centella asiatica can increase the intelligence. Indeed, Centella asiatica can relieve stress, and help us in staying focus. Soy milk is a kind of milk which come from extracted soybean. Soybean is rich in flafonoid. It has various advantages for our body. Which can also support child nutrition consumed. Soybean boosts immune system, helps digestive system, and in terms of food, soy bean exists as a source of nutrition. A method to get extraction of Centella asiatica is namely maserasi using ethanol. While making soybean milk with got the pollen of soybean. Both materials get mixed processed into hard candy with congelation of.

Keywords: Indonesia, Centella asiatica, Soy milk, alkaloid, flafonoid

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Authors: Alma Ramić, Mirjana Skočibušić, Renata Odžak, Tomica Hrenar, Ines Primožič

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In an attempt to identify a new class of antimicrobial agents, the antimicrobial potential of Cinchona alkaloid derivatives was evaluated. The bark of the Cinchona trees is the source of a variety of alkaloids, among which the best known are quinine, quinidine, cinchonine and cinchonidine. They are very useful as organocatalysts in stereoselective synthesis. On the other hand, quinine is traditionally used in the treatment of malaria. Furthermore, Cinchona alkaloids possess various analgesic, anti-inflammatory and anti–arrhythmic properties as well. In this work we present the synthesis of twenty quaternary derivatives of pseudo−enantiomeric Cinchona alkaloid derivatives to evaluate their antibacterial activity. Quaternization of quinuclidine moiety was carried out with groups diverse in their size. The structures of compounds were systematically modified to obtain drug-like properties with proper physical and chemical properties and avoiding toxophore. All compounds were prepared in good yields and were characterized by standard analytical spectroscopy methods (1D and 2D NMR, IR, MS). The antibacterial activities of all compounds were evaluated against series of recent clinical isolates of antibiotic susceptible Gram-positive and resistant Gram-negative pathogens by determining their zone of inhibition and minimum inhibitory concentrations. All compounds showed good to strong broad-spectrum activity, equivalent or better in comparison with standard antibiotics used. Furthermore, seven compounds exhibited significant antibacterial efficiency against Gram-negative isolates. To visualize the results, principal component analysis was used as an additional classification tool. Cytotoxicity of compounds with different cell lines in human cell culture was determined. Based on these results, substituted quaternary Cinchona scaffold can be considered as promising new class of antimicrobials and further investigations should be performed. Supported by Croatian Science Foundation, Project No 3775 ADESIRE.

Keywords: antibacterial efficiency, cinchona alkaloids, cytotoxicity, pseudo‐enantiomers

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Authors: Leonardo Parra, Manuel Chacón-Fuentes, Andrés Quiroz

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One of the most important factors in beef and dairy production in the world as well as also in Chile, is related to the correct choice of cultivars or mixtures of forage grasses and legumes to ensure high yields and quality of grassland. However, a great problem is the persistence of the grasses as a result of the action of different hypogeous as epigean pests. The complex insect pests associated with grassland include white grubs (Hylamorpha elegans, Phytoloema herrmanni), blackworm (Dalaca pallens) and Argentine stem weevil (Listronotus bonariensis). In Chile, the principal strategy utilized for controlling this pest is chemical control, through the use of synthetic insecticides, however, underground feeding habits of larval and flight activity of adults makes this uneconomic method. Furthermore, due to problems including environmental degradation, development of resistance and chemical residues, there is a worldwide interest in the use of alternative environmentally friendly pest control methods. In this sense, in recent years there has been an increasing interest in determining the role of endophyte fungi in controlling epigean and hypogeous pest. Endophytes from ryegrass (Lolium perenne), establish a biotrophic relationship with the host, defined as mutualistic symbiosis. The plant-fungi association produces a “cocktail of alkaloids” where peramine is the main toxic substance present in endophyte of ryegrass and responsible for damage reduction of L. bonariensis. In the last decade, few studies have been developed on the effectiveness of new ryegrass cultivars carriers of endophyte in controlling insect pests. Therefore, the aim of this research is to provide knowledge concerning to evaluate the alkaloid content, such as peramine and Lolitrem B, present in new experimental lines of ryegrass and feasible to be used in grasslands of southern Chile. For this, during 2016, ryegrass plants of six experimental lines and two commercial cultivars sown at the Instituto de Investigaciones Agropecuarias Carrillanca (Vilcún, Chile) were collected and subjected to a process of chemical extraction to identify and quantify the presence of peramine and lolitrem B by the technique of liquid chromatography of high resolution (HPLC). The results indicated that the experimental lines EL-1 and EL-3 had high content of peramine (0.25 and 0.43 ppm, respectively) than with lolitrem B (0.061 and 0.19 ppm, respectively). Furthermore, the higher contents of lolitrem B were detected in the EL-4 and commercial cultivar Alto (positive control) with 0.08 and 0.17 ppm, respectively. Peramine and lolitrem B were not detected in the cultivar Jumbo (negative control). These results suggest that EL-3 would have potential as future cultivate because it has high content of peramine, alkaloid responsible for controlling insect pest. However, their current role on the complex insects attacking ryegrass grasslands should be evaluated. The information obtained in this research could be used to improve control strategies against hypogeous and epigean pests of grassland in southern Chile and also to reduce the use of synthetic pesticides.

