ABSTRACT
Bupleuri Radix has both liver protection and hepatotoxicity. Saponins are the main pharmacodynamic and toxic components of Bupleuri Radix. Based on zebrafish physical model and the model of alcoholic fatty liver( AFL) pathology,the liver toxic and protective effect of saikosaponin a( SSa) were assessed. The results indicated that 1. 77 μmol·L-1 SSa showed protective effect to AFL zebrafish. 5. 30 μmol·L-1 SSa was hepatotoxic to healthy zebrafish,but it showed protective effect to AFL zebrafish. 5. 62 μmol·L-1 SSa was hepatotoxic to healthy and AFL zebrafish. This study is benefit for clinical safety of saikosaponin a.
Subject(s)
Animals , Chemical and Drug Induced Liver Injury , Fatty Liver, Alcoholic , Drug Therapy , Oleanolic Acid , Pharmacology , Toxicity , Saponins , Pharmacology , Toxicity , ZebrafishABSTRACT
Aim To investigate the protective effect of Qi ZhiXiaoke granules ( QZXK ) on nerve injury using zebrafish and nerve cell injury models. Methods The nerve injury model was established using wild zebrafish AB line, 72 hours after fertilization treated with 1-methyl-4-phenyl-1 , 2 , 3 , 6-four pyridine ( MPTP ) .Then QZXK of different doses were administered for three days,and the trajectory of the zebrafish behavior was recorded and analyzed. Neuroblastoma PC12 cells were incubated with different concentrations of QZXK and MPTP,and the cell viability of PC12 cells was de-tected by MTT. The mitochondrial membrane potential and expression of apoptosis related protein Caspase3 were measured by kits. Results Compared with con-trol group,MPTP reduced the movement distance of ze-brafish,and with the increase of concentration, QZXK promoted the movement distance and reversed the swimming behavior abnormality of zebrafish. Compared with control group, QZXK could inhibit the apoptosis induced by MPTP and promote the cell viability of PC12 cells with MPTP. QZXK improved the membranepotential and decreased the expression of Caspase3 . Conclusions QZXK exerts neuroprotective effect in the process of nerve injury induced by MPTP. The mechanism may be related with inhibiting apoptosis of neural cells. These experiment provides experimental and theoretical foundation for QZXK promoting cogni-tive function.
ABSTRACT
AIM: To investigate the chemical constituents and their biological activities of the aerial parts of Euphorbia tibetica. METHOD: Compounds were isolated and purified by various chromatographic methods, and their structures were elucidated through the use of extensive spectroscopic techniques including 2D-NMR, the structures of compounds 5 and 6 were confirmed by single-crystal X-ray crystallography. Bioactivities of all the isolated compounds were evaluated by the MTT method on A549 and anti-angiogenesis assay. RESULTS: One new compound, methyl 4-epi-shikimate-3-O-gallate (1), together with twenty-three known constituents (2-24) were isolated from the aerial parts of E. tibetica. CONCLUSION: Compound 1 is new, and the other compounds were isolated from this plant for the first time. Compounds 5-7, 9, 11, 17, 18 and 20 exhibited inhibitory effects on the growth of human lung cancer cell A549 and compounds 5, 7, 12, 13, 17 and 19 showed anti-angiogenic effects in a zebrafish model.
Subject(s)
Angiogenesis Inhibitors/chemistry , Angiogenesis Inhibitors/pharmacology , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Euphorbia/chemistry , Growth Inhibitors/chemistry , Growth Inhibitors/pharmacology , Animals , Cell Line , Cell Proliferation/drug effects , Humans , Molecular Structure , ZebrafishABSTRACT
To study the chemical constituents of K. oblongifolia, silica gel column chromatography, MCI and Sephadex LH-20 were used to separate the 70% acetone extract of the stems of K. oblongifolia. The structures of the isolated compounds have been established on the basis of physicochemical and NMR spectroscopic evidence as well as ESI-MS in some cases. Twenty compounds were obtained and identified as heteroclitalignan A (1), kadsulignan F (2), kadoblongifolin C (3), schizanrin F (4), heteroclitalignan C (5), kadsurarin (6), kadsulignan O (7), eburicol (8), meso-dihydroguaiaretic acid (9), kadsufolin A (10), tiegusanin M (11), heteroclitin B (12), (7'S)-parabenzlactone (13), angeloylbinankadsurin B (14), propinquain H (15), quercetin (16), kadsulignan P (17), schizanrin G (18), micrandilactone C (19) and (-)-shikimic acid (20). Compouds 1, 5, 8, 11-15, 18 and 20 were isolated from this plant for the first time. Toxicity of compounds 1-10 were evaluated with zebrafish model to observe the effect on its embryonic development and heart function. The results showed that compounds 7, 9 and 10 caused edema of zebrafish embryo and decreased the heart rate of zebrafish, which exhibited interference effect on heart development of zebrafish.
Subject(s)
Animals , Embryo, Nonmammalian , Guaiacol , Toxicity , Kadsura , Chemistry , Lignans , Toxicity , Plant Extracts , Toxicity , Quercetin , Toxicity , Triterpenes , Toxicity , Zebrafish , EmbryologyABSTRACT
AIM@#To investigate the chemical constituents and their biological activities of the aerial parts of Euphorbia tibetica.@*METHOD@#Compounds were isolated and purified by various chromatographic methods, and their structures were elucidated through the use of extensive spectroscopic techniques including 2D-NMR, the structures of compounds 5 and 6 were confirmed by single-crystal X-ray crystallography. Bioactivities of all the isolated compounds were evaluated by the MTT method on A549 and anti-angiogenesis assay.@*RESULTS@#One new compound, methyl 4-epi-shikimate-3-O-gallate (1), together with twenty-three known constituents (2-24) were isolated from the aerial parts of E. tibetica.@*CONCLUSION@#Compound 1 is new, and the other compounds were isolated from this plant for the first time. Compounds 5-7, 9, 11, 17, 18 and 20 exhibited inhibitory effects on the growth of human lung cancer cell A549 and compounds 5, 7, 12, 13, 17 and 19 showed anti-angiogenic effects in a zebrafish model.
