Antidiabetes constituents, cycloartenol and 24-methylenecycloartanol, from Ficus krishnae

Abstract

Ficus krishnae stem bark and leaves are used for diabetes treatment in traditional medicines. Stem bark of F. krishnae was sequentially extracted with hexane, methanol and water, and these extracts were tested for their antihyperglyceamic activity by oral glucose tolerance test (OGTT) in overnight fasted glucose loaded normal rats. Hexane extract showed significant glucose lowering activity in OGTT, and the triterpene alcohols (cycloar-tenol+24-methylenecycloartanol) (CA+24-MCA) were isolated together from it by activity guided isolation and characterized by NMR and mass spectroscopy. The ratio of the chemical constituents CA and 24-MCA in (CA+24-MCA) was determined as 2.27:1.00 by chemical derivatization and gas chromatographic quantification. (CA+24-MCA) in high fat diet-streptozotocin induced type II diabetic rats showed significant antidiabetes activity at 1 mg/kg and ameliorated derailed blood glucose and other serum biochemical parameters. Cytoprotective activity of (CA+24-MCA) from glucose toxicity was evaluated in cultured RIN-5F cells by MTT assay and fluorescent microscopy. (CA+24-MCA) in in vitro studies showed enhanced cell viability in RIN-5F cells and significant protection of beta cells from glucose toxicity. Both in in vivo and in vitro studies (CA+24-MCA) showed enhancement in insulin release from the beta cells. In short term toxicity studies in mice (CA+24-MCA) did not show any conspicuous toxic symptoms. The combination of the phytosterols (CA+24-MCA) obtained through activity guided isolation of the stem bark of F. krishnae showed significant activity, and therefore is a promising candidate for new generation antidiabetes drug development.

Aloe vera and Streptozotocin-Induced Diabetes Mellitus

“…To date, five steroids have been isolated from A. vera gel including cycloartanol ( 5 ), 24-methylene-cycloartanol, lophenol ( 6 ), 24-methyl-lophenol, and 24-ethyl-lophenol (Kahramanoğlu et al 2019 ). It has been shown in mouse model investigations that oral administration of lophenol and cycloartanol can prevent metabolic disorders such as obesity and diabetes (Misawa et al 2008 ; Misawa et al 2012a ; Misawa et al 2012b ; Nair et al 2020 ). The A. vera -isolated sterols can dose-dependently activate peroxisome proliferator-activated receptors (PPAR) (Nomaguchi et al 2011 ).…”

Triterpenoids with α-glucosidase inhibitory activities from the roots of Codonopsis pilosula var. modesta

“…modesta for the first time, and compound 2 was separated from the Codonopsis genus for the first time. Previous biological investigations of compounds 2 and 3 have demonstrated anti-inflammatory, 21 anticonvulsant, 21 and antifungal 22 activities of 2, and anti-diabetes, 23 antiinflammatory, 24 and antitubercular 25 activities of 3.…”

Deep-Sea Natural Products from Extreme Environments: Cold Seeps and Hydrothermal Vents

“…Novel fatty acids (1-10) (Figure 1) were purified from the two cold-seep-derived mussels Bathymodiolus japonicus and B. platifrons, collected at a depth of 1209 m at latitude 35 • The cold-seep clam Calyptogena phaseoliformis, collected in the Japan Trench at a depth of 6354-6367 m, yielded eight novel fatty acids (11)(12)(13)(14)(15)(16)(17)(18) (Figure 1). They were determined by gas chromatography-mass spectrometry analysis of 4,4-dimethyloxazoline derivatives.…”