Keywords: HPLC, Lolitrem B, peramine, pest

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Authors: Tariku Nefo Duke

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Embelia is a genus of climbing shrubs in the family Myrsinaceae. Embelia schimperi is as important in traditional medicine as the other species in the genus. The plant has been much known as a local medicine for the treatment of tapeworms. In this project, extraction, phytochemical screening tests, isolation, and characterization of berries of the Embelia schimperi plant have been conducted. The chemical investigations of methanol and ethyl acetate (1:1) ratio extracts of the berries lead to the isolation of three new compounds. The compounds were identified to be alkaloids coded as AD, AN, and AG. Structural elucidations of the isolated compounds were accomplished using spectroscopic methods (IR, UV, ¹H NMR, ¹³C NMR, DEPT and 2D NMR, HPLC, and LC-MS). The alkaloid coded as (AN) has a wide MIC range of 6.31-25.46 mg/mL against all tested bacteria strains.

Keywords: Embelia schimper, HPLC, alkaloids, 2D NMR, MIC

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Authors: Taiwo O. Margaret, Olaoluwa O. Olaoluwa

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Moraceae family has immense phytochemical constituents and significant pharmacological properties, hence have great medicinal values. The aim of this study was to screen and quantify phytochemicals as well as the antioxidant activities of the leaf and stem bark extracts and fractions (crude ethanol extracts, n-hexane, ethyl acetate and aqueous ethanol fractions) of Ficus sagittifolia. Leaf and stem bark of F. sagittifolia were extracted by maceration method using ethanol to give ethanol crude extract. The ethanol crude extract was partitioned by n-hexane and ethyl-acetate to give their respective fractions. All the extracts were screened for their phytochemicals using standard methods. The total phenolic, flavonoid, tannin, saponin contents and antioxidant activity were determined by spectrophotometric method while the alkaloid content was evaluated by titrimetric method. The amount of total phenolic in extracts and fractions were estimated in comparison to gallic acid, whereas total flavonoids, tannins and saponins were estimated corresponding to quercetin, tannic acid and saponin respectively. 2, 2-diphenylpicryl hydrazyl radical (DPPH)* and phosphomolybdate methods were used to evaluate the antioxidant activities of leaf and stem bark of F. sagittifolia. Phytochemical screening revealed the presence of flavonoids, saponins, terpenoids/steroids, alkaloids for both extracts of leaf and stem bark of F. sagittifolia. The phenolic content of F. sagittifolia was most abundant in leaf ethanol crude extract as 3.53 ± 0.03 mg/g equivalent of gallic acid. Total flavonoids and tannins content were highest in stem bark aqueous ethanol fraction of F. sagittifolia estimated as 3.41 ± 0.08 mg/g equivalent of quercetin and 1.52 ± 0.05 mg/g equivalent of tannic acid respectively. The hexane leaf fraction of F. sagittifolia had the utmost saponin and alkaloid content as 5.10 ± 0.48 mg/g equivalent of saponins and 0.171 ± 0.39 g of alkaloids. Leaf aqueous ethanol fraction of F. sagittifolia showed high antioxidant activity (IC₅₀ value of 63.092 µg/mL) and stem ethanol crude extract (227.43 ± 0.78 mg/g equivalent of ascorbic acid) for DPPH and phosphomolybdate method respectively and the least active was found to be the stem hexane fraction using both methods (313.32 µg/mL; 16.21 ± 1.30 mg/g equivalent of ascorbic acid). The presence of these phytochemicals in the leaf and stem bark of F. sagittifolia are responsible for their therapeutic importance as well as the ability to scavenge free radicals in living systems.

Keywords: Moraceae, Ficus sagittifolia, phytochemicals, antioxidant

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Authors: A. U. Adamu, E. D Paul, C. E. Gimba, I. G. Ndukwe

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The phytochemical and proximate composition of Aspillia kotschyi belonging to Compositae family which is commonly used as medicinal plant in Nigeria was determined on both the Methanolic and Petroleum sprit extract of the plant. The Methanolic extract of the plant revealed the presence of carbohydrates, cardiac glyscosides, flavonoids, triterpene, and alkaloids. The Petroleum sprit extract showed the presence of only carbohydrates and alkaloid. Proximate composition analysis shows moisture content of 5.7%, total ash of 4.03%, crude protein 10.94%, fibre 9.06%, fat value 0.83%, and nitrogen free extract of 70.19%. The results of this study suggest some merit in the popular use of Aspillia kotschi in herbal medicine.

Keywords: Aspillia kotschyi, herbal medicine, phytochemical, proximate composition

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Authors: Kakali Bhadra

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Harmalol administration caused remarkable reduction in proliferation of HepG₂ cells with GI₅₀ of 14.2 mM, without showing much cytotoxicity in embryonic liver cell line, WRL-68. Data from circular dichroism and differential scanning calorimetric analysis of harmalol-CT DNA complex shows conformational changes with prominent CD perturbation and stabilization of CT DNA by 8 ^oC. Binding constant and stoichiometry was also calculated using the above biophysical techniques. Further, dose dependent apoptotic induction ability of harmalol was studied in HepG₂ cells using different biochemical assays. Generation of ROS, DNA damage, changes in cellular external and ultramorphology, alteration of membrane, formation of comet tail, decreased mitochondrial membrane potential and a significant increase in Sub G_o/G₁ population made the cancer cell, HepG₂, prone to apoptosis. Up regulation of p53 and caspase 3 further indicated the apoptotic role of harmalol.

Keywords: apoptosis, beta carboline alkaloid, comet assay, cytotoxicity, ROS

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Authors: Thaís T. Valério Caetano, João Máximo De Siqueira, Carlos Alexandre Carollo, Arthur Ladeira Macedo, Vanessa C. Stein

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Nicotiana glauca, commonly known as wild tobacco or tobacco bush, belongs to the Solanaceae family. It is native to South America but has become naturalized in various regions, including Australia, California, Africa, and the Mediterranean. N. glauca is listed in the Global Invasive Species Database (GISD) and the Invasive Species Compendium (CABI). It is known for producing pyridine alkaloids, including anabasine, which is highly toxic. Anabasine is predominantly found in the leaves and can cause severe health issues such as neuromuscular blockade, respiratory arrest, and cardiovascular problems when ingested. Mistaken identity with edible plants like spinach has resulted in food poisoning cases in Israel and Brazil. Anabasine, a minor alkaloid constituent of tobacco, may contribute to tobacco addiction by mimicking or enhancing the effects of nicotine. Therefore, it is essential to investigate the production pattern of anabasine and its relationship to the developmental stages of the plant. This study aimed to establish the relationship between the phenological plant age, cultivation place, and the increase in anabasine concentration, which can lead to human intoxication cases. In this study, N. glauca plants were collected from three different rural areas in Brazil for a year to examine leaves at various stages of development. Samples were also obtained from cultivated plants in Marilândia, Minas Gerais, Brazil, as well as from Divinópolis, Minas Gerais, Brazil, and Arraial do Cabo, Rio de Janeiro, Brazil. In vitro cultivated plants on MS medium were included in the study. The collected leaves were dried, powdered, and stored. Alkaloid extraction was performed using a methanol and water mixture, followed by liquid-liquid extraction with chloroform. The anabasine content was determined using HPLC-DAD analysis with nicotine as a standard. The results indicated that anabasine production increases with the plant's development, peaking in adult leaves during the reproduction phase and declining afterward. In vitro, plants showed similar anabasine production to young leaves. The successful adaptation of N. glauca in new environments poses a global problem, and the correlation between anabasine production and the plant's developmental stages has been understudied. The presence of substances produced by the plant can pose a risk to other species, especially when mistaken for edible plants. The findings from this study shed light on the pattern of anabasine production and its association with plant development, contributing to a better understanding of the potential risks associated with N. glauca and the importance of accurate identification.

