Current Bioactive Compounds - Volume 16, Issue 3, 2020

Background: Molecular docking is probably the most popular and profitable approach in computer-aided drug design, being the staple technique for predicting the binding mode of bioactive compounds and for performing receptor-based virtual screening studies. The growing attention received by docking, as well as the need for improving its reliability in pose prediction and virtual screening performance, has led to the develop Read More

Background: Plant-based products and their derivatives have been widely used in the medicine, nutraceuticals, and the cosmetic and pharmaceutical field for a very long time. A large number of important drugs of modern medicine have also been derived from the plant's sources. Plant products specifically the pure phytochemical also known as ‘biomarkers’ have been used in the food and pharmaceutical industrie Read More

Background: The variety of biological applications of vanadium impressed researchers to develop vanadium based drugs. The most well-known fact of vanadium is that it is necessary for human beings as an insulin-enhancing agent and herein, we mainly provide an overview of vanadium-based drugs and their applications in the medicinal field for the treatment of diseases such as diabetes and cancer. The first part of this review Read More

Background: Valerian extract is widely used in dietary supplements as well as in conventional, traditional and alternative medicines. It is one of the most used herbal plants for the treatment of several disorders, mainly related to the digestive and the nervous systems. Dozens of chemical constituents with pharmacological and therapeutic properties were identified in essential oils and/or other extracts of valerian’s roots, rh Read More

Background: There is much epidemiological evidence that fruits, vegetables, medicinal plants, and their phytochemicals could lower the progression and development of various forms of cancer. The plants are active reservoirs for novel chemical entities and provide a promising resource for the management of cancer. Methods: Several analyses have signified that bioactive flavonoids and phenolic acids might be Read More

Background: Reactive oxygen species and reactive nitrogen species, which are collectively called reactive oxygen nitrogen species, are inevitable by-products of cellular metabolic redox reactions, such as oxidative phosphorylation in the mitochondrial respiratory chain, phagocytosis, reactions of biotransformation of exogenous and endogenous substrata in endoplasmic reticulum, eicosanoid synthesis, and redox reactions in th Read More

Background: Garcinielliptone FC corresponds to a polyprenylated acylphloroglucinol having a benzophenonic core (diphenylmethanone) substituted with isoprenyl(s) group(s) (3-methyl-2-butenyl) and 2-isopropenyl-hex-5-enyl. Objectives: The present work evaluated the antioxidant activity of garcinielliptone FC (GFC) in vitro against non-biological radicals [2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azinobis-3- ethylbenzothi Read More

Background: A series of 1-(2-(2-amino-5-carbamoyl-6-(1-(substitutedphenyl) prop-1-enyl) pyrimidin-4-yloxy)acetyl) semicarbazide (4a-i) derivatives was synthesized from substituted aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride and characterized by analytical and spectral data, FTIR, 1H-NMR and Mass spectroscopy data. Methods: The antiTB action of the synthesized compounds was screened in compariso Read More

Background: In the present study, a bioguided fractionation was realized to isolate bioactive compounds on Fusarium oxysporum f.sp. albedinis (Foa) from Citrullus colocynthis L. Foa is the causal agent of “ Bayoud”, a lethal disease of date palm. Methods: Extracts of Citrullus colocynthis fruits peels using four solvents (n-hexane, dichloromethane, ethanol, chloroform) were tested for antifungal effect on Foa with radial gro Read More

Background: Desert truffles (Terfezia species) are known by their vital nutritional benefits as they are considered as rich sources of vitamins, fatty acid, minerals and proteins. Methods: The chemical constituents of the different solvent extracts of Terfezia species were isolated and identified by column chromatography, spectroscopic and GC-MS analyses. Also, the ethyl acetate and acetone extracts of different fungal isolates, as Read More

Background: Codium intricatum, locally known as Pukpuklo, is a seasonal and edible green alga found in Ilocos Norte, Philippines. In this study, the biochemical content, cytotoxic and inhibitory potential against Matrix Metalloproteinase-1 (MMP-1) production of the polysaccharide-protein fractions from C. intricatum is first reported. MMPs are novel targets for therapeutic intervention with the potential to inhibit tumor grow Read More

Background: Salix gilgiana is a deciduous tree that grows in northern Japan, the Korean peninsula, eastern Russia along the Ussuri River, and northeast China. The stem of this tree is dried and consumed orally as a folk medicine. Our intensive screening of various plant materials found that the MeOH extract of its dried stem exhibited significant antiproliferative activity against HL-60 leukemic cells with an IC50 of 16 pp Read More

Background: Flueggea leucopyrus Willd. leaf has been used since ancient time for its sex enhancing activity by traditional physicians. So, the work was chosen to authenticate the knowledge of pharmaceutical significance of the plant. Methods: The dried leaves of Flueggea leucopyrus were extracted by cold maceration method using water. Aqueous extract of Flueggea leucopyrus leaf was screened for phytochemicals and i Read More

Background: The objective of this study was to investigate the antiproliferative effect of Stachys sieboldii MIQ. extracts on cancer cell lines. Methods: Dried S. sieboldii MIQ. was extracted using acetone/methylene chloride (A+M) or methanol (MeOH), and then fractionated using n-hexane, 85% aq. methanol (MeOH), butanol (BuOH) and distilled water. The cytotoxic activity of S. sieboldii MIQ. against AGS human gas Read More

Background: Novel carboxamides and thioureas of 2,3-dihydro-5,6-dimethoxy-2-((piperidin- 4-yl)methyl) inden-1-one were synthesized and their potential anticholinesterase activities were evaluated. The inhibition potency of the compounds 17a-j and 19a-j against AChE was measured and evaluated using Ellman’s spectrophotometric method. Among carboxamides series, compound 17f, 17i, 17j and among thiourea series, Read More

Background: Arctigenin is a lignan found in Arctium lappa L. (Asteraceae) that displays anti-inflammatory activities. Previous studies showed that the crude extract of A. Lappa has antitumor activity in human liver carcinoma, lung and stomach cancer cells. The aim of this study was to obtain arctigenin from A. lappa L., as well as to evaluate its antiproliferative effects in cells of liver carcinoma (HepG2) and fibroblasts (NIH/3T3) Read More

Background: The marine red alga Plocamium naturally produces halogenated monoterpenes with varied biological activities. In our continuing efforts to discover new lead compounds for the treatment of HIV/AIDS as well as novel antibacterial compounds, various Namibian Plocamium species have been investigated. Methods: A rare but known compound namely 1E,3R,4S,5E,7Z-1-bromo-3,4,8-trichloro-7- (dichlorometh Read More