Three New Polyphenol Derivatives from the Fruits of Macaranga Monandra and their Antioxidant Potential.

Phytochemical investigation of the methanol extract from the fruits of Macaranga monandra (Euphorbiaceae Muell. et Arg.) afforded one new geranylated 1',2'-dihydrophenanthrene and two new flavonoid derivatives, named macamondrin (1), macamondrione A (2) and B (3) respectively. The structures of these compounds were elucidated mainly by NMR, mass spectral data and in comparison with data from the literature. Along with compounds 1-3, nine known compounds among which oleanolic acid (4); daucosterol (5); 3ß-acetoxy-11α,12α-epoxytaraxerol (6); 3,3',4-tri-O-methylellagic acid (7); 3,3',4,4'-tetra-O-methylellagic acid (8); 4'-O-methyl-6-isoprenylapigenin (9); 4'-O-methyl-8 isoprenylkaempférol (10); 4'-O-methyl-6-isoprénylkaempférol (11); 6-isoprénylkaempférol (12), were also isolated. Crude extracts as well as isolated compounds were evaluated for their antioxidant activity using the ABTS, DPPH and FRAP methods. It appears that the 50 % radical scavenging concentrations ranging from 6.26 to 11.7 µg/ml on the ABTS radical, from 1.77 to 48.22 µg/ml on the DPPH radical, and from 1.54 to 67.97 µg/ml with the FRAP method. For the compounds tested, very good antioxidant activities were observed, which clearly shows that these molecules can have an anti oxidative stress potentiel.

Synthesis of Ester-Linked Ursolic Acid-Based Hybrid Compounds: Potential Antibacterial and Anticancer Agents.

The molecular hybridization of two or more drugs into a single molecule is an effective drug design approach to reduce pill burden and improve patient treatment adherence. Ursolic acid-based hybrid compounds were synthesized and characterized followed by molecular docking studies. In vitro studies against various bacterial strains and human cancer cells (MDA-MB-231, HeLa, and MCF-7) were performed. Compounds 14-19, 21, 34, 31, and 30 demonstrated significant antibacterial activities with MIC values of 15.625 µg/ml. Compounds 29 and 34 were more cytotoxic than ursolic acid, with IC50 values of 46.99 and 48.18 µg/ml. Compounds 29 and 34 in the docking studies presented favourable binding interactions and better docking energy against the Epidermal Growth Factor Receptor (EGFR) than the parent compound, ursolic acid. The findings revealed that the ursolic acid scaffold is a promising precursor for the development of molecules with promising anticancer and antimicrobial activities. However, more studies are needed to fully understand their mode of action.

Myrianthus arboreus P. Beauv (Cecropiaceae) Extracts Accelerates Sexual Maturation, and Increases Fertility Index and Gestational Rate in Female Wistar Rats.

Background: Despite the wide use of leaves of Myrianthus arboreus (Cecropiaceae) in several African countries including Cameroon as food and against amenorrhea and female infertility, it has never been tested for this purpose. Methods: Using immature female Wistar rats, the impact of M. arboreus on the sexual maturation parameters (vaginal opening, ovarian relative weight and follicle maturation, gonadotropins and ovarian hormones serum levels) and fertility index has been evaluated through a 30-day oral administration of aqueous and methanol extracts of leaves at the doses of 20, 110 and 200 g/kg/day. Results: Aqueous extract increased the ovarian relative weight (p < 0.001), progesterone (p < 0.001) and gonadotropins (p < 0.001) serum levels, and induced the maturation of ovarian follicles. The methanol extract additionally induced an early vaginal opening (p < 0.001), uterine growth (p < 0.01) and increased estradiol (p < 0.001) serum levels. The fertility index generally increased following treatments, while the gestation rate remained almost unaffected except at the highest tested dose of M. arboreus extracts where lowest values were observed. Conclusion: Globally, M. arboreus induced an early puberty onset and an increased fertility rate validating at least in part its traditional use for female infertility.