Dibenzocyclooctadiene lignans from Kadsura coccinea alleviate APAP-induced hepatotoxicity via oxidative stress inhibition and activating the Nrf2 pathway in vitro.

Phytochemical investigation on the roots of Kadsura coccinea led to the isolation five previously unknown dibenzocyclooctadiene lignans, named heilaohusuins A-E (1-5). Their structures determined by NMR spectroscopy, HR-ESI-MS, and ECD spectra. Hepatoprotection effects of a series of dibenzocyclooctadiene derivatives (1-68) were investigated against acetaminophen (APAP) induced HepG2 cells. Compounds 2, 10, 13, 21, 32, 41, 46, and 49 showed remarkable protective effects, increasing the viabilities to > 52.2% (bicyclol, 52.1 ± 1.3%) at 10 µM. The structure-activity relationships (SAR) for hepatoprotective activity were summarized, according to the activity results of dibenzocyclooctadiene derivatives. Furthermore, we found that one new dibenzocyclooctadiene lignan heilaohusuin B attenuates hepatotoxicity, the mechanism might be closely correlated with oxidative stress inhibition via activating the Nrf2 pathway.

Kadsura coccinea: A rich source of structurally diverse and biologically important compounds.

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family. It has been used in traditional Chinese medicine (TCM) for the treatment of rheumatoid arthritis and gastroenteric disorders. The initial phytochemical work focused on the identification of some structurally novel and diverse natural products, which turned the attention of many researchers towards this plant. Thus far, 202 compounds have been reported in this plant. Lignans and terpenoids were found as the main chemical constituents of this plant. Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers. The isolated compounds of this plant have shown different bioactivities including anti-tumor, anti-HIV, anti-inflammatory, nitric oxide (NO) production inhibitory and other pharmacological effects. This review systematically summarizes all the phytochemical and pharmacological work done so far on K. coccinea, and can be used as a reference for future research on this plant.

Microbial transformation of 18beta-glycyrrhetinic acid by Cunninghamella elegans and Fusarium lini, and lipoxygenase inhibitory activity of transformed products.

The microbial transformation of 18beta-glycyrrhetinic acid (1) by Cunninghamella elegans afforded a metabolite, 3beta,7beta-dihydroxy-11-oxo-olean-12-en-30-oic acid (2), while fermentation of 1 with Fusarium lini afforded a metabolite, 3,11-dioxo-olean-12-en-30-oic acid (3). Compound 3 exhibited a potent lipoxygenase (LOX) inhibitory activity. The structures of these metabolites were elucidated on the basis of spectroscopic techniques.

Urease inhibitor from Datisca cannabina linn.

A new flavonoid datisdirin (1), along with eight known compounds tectochrysine, cearoin, sideroxyline, ursolic acid, corosolic acid, arjunolic acid, erythrodiol and oleanolic acid, were isolated from the ethyl acetate fraction of D. cannabina Linn. The structure of compound 1 was deduced on the basis of its spectral data. Datisdirin showed activity against the ureases enzyme.

Alpha-glucosidase inhibitory and antioxidant acridone alkaloids from the stem bark of Oriciopsis glaberrima ENGL. (Rutaceae).

The CH2Cl2/MeOH extract of the stem bark of Oriciopsis glaberrima ENGL. afforded four new acridone alkaloids namely oriciacridone C, D, E and F along with six known compounds: atalaphyllidine, oleanolic acid, butulinic acid, beta-sitosterol, stigmasterol, glucoside of stigmasterol and one synthetically known acridone: 1,3,5-trihydroxy-4-prenylacridone. The structures were established on the basis of MS, 1D and 2D NMR experiments. The acridones 1, 4 and 5 showed potent activity against alpha-glucosidase, while the acridones 1-5 showed moderate free radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH).