Isolation Of Active Compounds Research Articles

Phytochemical and Pharmacological Potential of Enhydra fluctuans Available in Bangladesh

Objectives: The possible phytochemical constituents, thrombolytic and membrane stabilizing activities of the crude ethanolic extract of Enhydra fluctuans (CE) were investigated along with the antimicrobial, antioxidant and cytotoxic potentials of its petroleum ether (PESF), carbon tetrachloride (CTCSF), chloroform (CSF) and aqueous (AQSF) soluble fractions.
 Materials & Methods: The coarse leaf powder was extracted at room temperature with ethanol. Solvent-solvent partitioning was done to obtain the four soluble fractions. Anticoagulant potential was determined by the in vitro thrombolytic model, membrane stabilization method was used to assess in vitro anti-inflammatory activity, the disc diffusion method was used for anti-microbial screening, antioxidant potential was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and brine shrimp lethality bioassay method was used for cytotoxic activity determination.
 Results: Chemical screening of the crude extract evidenced the presence of alkaloids, saponins, tannins, flavonoids, reducing sugars and gums. It showed significant clot lysis property of 46.91%. It also significantly inhibited heat and hypotonic solution induced lysis of the human red blood cell membrane with values of 71.80% and 47.60%, respectively. CTCSF and PESF showed mild antimicrobial activity. AQSF showed most prominent antioxidant activity with IC50 value of 12.27 µg/mL. CTCSF showed LC50 value of 0.84 µg/mL, with most potent cytotoxic activity.
 Conclusion: Significant thrombolytic, membrane stabilizing, antioxidant and in vitro cytotoxic activities of the ethanolic plant extract were observed in this study. In vivo activities and isolation of active compound(s) from this extract are yet to be investigated.

Pharmacologic Application Potentials of Sulfated Polysaccharide from Marine Algae.

With the advent of exploration in finding new sources for treating different diseases, one possible natural source is from marine algae. Having an array of potential benefits, researchers are interested in the components which comprise one of these activities. This can lead to the isolation of active compounds with biological activities, such as antioxidation of free radicals, anti-inflammation, antiproliferation of cancer cells, and anticoagulant to name a few. One of the compounds that are isolated from marine algae are sulfated polysaccharides (SPs). SPs are complex heterogenous natural polymers with an abundance found in different species of marine algae. Marine algae are known to be one of the most important sources of SPs, and depending on the species, its chemical structure varies. This variety has important physical and chemical components and functions which has gained the attention of researchers as this contributes to the many facets of its pharmacologic activity. In this review, recent pharmacologic application potentials and updates on the use of SPs from marine algae are discussed.

Antioxidant and Antimelanogenesis Activities of Glyasperin A From Macaranga pruinosa Leaves

In our effort to find materials for drugs and cosmetics from tropical natural resources, we screened 21 methanol extracts from 7 Macaranga trees species ( Macaranga bancana, Macaranga gigantea, Macaranga hulle ttii, Macaranga pruinosa, Macaranga tanarius, Macaranga trichocarpa, and Macaranga triloba) for antioxidant and antimelanogenesis. The antioxidant and melanogenesis (tyrosinase enzyme assay and melanin inhibitor in B16 melanoma) assays were used to determine the activities. The fractionation and the isolation of active compound were done by various chomatographic methods and the structure was determined by spectroscopic analysis data. We isolated a prenylated flavonoid, named Glyasperin A, from M. pruinosa leaf. This compound showed a potency as antioxidant and inhibited melanin in B16 melanoma but not tyrosinase activity. These results showed that the methanol leaf extracts of M. pruinosa could be developed for cosmetic applications especially as a skin whitening agent.

