Elham Amin

Triterpenoidal saponins: bioactive secondary metabolites from Zygophyllum coccineum.

Phytochemical investigation of the aerial parts of Zygophyllum coccineum L. led to the isolation of nine ursane-type triterpene saponins (1- 9), including the new one; zygophylloside S (1), together with a known flavonoid glycoside (10) and a sterol glycoside (11). The isolated compounds were tested for antifungal activity against several important plant pathogens and for insecticidal activity against two important mosquito species. Among the isolated compounds 1, 3, 5, 6, and 9 showed 32-77 % fungal growth inhibition at a concentration of 30 µM against Phomopsis viticola. Compound 9 showed 90 % and 80 % mosquitocidal activity at 3.1 µg/0.5 µL against Aedes aegypti and Culex quinquefasciatus, respectively.

Biologically-guided isolation of leishmanicidal secondary metabolites from Euphorbia peplus L.

Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Moreover, the severe side effects and the reported drug resistance make it an urgent need to search for effective drugs that can replace or supplement those currently used. In a research program designed to investigate the antileishmanial activity of plants collected from the Egyptian flora, twenty extracts from fifteen plants growing in Egypt have been investigated for in vitro leishmanicidal activity against Leishmania donovani promastigotes. Among the tested extracts, the methanol extract of Euphorbia peplus aerial parts exhibited a significant antileishmanial activity as it produced 100% inhibition of growth with activity similar to amphotericin B. The total extract was subjected to liquid-liquid fractionation using solvents of different polarities, followed by testing the antileishmanial activity of the successive fractions. Phytochemical exploration of the active n-hexane fraction (which produced 75% inhibition of growth) led to isolation of four compounds: simiarenol (1), 1-hexacosanol (2), β-sitosterol (3), and β-sitosterol-3-O-glucoside (4) from the biologically active sub-fractions. Structure elucidation was aided by 1D and 2D NMR techniques. In conclusion, E. peplus plant has many non-polar secondary metabolites that can be used as drug leads for treatment of leishmaniasis.

Epigenetic Modifiers Induce Bioactive Phenolic Metabolites in the Marine-Derived Fungus Penicillium brevicompactum

Fungi usually contain gene clusters that are silent or cryptic under normal laboratory culture conditions. These cryptic genes could be expressed for a wide variety of bioactive compounds. One of the recent approaches to induce production of such cryptic fungal metabolites is to use histone deacetylases (HDACs) inhibitors. In the present study, the cultures of the marine-derived fungus Penicillium brevicompactum treated with nicotinamide and sodium butyrate were found to produce a lot of phenolic compounds. Nicotinamide treatment resulted in the isolation and identification of nine compounds 1–9. Sodium butyrate also enhanced the productivity of anthranilic acid (10) and ergosterol peroxide (11). The antioxidant as well as the antiproliferative activities of each metabolite were determined. Syringic acid (4), sinapic acid (5), and acetosyringone (6) exhibited potent in vitro free radical scavenging, (IC50 20 to 30 µg/mL) and antiproliferative activities (IC50 1.14 to 1.71 µM) against HepG2 cancer cell line. Furthermore, a pharmacophore model of the active compounds was generated to build up a structure-activity relationship.

Acylated Iridoids and Rhamnopyranoses from Premna odorata (Lamiaceae) as Novel Mesenchymal–Epithelial Transition Factor Receptor Inhibitors for the Control of Breast Cancer

Phytochemical investigation of Premna odorata Blanco, Lamiaceae, leaves afforded three new acylated iridoid glycosides 1–3 and two new acylated rhamnopyranoses 9 and 10, in addition to ten known compounds. The structures of the new compounds were confirmed using extensive 1D and 2D NMR analysis. Molecular modeling study suggested the potential of the acylated rhamnopyranoses to bind at the c‐Met kinase domain. Cell‐free Z′‐LYTE™ assay testing revealed the good c‐Met phosphorylation inhibitory activity of 9, followed by 8, and 10, with IC50 values of 2.5, 6.9, and 12.7 μM, respectively. The (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) cell proliferation assay testing against the human c‐Met expressing highly invasive MDA‐MB‐231 suggested compound 9 as the most active with IC50 value of 13.3 μM. Testing of compound 9 against multiple phenotypic breast cancer cell lines including MCF‐7, BT‐474 cells, and MDA‐MB‐468 proved enhanced activity against the highly c‐Met expressing triple‐negative breast cancer cell lines. Acylated rhamnopyranoses are potential novel c‐Met inhibitors appropriate for future optimizations to control c‐Met‐dependent breast malignancies. Copyright

Premna odorata Volatile Oil as a New Mycobacterium tuberculosis Growth Inhibitor for the Control of Tuberculosis Disease

Aims: This study aimed to identify and compare Premna odorata Blanco volatile oil (VO) for the first time; isolated from different plant organs (leaves, young stems, and flowers) with evaluating the oil antituberculosis (anti-TB) activity. Study Design: Experimental design was carried out by using hydrodistillation method, GC/MS analysis and MeDipro Mycobacterium tuberculosis (MTB) Antigen ELISA Technique (MMA-ELISA) accompanied by polymerase chain reaction (PCR) analysis. Place and Duration of Study: This study was carried out at Faculty of Pharmacy, Beni-Suef University, between May to July 2017. Methodology: P. odorata VO was identified using GC/MS analysis, the oil anti-TB activity was evaluated using in vitro and in vivo MMA-ELISA accompanied by PCR analysis. Original Research Article Elmaidomy et al.; EJMP, 21(4): 1-11, 2017; Article no.EJMP.38375 2 Results: GC/MS analysis revealed that P. odorata VO consisted of monoterpenes, sesquiterpenes, diterpenes and higher alkanes; where monoterpenes and sesquiterpenes were represented the major oils fractions. Trans-caryophyllene (29.403% & 14.638%) and β-phellandrene (22.390% & 11.701%) were the major compounds in the leaves and young stems oils, respectively. While αpinene (38.160%) was a characteristic component of the flowers oil. MMA-ELISA showed that a dose of 100 μl/ml in vitro and 300 μl/ml in vivo; the leaves, young stems, and the flowers oils separately had significant anti-TB activities with measured values > 1.5 μg/ml MTB antigen; while the three organs oils in combination 1:1:1 increased the potency of the oils against MTB with measured values < 1.5 μg/ml MTB antigen with PCR negative analysis. Conclusion: P. odorata VO exhibited Anti-TB activity which Anti-TB could be related to the presence of cyclic terpenes (major) and acyclic oxygenated terpenes (minor) compounds.