ABSTRACT
Objective Study on the effect of isocorydine in human cervical cancer Siha cells xenografts in nude mice , to explore the inhibition mechanism of isocorydine in cervical carcinoma .Methods Establishment of human cervical cancer Siha cells subcutaneous xenografts model in BALB /c (nu/nu) nude mice.When the average diameter of the transplanted tumor≥0.5 cm, mice were randomly assigned into control group and experimental group .In experimental group, the model was administered by intraperitoneal injection of different doses of isocorydaline .After 4 weeks, the tumor tissues were removed , the histopathological changes of the tumor were observed by HE staining , and the ex-pression of proteins in the tumor tissue were observed by immunohistochemical staining and Western blot .Results Compared with the control group , the tumor volume of experimental group was significantly decreased ( P<0.05);the cell morphology transformed from stem cells to epithelioid cells , and the expression of E-cadherin was significantly in-creased while the expression of HPV 16E6 and vimentin was decreased .Conclusions Isocorydine may inhibit the de-velopment of cervical cancer by inhibiting the expression of E 6 protein and EMT-related signaling pathway .
ABSTRACT
Isocorydine and its analogs were extracted from Dicranostigma leptopodum and Stephania yunnanensis through the method of natural products chemistry. Its derivatives were prepared by chemical structure modifications from isocorydine. MTT method was used to study the inhibitory effect of those compounds on the growth of HepG2, HeLa and MGC-803 cancer cell lines in vitro. The results showed that isocorydine and its analogs all have the growth inhibition for those cancer cell lines. This paper investigated the structure-activity relationship of isocorydine and its derivatives with anticancer activity in the aspect of stereochemical structure, functional groups positions of the compounds and the electron density of aromatic rings based on the single crystal diffraction structure and the molecular docking of EGFR and isocorydine.
ABSTRACT
Aim To investigate the effect of isocorydine on arrhythmia in rats induced by myocardial ischemia/reperfusion injury. Methods SD rats were randomly divided into 6 groups: sham group, myocardial ische-mia/reperfusion group, verapamil group and isoc-orydine group of 2. 5 , 5 , 10 mg · kg-1 , each group having 16 rats. Left anterior descending ( LAD ) was tied up to establish the injury model of myocardial is-chemia. ECG was recorded for analysis. The ischemic and infarction area was measured and indexes of SOD, MDA, GSH-Px in the myocardial were determined. Re-sults Isocorydine could significantly reduce the inci-dence of arrhythmia induced by ischemic/reperfusion, including VT, VF;and reduce ischemic and infarction area. Further study demonstrated that isocorydine could increase myocardial SOD and GSH-Px, but de-crease myocardial MDA. Conclusion Isocorydine has a protective effect on the myocardial ischemia/reperfu-sion injury, which might be related to its anti-oxidative function.
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A simple and effective high-performance liquid chromatography with diode-array detection method coupled with a liquid-liquid extraction pretreatment has been developed for determining the pharmacokinetics and tissue distribution of a novel structurally modified derivative (8-acetamino-isocorydine) of isocorydine. According to the in vivo experiments data calculations by DAS 2.0 software, a two-compartment metabolic model was suitable for describing the pharmacokinetic of 8-acetamino-isocorydine in rats. 8-Acetamino-isocorydine was absorbed well after oral administration, and the absolute bioavailability was 76.5%. The half-life of 8-acetamino-isocorydine after intravenous and oral administration was 2.2 h and 2.0 h, respectively. In vivo, 8-acetamino-isocorydine was highly distributed in the lungs, kidney and liver; however, relatively little entered the brain, suggesting that 8-acetamino-isocorydine could not easily pass through the blood brain barrier. Our work describes the first characterization of the pharmacokinetic parameters and tissue distribution of 8-acetamino-isocorydine. The acquired data will provide useful information for the in vivo pharmacology of 8-acetamino-isocorydine, and can be applied to new drug research.
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Objective: To study the alkaloids chemical composition from stem of Corydalis decumbens. Methods: The compounds from the ethyl acetate part were separated and purified through various kinds of chromatographic methods and their structures were identified by physico-chemical properties of spectroscopic methods. Results: Eleven alkaloids compounds were isolated and identified. They were protopine (1), muramine (2), β-allocryptopine (3), cryptopine (4), (6S, 6aS, M)-isocorydine (5), bulbocapine (6), (+)-egenine (7), (-)-corypalmine (8), bicuculline (9), (-)-7'-O-methylegenine (10), and epi-coryximine (11). Conclusion: Compounds 5 and 10 are isolated from this genus for the first time. Compound 3, 8, and 10 are isolated from this plant for the first time.
ABSTRACT
After 45 min ligation of the gerbils' bilateral carotid arteries and then 24h reperfusion,the effects of water soluble Pollen flavone element from buckwheat, Isocorydine on the stroke index of 45 min cerebral ischemia followed by reperfusion 6h and the mortality of reperfusion 24h were evaluated .The results indicated that pollen element from buckwheat could decrease the stroke index and mortality rate dramatically, while Isocorydine had no effects.It was speculated that the beneficial effects of pollen element from buckwheat on cerebral damage following ischemia with reperfusion might be due to its depressing effect on the metabolism of free radicals.