Isolation of active compounds from the leaf extract of patah kemudi (Abroma augusta L.) and its anti-inflammatory activity

Patah kemudi (Abroma augusta L.) is one of the shrubs that live on the edge of a river. A. augusta contains several secondary metabolite compounds including alkaloids, triterpenoids, steroids and flavonoids. The aim of this study was to isolate the compounds contained in the leaves of Abroma augusta and determine anti-inflammatory activity. Extraction and fractionation were performed by multilevel maceration. Isolation of compounds was carried out by column chromatography. The anti-inflammatory activity test was done using the Winter method. The n-hexane extract was separated by vacuum column chromatography and continued with gravity column chromatography to obtain isolate 8.1, which was then characterized using UV-Vis and IR spectrophotometer. The results of UV-Vis spectrophotometer on isolate 8.1 showed absorption at a maximum wavelength of 268 indicating a conjugate double bond which may be an aromatic originating from steroid compounds. While, the results of IR spectrophotometer characterization from isolate 8.1 manifested the presence of steroid compounds. The results of the activity test of isolate 8.1 with a dose of 10 mg presented the best anti-inflammatory activity compared to the positive control of diclofenac sodium. From the results of the GCMS shows that isolates contain γ-sitosterol compounds with a value of m/z 414.

Acute anti-inflammatory and anti-nociceptive activities of crude extracts, alkaloid fraction and evolitrine from Acronychia pedunculata leaves

Ethnopharmacological relevanceAcronychia pedunculata (family: Rutaceae) is one of the commonly used medicinal plants in Sri Lankan traditional medicine. Different parts of this plant are used for the treatment of inflammatory conditions in the form of medicinal oils and herbal porridge. Aim of the studyThe present study aimed to evaluate the anti-nociceptive activity and anti-inflammatory activity with their mechanisms and the acute toxicity of crude extracts of the fresh leaves of A. pedunculata for scientific validation of the ethnopharmacological claims for this plant. Further, attention has been focused on the isolation of active compounds from active fractions of the crude extracts. Materials and methodsThe acute anti-inflammatory effect of the aqueous (AELA) and 70% ethanol crude extracts (EELA) and alkaloid fraction of A. pedunculata leaves were evaluated by the determination of inhibition of hind paw oedema induced by carrageenan in Wistar rats. Evolitrine was identified as the major alkaloid with significant bioactivities by column chromatography and NMR. The anti-nociceptive and anti-histamine activities of EELA and evolitrine were evaluated by acetic acid induced writhing and wheal formation tests respectively. In addition, in-vitro (2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay) and in-vivo (lipid peroxidation assay) anti-oxidant activity, nitric oxide (NO) inhibitory activity and acute toxicity of EELA were evaluated. ResultsAcute anti-inflammatory activity of AELA and EELA were dose-dependent. EELA was more active than AELA. The 200 mg/kg body weight (b. w.) dose of EELA was found as the minimum effective dose with maximum inhibition (78%) of oedema at 5th hour compared to the negative control (p < 0.05). Evolitrine was isolated and identified as an active anti-inflammatory and analgesic compound from active alkaloid fraction of EELA. Evolitrine showed activity enhancement when compared with crude EELA. The anti-inflammatory and analgesic activities of evolitrine (50 mg/kg b. w.) were comparable to that of reference drugs indomethacin (5 mg/kg b. w) and acetylsalicylic acid (100 mg/kg b. w.). The significant (p < 0.05) anti-histamine activity, DPPH scavenging in-vitro anti-oxidant activity, in-vivo lipid peroxidation inhibitory activity in-vivo, NO inhibitory activity of EELA as compared with relevant negative controls, were identified as probable mechanisms which mediated its anti-inflammatory action. Further, EELA showed a high safety margin in the limited dose acute toxicity study. ConclusionThe findings of the current study rationalize the usage of leaves of A. pedunculata in Sri Lankan traditional medicine as an analgesic and anti-inflammatory agent. Possible mechanisms mediating this activity included anti-histamine, anti-oxidant and NO inhibitory activities. Evolitrine is the major analgesic and anti-inflammatory compound isolated from the active alkaloid fraction of EELA.