Keywords: nicotiana glauca graham, global invasive species database, alkaloids, toxic

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Authors: Mai M. Farid, Ximeng Yang, Tomoharu Kuboyama, Chihiro Tohda

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Trigonelline is a major alkaloid component derived from Trigonella foenum-graecum L. (fenugreek) and has been reported before as a potential neuroprotective agent, especially in Alzheimer’s disease (AD). However, the previous data were unclear and used model mice were not well established. In the present study, the effect of trigonelline on memory function was investigated in Alzheimer’s disease transgenic model mouse, 5XFAD which overexpresses the mutated APP and PS1 genes. Oral administration of trigonelline for 14 days significantly enhanced object recognition and object location memories. Plasma and cerebral cortex were isolated at 30 min, 1h, 3h, and 6 h after oral administration of trigonelline. LC-MS/MS analysis indicated that trigonelline was detected in both plasma and cortex from 30 min after, suggesting good penetration of trigonelline into the brain. In addition, trigonelline significantly ameliorated axonal and dendrite atrophy in Amyloid β-treated cortical neurons. These results suggest that trigonelline could be a promising therapeutic candidate for AD.

Keywords: alzheimer’s disease, cortical neurons, LC-MS/MS analysis, trigonelline

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Authors: Ait Slimane-Ait Kaki Sabrina, Foudi Lamia

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The present work consists of the study of the bio-ecology and the therapeutic effects of the belladone (Atropa belladonna L.). It is a medicinal plant of the Solanacées family, herbaceous, robust 0.5 up to 1.50 m high. The phytochemical analysis of leaves revealed alkaloids, tannins, catechin, coumarins, mucilages, saponins, starch, and reducing compounds. The experimental study concerns the extraction and characterization of belladonna alkaloids. Analysis of the purified extract by staining tests confirmed the presence of tropane alkaloids. The dosage chromatography revealed the presence of components that have been identified atropine, scopolamine and hyoscyamine. Evaluation of antimicrobial and antifungal alkaloids from the methanol extract and aqueous extract of belladonna on pathogenic germs showed a positive bactericidal against strains of Escherichia coli and Staphylococcus aureus. Our preliminary results allow us an overall assessment of the medicinal value of Atropa belladonna.

Keywords: belladone, alkaloid, antibacterial activity, antifungal activity

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Authors: Nahid H. Hajrah, Jamal S. M. Sabir, Neil Hall

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The jasmonic pathway is ubiquitous in plants and is crucial to plant development. It Is involved in fertility, ripening, and sex determination as well as in response to environmental stresses such as herbivory, pathogen drought or temperature shock. Essentially the jasmonic pathway acts to shut down growth in order to induce defence pathways. These pathways include the production of secondary metabolites which have evolved to defend against herbivores and pathogens but are of increasing interest due to their roll in medicine and biotechnology. Here we describe the transcriptional response of Rhazia stricta (a poisonous shrub widely used in traditional medicine) to jasmonic acid, in order to better characterize the genes involved in secondary metabolite production and its response to stress. We observe coordinated upregulation of flavonoid biosynthesis pathway leading to flavonols, flavones and anthocyanins but no similar coordination of the monoterpene indole alkaloid pathway.

