Identification and Cytotoxic Evaluation of Pregnane Saponins from the Twigs and Leaves of Dregea volubilis.

Four new polyhydroxy pregnane glycosides, named volubilosides G-K (3, 5-7), along with three known secondary metabolites, dregeoside Da1 (1), dregeoside Ka1 (2), and volubiloside E (4) were isolated from the twigs and leaves of Dregea volubilis (DV). The chemical structures of these compounds (1-7) were elucidated using spectroscopic techniques (1D and 2D NMR and HR-ESI-MS analyses) and compared with those in the published literature. Compounds (1-7) were evaluated for cytotoxicity against eight cancer cell lines (MB49, K562, MKN-7, HT29, A549, MCF-7, MDA-MB-231, and HepG2), revealing varying levels of cytotoxic effects with IC50 values ranging from 4.29 to 21.05 µM. The results indicated that compounds 1-7 may serve as potential lead compounds for the discovery and development of novel anti-cancer drugs.

Spray-dried Solid Lipid Nanoparticles for Enhancing Berberine Bioavailability via Oral Administration.

BACKGROUND: Berberine (BBR), an Eastern traditional medicine, has expressed novel therapeutic activities, especially for chronic diseases like diabetes, hyperlipemia, hypertension, and Alzheimer's disease. However, the low oral bioavailability of BBR has limited the applications of these treatments. Hence, BBRloaded solid lipid nanoparticles (BBR-SLNs) were prepared to improve BBR absorption into systemic circulations via this route. METHODS: BBR-loaded solid lipid nanoparticles (BBR-SLNs) were prepared by ultrasonication and then transformed into solid form via spray drying technique. The size morphology of BBR-SLNs was evaluated by dynamic light scattering (DLS) and scanning electron microscope (SEM). Crystallinity of BBR and interaction of BBR with other excipients were checked by spectroscopic methods. Entrapment efficiency of BBR-SLNs as well as BBR release in gastrointestinal conditions were also taken into account. Lastly, SLN's cytotoxicity for loading BBR was determined with human embryonic kidney cells (HEK293). RESULTS: Stearic acid (SA), glyceryl monostearate (GMS), and poloxamer 407 (P407) were selected for BBRSLNs fabrication. BBR-SLNs had homogenous particle sizes of less than 200 nm, high encapsulation efficiency of nearly 90% and loading capacity of above 12%. BBR-SLN powder could be redispersed without significant changes in physicochemical properties and was stable for 30 days. Spray-dried BBR-SLNs showed a better sustained in vitro release profile than BBR-SLNs suspension and BBR during the initial period, followed by complete dissolution of BBR over 24 hours. Notably, cell viability on HEK293 even increased up to 150% compared to the control sample at 100 µg/mL BBR-unloaded SLNs. CONCLUSION: Hence, SLNs may reveal a promising drug delivery system to broaden BBR treatment for oral administration.