Antimicrobial Activity of 4-O-methylgallic Acid Isolated from Phyllanthus polyphyllus L. against Foodborne Pathogenic Bacteria and Yeasts

The aim of this study was to evaluate the antimicrobial activity of 4-O-methylgallic acid isolated from Phyllanthus polyphyllus L. and examine its possible antimicrobial mode of action against food-borne pathogenic bacteria and yeast. The bioassay-guided fractionation of methanol extract of leaves led to the isolation of active compound 4-O-methylgallic acid (4-O-MGA). The antimicrobial activity were assessed against two Gram-positive (Staphylococcus aureus and Streptococcus faecalis), five Gram-negative (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris and Salmonella typhimurium) bacteria and two yeasts (Candida albicans and Cryptococcus neoformans) using disk diffusion method followed by a standardized microdilution assay. 4-O-MGA exhibited antimicrobial activity against all tested bacteria with MIC ≥ 0.125 mg/mL and MBC ≥ 0.25 mg/mL. Among tested organisms, Gram-positive bacteria were more sensitive than Gram-negative, and yeasts showed more resistance with higher MIC 1.0 mg/mL and MFC ≥ 2.0 mg/mL. Much effort was focused on elucidating the mechanism of antimicrobial action of 4-O-MGA against S. aureus and E. coli by observing the changes in membrane integrity as confirmed by release of loss of 260 nm absorbing materials and leakage of potassium with outer membrane permeability, and against a yeast C. albicans as confirmed by inhibitory effects on biofilm formation and sterol content in the plasma membrane. The antimicrobial properties of 4-O-MGA suggest that, also considering its antioxidant and well known nutritional functions, it has potential for development as an antimicrobial agent for control of food-related pathogenic microbes.

Ultrastructure-based Insights on Anti-Trichomonas vaginalis Effects of Selected Egyptian Red Sea Marine Resources

Background:Metronidazole is used for the treatment of trichomoniasis. However, a growing number ofTrichomonas vaginalis(T. vaginalis) isolates are now resistant, which is an urgent issue to search for new alternatives. Worldwide marine pharmacy confirms the enormous potential of sea species as a source of novel pharmaceuticals.Objective:This study aimed to investigate the anti-T. vaginalisactivities of ethanolic extracts of Red Sea marine resources, soft corals;Sarcophyton glaucumandLitophyton arboreumand methanolic extracts of Red Sea brown algae;Liagora farinosa, Colpomenia sinuosa, Hydroclathrus clathratus,andSargassum graminifolium, as well as sea cucumber (Holothuria fuscocinerea) and sea urchin (Echinometra mathaei).T. vaginalisgrowth inhibition was determined using 2 concentrations for each marine extract 10 and 100 µg/ml in comparison to media control. Drugs that showed good initial activity were further tested to calculate their IC50 in comparison to metronidazole. The ultrastructural impact of the more effective extracts was further assessed.Results:H. clathratus,L. farinose, sea urchinE. mathaeiand sea cucumberH. fuscocinereareduced the growth ofT. vaginaliseffectively and showed high activity with IC50 of 0.985±0.08, 0.949±0.04, 0.845±0.09 and 0.798±µg/ml±SD, respectively. Concerning microscopic analysis, marine extract and metronidazole-treated cells presented similar morphological changes. The nuclear membrane was damaged, the nuclei were dissolved, the rough endoplasmic reticulum was widened, and the chromatin was accumulated. In the cytoplasm, numerous autophagic vacuoles appeared, the organelles were disintegrated, the flagella were internalized and hydrogenosomes with altered morphologies were observed. The cell membrane was partially damaged, with cytoplasmic leakage and cell disintegration.Conclusion:This study describes the report on the activity and morphological changes induced by Egyptian Red Sea marine resources againstT. vaginalis. The results obtained herein presented new opportunitiess. Further, bio-guided fractionation and isolation of active compounds are needed.

In vitro antitoxoplasmal activity of some medicinal plants

Background: Toxoplasmosis is a serious zoonotic protozoal disease that is distributed worldwide and can infect almost all warm-blooded animals, including humans. In most cases, it is asymptomatic, but in immunocompromised individuals, it is associated with severe neurological and gastrointestinal disorders. A previous serological prevalence investigation in Saudi Arabia indicated that the disease prevalence ranged between 25% and 51% in various areas. Recommended commercial drugs cannot achieve 100% clearance due to side effects. Hence, the development of new safe and affordable drugs is an important goal. Aim: In the present study, extracts from the leaves and fruit of Azadirachta indica A. Juss. collected from different areas, along with two other medicinal plants (Argemone mexicana L. and Xanthium brasilicum Vell.) with established antiprotozoal activity, will be evaluated for antitoxoplasmal activity using an in vitro technique. Materials and Methods: All plants were extracted with 100% methanol and examined for activity against the Toxoplasma gondii RH strain via an intracellularly invaded Vero cell line with calculated inhibition percentages. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay against the Vero cell line was used for cytotoxic evaluation, followed by selectivity index (SI) calculation. Results: X. brasilicum exhibited the best antitoxoplasmal activity with an IC50of 7.19 μg/ml, followed by the A. indica fruits collected from Qassim, Kingdom of Saudi Arabia, and leaves collected from Central Sudan with an IC50of 17.26 and 18.43 μg/ml, respectively. The best SI was obtained from the leaves of A. indica (6.28) collected from Sudan. Conclusion: Although X. brasilicum proved to have very potent antitoxoplasmal activity, the cytotoxicity was also very high, so the isolation of active compounds is highly recommended.

Bioassay-guided isolation of active compounds from Adenosma buchneroides essential oil as mosquito repellent against Aedes albopictus

Ethnopharmacological relevanceA folk herb Adenosma buchneroides found in the previous ethnobotanical investigation plays an important role as an insect repellent among the Aini people in southwest of China, but the active compounds responsible for repellent activity of the plant have not yet been investigated. Aim of the studyThe main purpose of the study is to identify the active components of the essential oil which responsible for its repellent activity against Aedes albopictus to support the usage of the plant as mosquito repellent by Aini people. In addition, to supply a class of potential alternatives characterized carvacrol analogues to develop natural repellent products. Material and methodsThe essential oil from aerial part of Ad. buchneroides was extracted by hydrodistillation. A systematic bioassay-guided isolation of repellent compounds from the essential oil was conducted through chromatographic fractionation combined with in-cage mosquito repellent bioassay. The identification of the essential oil components was accomplished by GC-MS and GC-FID techniques. The structural elucidation of compounds was performed on the basis of IR, HR-ESI-MS and NMR. Larvicidal activity and cytotoxicity of all repellent compounds also tested by larval bioassays and MTS assays, respectively. Structure-activity relationship (SAR) of carvacrol analogues was investigated by in-cage mosquito repellent bioassay. ResultsThe essential oil of the plant showed strong mosquito repellent activity with minimum effective dosage (MED) of 0.019 ± 0.007 mg/cm2, compared to reference standard N,N-diethyl-3-methylbenzamide (DEET) (0.031 ± 0.014 mg/cm2). 26 compounds representing 97.8% of the essential oil were identified. Carvacrol, carvacrol methyl ether and a new fragrant compound, adenosmin A (1) were found to be repellent compounds by systematic bioassay-guided isolation, with MEDs in the range of 0.011–0.125 mg/cm2. An investigation on SAR of carvacrol analogues led to the discover of three analogues with further lower MEDs (0.002–0.009 mg/cm2) than that of DEET, and other three compounds with similar MEDs (0.029–0.039 mg/cm2) to that of DEET. Carvacrol (LD50 of 24.8 ppm) was the best larvicide among tested repellent compounds. The essential oil and repellent compounds against seven mammalian cell lines revealed low or no cytotoxicity. ConclusionsScientific evidences reported here validate the plant's traditional use as insect repellent and imply promising application of the essential oil and carvacrol analogues as natural mosquito repellents.

Antiplasmodial activity and cytotoxicity, isolation of active alkaloids, and dereplication of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS.

To assess the antiplasmodial activity of the ethanol extract of Xylopia sericea leaves, Annonaceae, often associated with antimalarial use and to perform a bioguided isolation of active compounds. Dereplication of ethanol extract by the UPLC-DAD-ESI-MS/MS technique allowed the identification of the major constituents, isolation and identification of alkaloids. The antiplasmodial and cytotoxic activity of the extract, fractions and isolated compounds was evaluated against the chloroquine-resistant W2 strain Plasmodium falciparum and HepG2 cells, respectively. Ethanol extract showed high reduction of parasitemia as well as moderate cytotoxicity (86.5±3.0% growth inhibition at 50μg/ml and CC50 72.1±5.1μg/ml, respectively). A total of eight flavonoids were identified, and two aporphine alkaloids, anonaine and O-methylmoschatoline, were isolated. Anonaine disclosed significant antiplasmodial effect and moderate cytotoxicity (IC50 23.2±2.7μg/ml, CC50 38.3±2.3μg/ml, SI 1.6) while O-methylmoschatoline was not active against P.falciparum and showed a low cytotoxicity (33.5±1.9% growth inhibition at 50μg/ml, CC50 274.4±0.5μg/ml). Characterization of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS as well as its antiplasmodial activity and the occurrence of anonaine and O-methylmoschatoline in this Xylopia species are reported by the first time.

Antioxidant activity of different species and varieties of turmeric (Curcuma spp): Isolation of active compounds

There are >80 species of turmeric (Curcuma spp.) and some species have multiple varieties, for example, Curcuma longa (C. longa) has 70 varieties. They could be different in their chemical properties and biological activities. Therefore, we compared antioxidant activity, total phenolic and flavonoid content of different species and varieties of turmeric namely C. longa [variety: Ryudai gold (RD) and Okinawa ukon], C. xanthorrhiza, C. aromatica, C. amada, and C. zedoaria. The antioxidant activity was determined using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, oxygen radical absorbance capacity (ORAC), reducing power and 2-deoxyribose (2-DR) oxidation assay. Our results suggested that RD contained significantly higher concentrations of total phenolic (157.4 mg gallic acid equivalent/g extract) and flavonoids (1089.5 mg rutin equivalent/g extract). RD also showed significantly higher DPPH radical-scavenging activity (IC50: 26.4 μg/mL), ORAC (14,090 μmol Trolox equivalent/g extract), reducing power absorbance (0.33) and hydroxyl radical scavenging activity (IC50: 7.4 μg/mL). Therefore, RD was chosen for the isolation of antioxidant compounds using silica gel column, Toyopearl HW-40F column, and high-performance liquid chromatography. Structural identification of the compounds was conducted using 1H NMR, 13C NMR, and liquid chromatography-tandem mass spectrometry. The purified antioxidant compounds were bisabolone-9-one (1), 4-methyllene-5-hydroxybisabola-2,10-diene-9-one (2), turmeronol B (3), 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)-1-hepten-3-one (4), 3-hydroxy-1,7-bis(4-hydroxyphenyl)-6-hepten-1,5-dione (5), cyclobisdemethoxycurcumin (6), bisdemethoxycurcumin (7), demethoxycurcumin (8) and curcumin (9). The IC50 for DPPH radical-scavenging activity were 474, 621, 234, 29, 39, 257, 198, 47 and 18 μM and hydroxyl radical-scavenging activity were 25.1, 24.4, 20.2, 2.1, 5.1, 17.2, 7.2, 3.3 and 1.5 μM for compound 1, 2, 3, 4, 5, 6, 7, 8 and 9, respectively. Our findings suggested that the RD variety of C. longa, developed by the University of the Ryukyus, Okinawa, Japan, is a promising source of natural antioxidants.

Phytochemical analysis and antimicrobial activity of some medicinal plants against selected pathogenic microorganisms

