ABSTRACT
<p><b>OBJECTIVE</b>To compare the anti-hypercholesterolemic and cholesterol absorption inhibitory activities between total saponin of Dioscorea panthaica (TSDP) and diosgenin (Dio).</p><p><b>METHOD</b>TSDP and Dio were given ig or i.p. to mice or rats treated with cholesterol feed to evaluate their preventive and therapeutic effect on hypercholesterolemia. TSDP or Dio and cholesterol were mixed with pig bile to form the micelle, then the freeing cholesterol was detected to evaluate inhibitory effect of the both compounds on cholesterol absorption.</p><p><b>RESULT</b>Dio (80 and 160 mg.kg-1) showed significantly therapeutic and preventive effect on hypercholesterolemia in mice, while TSDP showed a certain preventive activity only at a big dose (400 mg.kg-1). The intraperitoneal injection of Dio (20 and 40 mg.kg-1) to mice suffered from hypercholesterolemia was effective, but TSDP showed no effective. The serum total cholesterol level was decreased when rats were pre-treated with TSDP (200 and 400 mg.kg-1, ig) and Dio (200 and 100 mg.kg-1, ig). However, the hypercholesterolemia-preventing activity of Dio was stronger than that of TSDP. In addition, inhibitory effect of Dio on cholesterol micelle formation was still stronger than that of TSDP.</p><p><b>CONCLUSION</b>The preventive and therapeutic activity of Dio against hypercholesterolemia indused by cholesterol in mice or rats is stronger than that of TSDP. The anti-hypercholesterolemia mechanism of Dio is probably related with its cholesterol absorption inhibitory activity.</p>
Subject(s)
Animals , Female , Male , Mice , Rats , Anticholesteremic Agents , Pharmacology , Cholesterol , Blood , Dioscorea , Chemistry , Diosgenin , Pharmacology , Hypercholesterolemia , Blood , Drug Therapy , Phytotherapy , Plants, Medicinal , Chemistry , Rats, Wistar , Saponins , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To investigate the antitumor activity of Diosgenin in vivo and in vitro.</p><p><b>METHOD</b>S-180, HepA, U14 and EAC transplant mice were given Diosgenin ig or i.p. everyday for 10 days, from the next day when they were inoculated in axilla. Tumor growth inhibit rates were calculated. Four kinds of cells, MCF, L929, A375-S2 and HeLa, were incubated respectively with Diosgenin in vitro. Tumor growth inhibit rates were also calculated.</p><p><b>RESULT</b>In vivo, both ig and i.p., Diosgenin inhibited S-180, HepA, U 14 mice transplant tumor, the inhibit rates being 30%-50%, but it did not inhibit the EAC mice transplant tumor. In vitro, Diosgenin inhibited L929, HeLa, MCF cell growth, and IC50 were 1.2, 18.2, 19.8 micrograms.mL-1 respectively, but it did not significantly affect A375-S2 cells.</p><p><b>CONCLUSION</b>Diosgenin has an obvious antitumor activity on S-180, HepA, U14 transplant mice in vivo and L929, HeLa, MCF cells in vitro.</p>
Subject(s)
Animals , Female , Humans , Male , Mice , Antineoplastic Agents, Phytogenic , Therapeutic Uses , Carcinoma, Ehrlich Tumor , Drug Therapy , Dioscorea , Chemistry , Diosgenin , Therapeutic Uses , Inhibitory Concentration 50 , Neoplasm Transplantation , Phytotherapy , Plants, Medicinal , Chemistry , Sarcoma 180 , Drug Therapy , Tumor Cells, CulturedABSTRACT
<p><b>OBJECTIVE</b>To study the rat intestinal bacteria metabolism of total saponins of Dioscorea pathaica (TSDP) in vitro, and characterize the metabolites in serum and urine of rats after oral administration of TSDP 900 mg.kg-1.</p><p><b>METHOD</b>TSDP metabolites were detected with thin-layer chromatography (TLC) and combination of electrospray ionization mass spectrometry (ESI-MS) and sequential tandem mass spectrometry (MSn).</p><p><b>RESULT</b>In vitro, TSDP was decomposed easily by rat intestinal bacteria, and metabolites DP-1, DP-2, DP-4, DP-5 and diosgenin (Dio) were observed with prolongation of incubation time by ESI-MS2. In vivo, in the full-scan positive mass spectrum of the rat urine sample, the ion peak at m/z 415 (M-H) and its characteristic fragmentations at m/z 397 and m/z 271 in the MS/MS spectrum were identified with that of metabolite Dio, therefore metabolite Dio was deduced to exist in the rat urine, and metablite Dio was allso detected in the rat serum sample.</p><p><b>CONCLUSION</b>TSDP is decomposed easily by rat intestinal bacteria and metabolite diosgenin is absorbed into blood after oral administration of TSDP.</p>
Subject(s)
Animals , Male , Rats , Biotransformation , Dioscorea , Chemistry , Diosgenin , Metabolism , Gram-Negative Anaerobic Bacteria , Metabolism , Intestines , Microbiology , Molecular Structure , Plants, Medicinal , Chemistry , Rats, Wistar , Saponins , Pharmacokinetics , Spectrometry, Mass, Electrospray IonizationABSTRACT
<p><b>AIM</b>To study the mechanism of evodiamine-induced growth inhibition of HeLa cells.</p><p><b>METHODS</b>HeLa cells viability and the effect of caspase inhibitors on evodiamine-induced apoptosis were measured by crystal violet assay. Changes in cellular morphology were observed by phase-contrast microscopy. Apoptosis-specific nucleosomal DNA fragmentation was assayed by agarose gel electrophoresis.</p><p><b>RESULTS</b>Evodiamine was found to inhibit HeLa cell growth in dose- and time-dependent manners. Caspase-3 inhibitor, z-Asp-Glu-Val-Asp-fmk (z-DEVD-fmk) was shown to partially inhibit evodiamine-induced apoptosis. However, caspase-1 inhibitor, Ac-Tyr-Val-Ala-Asp-chloromethyl-ketone (Ac-YVAD-cmk), did not antagonize evodiamine induced cell death.</p><p><b>CONCLUSION</b>Evodiamine suppresses the growth of HeLa cells in vitro by apoptosis. Evodiamine-induced apoptosis is partially dependent on caspase-3 pathway in HeLa cells. Other apoptotic pathways might be also related to the induction of apoptosis by evodiamine.</p>