Keywords: medicinal plants, Rhazia stricta, jasmonic acid, transcriptional analysis

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Authors: Srie Rezeki Nur Endah, Richa Mardianingrum

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Cancer is one of the most feared diseases and is considered the leading cause of death worldwide. Generally, cancer drugs are synthetic drugs with relatively more expensive prices and have harmful side effects, so many people turn to traditional medicine, for example by utilizing herbal medicine. Erythrina poeppigiana is one of the plants that can be used as a medicinal plant containing 10,11-dihidroerisodin compounds that are useful anticancer etnofarmakologi. The purpose of this study was to identify the target of 10,11 dihydroerisodin receptor compound as in silico anticancer candidate. The pure isolate was tested physicochemically by MS (Mass Spectrometry), UV-Vis (Ultraviolet – Visible), IR (Infra Red), 13C-NMR (Carbon-13 Nuclear Magnetic Resonance), 1H-NMR (Hydrogen-1 Nuclear Magnetic Resonance), to obtain the structure of 10,11-dihydroerisodin alkaloid compound then identified to target receptors in silico. From the results of the study, it was found that 10,11-dihydroerisodin compound can work on the Serine / threonine-protein kinase Chk1 receptor that serves as an anti-cancer candidate.

Keywords: anti-cancer, Erythrina poeppigiana, target receptor, 10, 11- dihidroerisodin

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Authors: Afifah Nur Aini, Elsa Mega Suryani, Betty Lukiaty

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Drymoglossum piloselloides or more commonly known as sisik naga fern is a member of Polipodiaceae Family that is abundant and widely distributed in nature. That being said, there hasn’t been many studies reporting about the benefits of this fern. The aim of this study was to find out the active compounds and antioxidant activity of water fraction extract of sisik naga leaves. The study will be able to optimize the use of this fern in the future. In this study, phytochemical test was done qualitatively by using Mayer, Dragendorff and Wagner reagent for alkaloid test; FeCl3 for phenolic test; Shinoda test for flavonoid; Liebermann-Burchard test for triterprnoid and Forth test for saponin. Antioxidant activity test was done by using 20D spectronic spectrophotometer to determine the percentage of DPPH free radical inhibition. The results showed that water fraction extract of sisik naga leaves contain phenolic and IC50 = 5.44 μg/ml. This means that sisik naga leaves can be used as an antioxidant.

Keywords: antioxidant activity test, dpph, phytochemical test, drymoglossum piloselloides

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Authors: Muhammad Isah Legbo

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The phytochemical screening and antimicrobial activity of Nauclea lotifolia fruit, leaf and stem-bark extracts at various concentration of (20.0,10.0, 5.0, and 2.5 mg/ml) were evaluated against some pathogenic microorganisms such as Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Staphylococcus aureus, Aspergillus niger and Candida albicans. The antimicrobial activity was assayed using agar well diffusion method. The result obtained show appreciable inhibitory effort of acetone, aqueous and methanolic extracts of Nauclea lotifolia. However, result obtained was less active compared to that of the control antibiotic (Ciprofloxacillin). The minimum inhibitory concentration (MIC) was determined using serial doubling dilution method and ranged from 5.0-10.0mg/ml, while the minimum bactericidal concentration (MBC) was determined by plating various dilution of extracts without turbidity and the result ranged from 5.0-7.5mg/ml. The phytochemical screening revealed the presence of alkaloid, anthraquinones, flavonoids, resin, steroid and saponin. The activities of the plant extract therefore justify their utilization in the treatment of various ailments associated with the test organism.