The aim of the present study is to investigate the antimicrobial potency of leaves from various extracts of Capparis zeylanica, Streblus asper and Tribulus terrestris were evaluated. In addition, this is the first report on MIC, MBC/MFC antimicrobial activities of above mentioned plants and also identify the phytochemical, functional groups by GC-MS and FT-IR respectively. Soxhlet extraction method was used for preparation of different extracts viz., aqueous, petroleum ether, ethyl acetate and methanol. The extracts were examined against Staphylococcus epidermidis, Enterococcus faecallis, Salmonella paratyphi, Shigella dysenteriae, Candida albicans and Mycobacterium tuberculosis by agar well diffusion method, and Minimum Inhibitory Concentratioon (MIC), Minimum Bactericidal/Fungicidal Concentration (MBC/MFC) values were determined through micro dilution method. Phytochemical analysis of compounds was carried out by GC-MS analysis and functional groups were identified by FT-IR. Based on the outcome of our results, Ethyl acetate extract Showed significant antimicrobial activity against the tested pathogens especially, for C. albicans (40 mm) followed by ethyl acetate of S. asper against S. paratyphi (38 mm). While, the least inhibition was observed with aqueous extract of T. terrestris against S. paratyphi (10 mm). The MIC ranged from 3.21 mg/ml to 50 mg/ml and MBC/MFC 6.25 mg/ml to 50 mg/ml was recorded. Ethyl acetate extracts of almost all samples showed better activity than other extracts in inhibition growth of pathogens. Phytochemical analysis exhibited the presence of Steroids, tannins and cardiac glycosides were found only in ethyl acetate extract of C. zeylanica. Functional group of leaf extract was confirmed by FT-IR spectrum and GC-MS analysis of the ethyl acetate extract revealed the presence of 20 compounds. The results revealed that ethyl acetate extract of C. zeylanica leaves has potential activity than the other extracts as well as standard drugs (Gentamycin and Ketocozole). Hence, this plant may be recommended for further studies in isolation of active compounds and related pharmacological activities.

A Review of Malaysian Medicinal Plants with Potential Anti-Inflammatory Activity.

This article aims to provide detailed information on Malaysian plants used for treating inflammation. An extensive search on electronic databases including PubMed, Google Scholar, Scopus, and ScienceDirect and conference papers was done to find relevant articles on anti-inflammatory activity of Malaysian medicinal plants. The keyword search terms used were “inflammation,” “Malaysia,” “medicinal plants,” “mechanisms,” “in vitro,” and “in vivo.” As a result, 96 articles on anti-inflammatory activity of Malaysian medicinal plants were found and further reviewed. Forty-six (46) plants (in vitro) and 30 plants (in vivo) have been identified to possess anti-inflammatory activity where two plants, Melicope ptelefolia (Tenggek burung) and Portulaca oleracea (Gelang pasir), were reported to have the strongest anti-inflammatory activity of more than 90% at a concentration of 250 µg/ml. It was showed that the activity was mainly due to the occurrence of diverse naturally occurring phytochemicals from diverse groups such as flavonoids, coumarins, alkaloids, steroids, benzophenone, triterpenoids, curcuminoids, and cinnamic acid. Hence, this current review is a detailed discussion on the potential of Malaysian medicinal plants as an anti-inflammatory agent from the previous studies. However, further investigation on the possible underlying mechanisms and isolation of active compounds still remains to be investigated.

New Records of Potent In-Vitro Antidiabetic Properties of Dalbergia tonkinensis Heartwood and the Bioactivity-Guided Isolation of Active Compounds.

Alpha-glucosidase inhibitory activity has been commonly used for the evaluation of antidiabetic property in vitro. The aim of this study is to investigate and characterize Dalbergia tonkinensis as a potential source of antidiabetic compounds. The screening of the active parts used, such as trunk bark, heartwood, and the leaves of Dalbergia tonkinensis indicated that all these extracted parts used with methanol demonstrated potent α-glucosidase inhibitory activity. The in vitro antidiabetic property of Dalbergia tonkinensis was notably recorded for the first time and showed activity (EC50 = 0.17–0.78 mg/mL) comparable to those of reported potent herbal extracts (EC50 = 0.25–4.0 mg/mL) and higher activity than that of acarbose, a commercial antidiabetic drug (EC50 = 1.21 mg/mL). The stability tests revealed that the heartwood of Dalbergia tonkinensis extract (HDT) possesses high pH stability with relative activity in the range of 80–98%. Further bioassay-guided purification led to the isolation of 2 active compounds identified as sativanone and formononetin from the ethyl acetate fraction and water fraction of HDT, respectively. These α-glucosidase inhibitors (aGIs) show promising inhibition against various types of α-glucosidases. Remarkably, these inhibitors were determined as new mammalian aGIs, showing good effect on rat α-glucosidase. The results suggest that Dalbergia tonkinensis is a potent source of aGIs and suggest promise in being developed as functional food with antidiabetic efficacy. The results of this study also enrich our knowledge concerning current biological activity and constituents of Dalbergia tonkinensis species.

Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery.

The therapeutic properties of plants have been recognised since time immemorial. Many pathological conditions have been treated using plant-derived medicines. These medicines are used as concoctions or concentrated plant extracts without isolation of active compounds. Modern medicine however, requires the isolation and purification of one or two active compounds. There are however a lot of global health challenges with diseases such as cancer, degenerative diseases, HIV/AIDS and diabetes, of which modern medicine is struggling to provide cures. Many times the isolation of “active compound” has made the compound ineffective. Drug discovery is a multidimensional problem requiring several parameters of both natural and synthetic compounds such as safety, pharmacokinetics and efficacy to be evaluated during drug candidate selection. The advent of latest technologies that enhance drug design hypotheses such as Artificial Intelligence, the use of ‘organ-on chip’ and microfluidics technologies, means that automation has become part of drug discovery. This has resulted in increased speed in drug discovery and evaluation of the safety, pharmacokinetics and efficacy of candidate compounds whilst allowing novel ways of drug design and synthesis based on natural compounds. Recent advances in analytical and computational techniques have opened new avenues to process complex natural products and to use their structures to derive new and innovative drugs. Indeed, we are in the era of computational molecular design, as applied to natural products. Predictive computational softwares have contributed to the discovery of molecular targets of natural products and their derivatives. In future the use of quantum computing, computational softwares and databases in modelling molecular interactions and predicting features and parameters needed for drug development, such as pharmacokinetic and pharmacodynamics, will result in few false positive leads in drug development. This review discusses plant-based natural product drug discovery and how innovative technologies play a role in next-generation drug discovery.

Antimicrobial Properties of Plants of Chungtia Village Used Customarily to Treat Skin Related Ailments: From Antimicrobial Screening to Isolation of Active Compounds

Antimicrobial Properties of Plants of Chungtia Village Used Customarily to Treat Skin Related Ailments: From Antimicrobial Screening to Isolation of Active Compounds

Antioxidant activity, antibacterial potential and characterization of active fraction of Dioscorea pentaphylla L. tuber extract collected from Similipal Biosphere Reserve, Odisha, India

ABSTRACT Dioscorea pentaphylla L., a wild tuber is used both as food and medicines among different ethnic groups of Similipal Biosphere Reserve, India. Tubers are used against skin infections. In order to establish and confirm tribal claims, methanol extract was subjected to fractionation. The active fraction (DP1) was subsequently used for further purification and NMR (Nuclear magnetic resonance) characterization. The phytochemical analysis revealed the presence of saponin groups. The antibacterial activity of DP1 was done against selected bacterial strains (Salmonella typhi, Shigella flexneri, Streptococcus pyogenes, Streptococcus mutans and Vibrio cholerae) using DD (disc diffusion), AWD (agar well diffusion) and broth dilution assay. The activity was compared with antibiotics Penicillin and Kanamycin. It was observed that DP1 showed significant inhibitory activity against the tested bacteria. The characterization of DP1 through NMR analysis and presence of proton in carbon position at C-3, C-19, C-18, C-21 and C-27 was same as the known compound “Diosgenin”. Therefore, isolated compound was confirmed to be Diosgenin. The study for the first time showed that, diosgenin present in D. pentaphylla tuber was responsible for antibacterial and antioxidant potential. Present study highlights the importance of Dioscorea species as sources of diverse secondary metabolites for the isolation of active compound(s).

Hypoglycemic and hypolipidemic activity of aqueous leaf extract of Passiflora suberosa L.

