ABSTRACT
AIM To study the scavenging free radicals and antioxidant effect of diterpenoid compounds. METHODS Reductive cytochrome C (cytc Ⅱ) in fenton reaction system was detected by spectrophotometer to indicate the scavenging capability of the test compounds scavenging. The NO - 2 content was measured by spectrophotometery. DNTB method was used to measure the content of GSH. RESULTS oridonin (Orid), ponicidin (Pon), amethystonal(Ame), Isodonoiol(Iso) 50,100,200 ?mol?L -1 could scavenge hydroxyl radicals(?OH) in Fenten's reaction. Orid, Pon, Ame, Iso 400, 800 ?mol?L -1 could scavenge superoxide anion(O -? 2) in xanthine/xanthine oxidase system. Orid, Pon, Ame, Iso 2,4 ?mol?L -1 decreased the content of NO - 2, in macrophages stimulated by LPS and also inhibited the decrease of GSH content in liver cell caused by CCl 4. CONCLUSION Orid, Pon, Ame, Iso all have antioxidative effect through scavenging ?OH, NO - 2 and inhibiting lipid peroxidation.
ABSTRACT
Probimane was first synthesized and developed in Shanghai Institute of Materia Medica, Chinese Academy of Science as a novel antit umor agent. Male mice were injected iv 〔14C〕 probimane 3.7?105Bq/20g( 5.62? 107Bq/g ) . At 0.5h,higher radioactivities were found in S87 tumor, kidney, bladder, and vertebra, moderate in skim, lung, liver, blood vessel and gut. The radioactivities tended to decre-aseafter 3h except in the tumor, kidney, and gut in which radioactivities persisted. After 12h, only a trace of radioactivity was detected n intestine. The distribution of probimane correlated with its therepeutic efficacy and toxicity.
ABSTRACT
AIM To study oridonin induced apoptosis in human leukemia HL 60 cells. METHODS Cell morphology, agarose gel electrophoresis and flow cytometry were used. RESULTS Oridonin had significant apoptotic inductive effect on HL 60 cells in both concentration and time dependent fashion. The marked morphological changes including condensed chromatin, nuclear fragmentation and apoptotic body were observed. Typical DNA ladder in agarose gel electrophoresis and pre G 1 peak in flow clytometric analysis were also observed in the cells exposed to Ori. CONCLUSION Oridonin can induce apoptosis in human leukemia HL 60 cells.
ABSTRACT
Pharmaco kinetics of probimane in rabbits was studied by using high-performance liguid chromatography. After the oral adiminis-tration of probimane 75mg/kg to rabbits,the phatmacokinetic characteristics are found to fit a two compartment open model. The pharmacokinetic parameters are: tl/2? = 0.1933h, tl/2? = 4.9568h, K21 =2.9410h-1, K10=0.6492h-1 K12=3.75l2h-1 AUC = 98.9l01h ? mg/L, Cls=0.7583L? kg-1 ? h-1, V/f(c) = 1.0924L ? kg-1, VSS=1.5114L. kg-1.
ABSTRACT
It has been reported that bimolane can inhibit either humoral or cell-mediated immunological responses in vivo in mice & the inhibition of humoral immunity (by bimolane) is stronger than that of cellular immunity. Author investigated the influence of bimolane on the mitogen-induced mouse lymphocyte proliferation. Bimolane inhibited the lymphocyte proliferation induced by Con A(concana-valin A), PHA ( phy tohemagglutinin ) or LPS(lipopoiysaccharide) . Bimolane dose-dependently inhibited LPS-induced lymphocyte proliferation with remarkable inhibition at 1.56 mg/L bimolane. The inhibition of Con A-induced or PHA-induced lymphocyte proliferation by bimolane, however, began to appear at above 6.25 mg/L bimolane. The bimolane-mediated inhibition of the proliferation of the lymphocytes was not due to a nonspecific toxicity, because the preincubation of spleen cells with 25 mg/L bimolane for 24h did not make the cells died tested by trypanblau exclusion method.The data suggest that B lymphocytes are more sensitive to the bimolane-mediated inhibition than T lymphocytes.
ABSTRACT
Lentinan could enhance the proliferative response of the mouse spleen lymphocytes to FHA, LPS ( Lipopolysaccharides ) and MLR ( Mixed Lymphocyte Reaction ) in vitro in a concentration-dependent manner. At the concentration of 25M-g/ml, it had the most prominent effects and the enhancing rates were 42.1%, 24.1% and 27.1% respectively. At much higher or lower concentrations, however, it had almost no effects. But lentinan at 25H-g/ml could inhibit the prolifera-tire response to Con A ( Concanavalin A ) and the inhibitory action increased with the increase in the concentration. At the concentration of 200 p-g/ml, the inhibition rate was 52.2%.