Keywords: Nauclea, lotifolia, antimicrobial, pathogens, saponin, extract

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Authors: Benarous Khedidja, Yousfi Mohamed

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Infections caused by Candida species manifest in a number of diseases, including candidemia, vulvovaginal candidiasis, endocarditis, and peritonitis. These Candida species have been reported to have lipolytic activity by secretion of lipolytic enzymes such as esterases, lipases and phospholipases. These Extracellular hydrolytic enzymes seem to play an important role in Candida overgrowth. Candidiasis is commonly treated with antimycotics such as clotrimazole and nystatin, which bind to a major component of the fungal cell membrane (ergosterol). This binding forms pores in the membrane that lead to death of the fungus. Due to their secondary effects, scientists have thought of another treatment basing on lipase inhibition but we haven’t found any lipase inhibitors used as candidiasis treatment. In this work, we are interested to lipases inhibitors such as alkaloids as another candidiasis treatment. In the first part, we have proceeded to optimize the alkaloid structures and protein 3D structure using Hyperchem software. Secondly, we have docked inhibitors using Genetic algorithm with GOLD software. The results have shown ten possibilities of binding inhibitor to Candida rugosa lipase (CRL) but only one possibility has been accepted depending on the weakest binding energy.

Keywords: marrubiin, candida rugosa lipase, docking, gold

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Authors: Mehran Fadaeinasab, Hamed Karimian, Najihah Mohd Hashim, Hapipah Mohd Ali

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In this study, three indole alkaloids namely; rauvolfine B, macusine B, and isoreserpiline have been isolated from the dichloromethane crude extract of Rauvolfia reflexa bark (Apocynaceae). The structural elucidation of the isolated compounds has been performed using spectral methods such as UV, IR, MS, 1D, and 2D NMR. Rauvolfine B showed anti proliferation activity on HCT-116 cancer cell line, its cytotoxicity induction was observed using MTT assay in eight different cell lines. Annexin-V is serving as a marker for apoptotic cells and the Annexin-V-FITC assay was carried out to observe the detection of cell-surface Phosphatidylserine (PS). Apoptosis was confirmed by using caspase-8 and -9 assays. Cell cycle arrest was also investigated using flowcytometric analysis. rauvolfine B had exhibited significantly higher cytotoxicity against HCT-116 cell line. The treatment significantly arrested HCT-116 cells in the S phase. Together, the results presented in this study demonstrated that rauvolfine B inhibited the proliferation of HCT-116 cells and programmed cell death followed by cell cycle arrest.

Keywords: apocynacea, indole alkaloid, apoptosis, cell cycle arrest

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Authors: Mahdeb Nadia, Ghadjati Nadhra, Bettihi Sara, Daamouche Z. El Youm, Bouzidi Abdelouahab

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The effects of subacute administration of total alkaloids of seeds Peganum harmala were studied in female Albino-Wistar rats. After intraperitoneal administration of dose 50 mg/kg for 10 days and 40 mg/kg for 7 days of total alkaloids to the seeds of Peganum harmala (animal treatment lasted 17 days), there were remarkable changes in general appearance and deaths occurred in experimental group. After 17 days a significant reduction was observed in the surviving animals treated with total alkaloid seeds.The Red Blood Cells (RBC), Hematocrit (HCT), Hemoglobin (HGB) and White blood cells (WBCs), show significant reduction in the treated groups. There were no statistical differences in Glutamic-Oxaloacetic Transaminase (GOT), Glutamic-pyruvic Transaminase (GPT) and Alkaline Phosphatase (ALP), total protein, glucose and creatinine observed between groups. However the urea was significantly higher in the treated female rats than the control group. Histological examination of liver showed no histopathological changes. Alkaloids of Peganum harmala showed significant toxicity in female rats.

Keywords: Peganum harmala, rat, liver, kidney, alkaloids, toxicity

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Authors: Amornnat Thuppia, Pornrut Rabintossaporn, Suphaket Saenthaweesuk, Nuntiya Somparn

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The aim of this present study was to determine the antioxidant effects and its mechanism of aqueous leaves extract of Bauhinia acuminata (BA) in rat. The extract was screened for its phytochemical contents and antioxidant activity in vitro. Moreover, the extract was studied in rats to evaluate its effects in vivo. Rats were orally administered with the extract at the dose of 50, 100 and 200 mg/kg for 28 days. Phytochemical screening of plant extracts showed the presence of saponin, alkaloid, cardiac glycosides, flavonoids, tannin and steroid compounds. The extract contained phenolic compounds 53.36 ± 1.01 mg of gallic acid equivalents per gram BA extract. The free radical scavenging activity assessed by DPPH assay gave IC50 of 44.47 ± 2.83 µg/mL, which is relatively lower than that of BHT with IC50 of 12.34 ± 1.14µg/mL. In the animals, the extract was well tolerated by the animals throughout the 28 days of study as shown by normal serum levels AST, ALP, ALT, BUN and Cr as well as normal histology of liver and pancreatic and kidney tissue. Significantly, reduction of serum oxidative stress markers malondialdehyde (MDA) was found in rat treated with BA extract compared with control. Taken together, this study provides evidence that Bauhinia acuminata (BA) exhibits direct antioxidant properties and induces cytoprotective enzyme in vivo.

Keywords: Bauhinia acuminata, antioxidant, malondialdehyde (MDA), oxidative marker

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Authors: Mansur Abdulrasheed, Ibrahim I. Hussein, Ahmed M. Mubarak, Ahmed F. Umar

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This study was aimed at evaluating the phytochemical constituents and the antimicrobial activity of the seed oil of Moringa oleifera and garlic against some selected food-borne microorganisms (Staphylococcus aureus, Escherichia coli, Salmonella spp and Pseudomonas aeruginosa) using disc diffusion method. The results of the phytochemical screening revealed differences in the presence of the phytochemicals among the extracts. Saponins were detected in both Moringa oleifera and garlic seed oil, while alkaloid and tannins were observed in seed oil of garlic. Furthermore, the antibacterial assay results show that the seed oil of Moringa oleifera was inactive against all the tested organisms, even at 100 % concentration. In contrast, garlic oil was found to be active against all the tested organisms. The highest inhibition was observed in E. coli (12 mm) at 100 % concentration, while at 20 % concentration, Salmonella Sp and P. aeruginosa showed the least inhibiton (6 mm). The antimicrobial activity of the seed oil of garlic may be attributed to its phytochemicals components which were not detected in the seed oil of Moringa oleifera. The results of this study have shown the potentials of the seed oil of garlic as an antimicrobial agent more especially in foods, by inhibiting the growth of the test organisms, which range from food-borne pathogens to food spoilage organisms.

Keywords: antimicrobial, garlic, Moringa oleifera, food borne pathogens

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Authors: Eva Tvrdá, Hana Greifová, Peter Ivanič, Norbert Lukáč

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The aim of this study was to evaluate the dose- and time-dependent in vitro effects of berberine (BER), a natural alkaloid with numerous biological properties on bovine spermatozoa during three time periods (0 h, 2 h, 24 h). Bovine semen samples were diluted and cultivated in physiological saline solution containing 0.5% DMSO together with 200, 100, 50, 10, 5, and 1 μmol/L BER. Spermatozoa motility was assessed using the computer assisted semen analyzer. The viability of spermatozoa was assessed by the metabolic (MTT) assay, production of superoxide radicals was quantified using the nitroblue tetrazolium (NBT) test, and chemiluminescence was used to evaluate the generation of reactive oxygen species (ROS). Cell lysates were prepared and the extent of lipid peroxidation (LPO) was evaluated using the TBARS assay. The results of the movement activity showed a significant increase in the motility during long term cultivation in case of concentrations ranging between 1 and 10 μmol/L BER (P < 0.01; P < 0.001; 24 h). At the same time, supplementation of 1, 5 and 10 μmol/L BER led to a significant preservation of the cell viability (P < 0.001; 24 h). BER addition at a range of 1-50 μmol/L also provided a significantly higher protection against superoxide (P < 0.05) and ROS (P < 0.001; P < 0.01) overgeneration as well as LPO (P < 0.01; P<0.05) after a 24 h cultivation. We may suggest that supplementation of BER to bovine spermatozoa, particularly at concentrations ranging between 1 and 50 μmol/L, may offer protection to the motility, viability and oxidative status of the spermatozoa, particularly notable at 24 h.

Keywords: berberine, bulls, motility, oxidative profile, spermatozoa, viability

Procedia PDF Downloads 102