Leaves of Passiflora suberosa L. (Family: Passifloraceae; common name: wild passion fruit, devil’s pumpkin) are used in Sri Lankan traditional medicine for treating diabetes. The present study investigated the in vivo ability of P. suberosa leaves to manage blood sugar status and associated cholesterol levels. Mechanisms of action and toxicity were also determined. Phytochemical screening of aqueous extracts of P. suberosa leaves and carbohydrate content of the leaves were determined according to previously published methods. In two group of male mice (n = 9), effects on fasting and random blood glucose levels (BGLs) of different acute doses (0, 25, 50, 100 and 200 mg/kg) of the aqueous leaf extract (ALE) were evaluated at 1, 3, and 5 h post-treatment. In another set of mice, the fasting BGL was evaluated following treatment of 0 or 50 mg/kg ALE (dose prescribed in traditional medicine) for 30 consecutive days. The lipid profile, some mechanism of ALE action (diaphragm glucose uptake, glycogen content in the liver and skeletal muscles) and its toxicity (behavioural observation, food and water intake, hepatoxicity) were also assessed following 30-day treatment. However, sucrose and glucose tolerance tests and intestinal glucose uptake were conducted to determine portion of mechanisms of action following single dose of 50 mg/kg ALE. Phytochemical screening revealed the presence of alkaloids, unsaturated sterols, triterpenes, saponins, flavonoids, tannins and proanthocyanidins. Carbohydrate content of the leaves was 12.97%. The maximum hypoglycemic effect was observed after 4 h of 50 and 100 mg/kg ALE administration. The extract decreased fasting BGL (18%) following an oral sucrose challenge and inhibited (79%) glucose absorption from the intestine. Correspondingly, the levels of glycogen in the liver (61%) and in the skeletal muscles (57%) were found be higher than that of the control group. The levels of total cholesterol (17%) and tri-glyceraldehyde levels (12%) found to be reduced in treated groups. Furthermore, no significant toxic effects were observed in treated groups. The present results suggest that the leaves of P. suberosa can be used to manage blood glucose and cholesterol levels. Isolation of active compounds are recommended for further analysis.

ANTIOXIDANT ACTIVITY OF RED DRAGON FRUIT PEEL (HYLOCEREUS POLYRHIZUS (F.A.C. WEBER) BRITTON AND ROSE) ISOLATES USING 2,2-DIPHENYL-1-PICRYLHYDRAZYL METHOD

Objective: Indonesia is a country which has various natural resources including medicinal plants. Among the plants, red dragon fruit is interesting to be studied. In this study, antioxidant activity of red dragon fruit peel (Hylocereus polyrhizus (F.A.C. Weber) Britton and Rose) isolate was tested using 2,2-diphenyl-1-picrylhydrazyl method.Methods: Isolation of active compounds was performed through the application of vacuum liquid chromatography and preparative thin-layer chromatography (TLC). Antioxidant activity was tested using both TLC and spectrophotometry.Result: Results revealed that the values of IC50 of isolate 1 and 2 were 2.952, 14 μg/mL and 25.635,95 μg/mL, respectively.Conclusion: Isolate of dragon fruit has antioxidant activity. The compound which results in antioxidant activity is terpenoid and steroid.

ANTIOXIDANT ACTIVITY OF RED DRAGON FRUIT PEEL (HYLOCEREUS POLYRHIZUS (F.A.C. WEBER) BRITTON AND ROSE) ISOLATES USING 2,2-DIPHENYL-1-PICRYLHYDRAZYL METHOD

Objective: Indonesia is a country which has various natural resources including medicinal plants. Among the plants, red dragon fruit is interesting to be studied. In this study, antioxidant activity of red dragon fruit peel (Hylocereus polyrhizus (F.A.C. Weber) Britton and Rose) isolate was tested using 2,2-diphenyl-1-picrylhydrazyl method.Methods: Isolation of active compounds was performed through the application of vacuum liquid chromatography and preparative thin-layer chromatography (TLC). Antioxidant activity was tested using both TLC and spectrophotometry.Result: Results revealed that the values of IC50 of isolate 1 and 2 were 2.952, 14 μg/mL and 25.635,95 μg/mL, respectively.Conclusion: Isolate of dragon fruit has antioxidant activity. The compound which results in antioxidant activity is terpenoid and steroid.