Effect of C21 steroidal glycoside of Cynanchum auriculatum on liver and kidney fibrosis through TLR4 pathway / 中国中药杂志

The liver and kidney fibrosis model was established by thioacetamide(TAA) and unilateral ureteral obstruction(UUO) in SD rats. The rats were randomly divided into three groups: model group, low and high-dose groups of C21 steroidal glycosides of Cynanchum auriculatum. Another blank control group was set. Four weeks later, serum was taken to detect the biochemical indexes of liver and kidney function. Urine protein and urine creatinine were detected by kits. Liver and kidney tissue samples were stained with HE and Masson staining, and hydroxyproline content was detected. Western blot was used to detect expressions of fibrotic proteins, inflammatory factors and TLR4 signaling pathways, so as to observe the preventive and therapeutic effects of C21 steroidal glycosides from C. auriculatum on hepatic and renal fibrosis and explore its molecular mechanism. Four weeks later, serum biochemical results showed that liver and kidney functions were seriously damaged, and pathological sections showed that inflammatory cell infiltration, decrease of parenchymal cells, and increase of interstitial fibrosis in liver and kidney tissues. The results showed that low and high doses(150, 300 mg·kg~(-1)) of C21 steroidal glycosides could significantly reduce the collagen deposition and the pathological changes of liver and kidney fibrosis compared with the model group. At the same time, we found that the expression levels of TLR4 and MyD88 signaling pathway proteins were significantly increased in the liver and kidney tissues of the model group, and a large number of NF-κB signaling pathway proteins migrated into the nucleus. On the contrary, the expression levels of TLR4, MyD88 signaling pathway proteins and the nuclear migration of NF-κB were significantly inhibited in the low and high dose groups of C21 steroidal glycosides from C. auriculatum. Therefore, it was speculated that the mechanism of C21 steroidal glycoside for preventive and therapeutic effect on hepatic and renal fibrosis was related to inhibit TLR4/MYD88/NF-κB inflammatory pathway, thus preventing hepatic and renal fibrosis.

Research progress on antitumor activities of C21 steroidal glycosides of Cynanchi Bungei Radix / 中草药

Cynanchi Bungei Radix is a precious Chinese meteria medica of tonifying kidney, benefiting liver, keeping fit, and preventing senility, which also has the pharmacological effect of cancer prevention and anticancer. C21 steroids glycosides are considered as one of its main anticancer active components. In this paper, the main types of C21 steroids and glycosyl groups, the main antitumor mechanism of C21 steroidal glycosides, the effect of C21 steroidal glycosides on different tumors and the influencing factors, and the toxicological research status of C21 steroidal glycosides were reviewed, which can provide references for the following research of C21 steroidal glycosides in Cynanchi Bungei Radix.

Research progress on Cynanchi Bungei Radix / 中草药

Cynanchi Bungei Radix is a traditional Chinese herbal medicine which has been used as a tonic agent owing to its primary abilities of tonifying liver and kidney, nourishing blood and replenishing semen, strengthening tendons and bones, promoting hair growth, and prolonging life. Pharmacological effects and material basis of Cynanchi Bungei Radix have been extensively investigated. This paper reviews the recent research progress of Cynanchi Bungei Radix based on the difference in the pharmacological effects and content of different chemical constituents in different species of Cynanchi Bungei Radix. It provides a scientific basis for further rational application of the medicinal value of different varieties of Cynanchi Bungei Radix.

Two new C steroidal glycosides isolated from Cynanchum komarovii / 中国天然药物

The present study was designed to further investigate the C steroidal glycosides in Cynanchum plants. Two new steroidal glycosides based on a 13, 14:14, 15-disecopregnane-type aglycone, komaroside P (1) and komaroside Q (2), together with three known compounds (3-5) were isolated from the whole herbs of Cynanchum komarovii. The aglycones of compounds 1 and 2 were two new disecopregnane. Their structures were elucidated on the basis of 1D, 2D NMR spectroscopic data and acid hydrolysis. All the compounds (1-5) showed potent inhibitory activities against human leukemia cell lines (HL-60) with IC values ranging from 16.6 to 26.3 μmol·L, compared to the positive control 5-fluorouracil (6.4 μmol·L).

Effects of total C-21 steroidal glycosides from Baishouwu on proliferation invasion and apoptosis of human hepatic cancer HepG2 cells / 中国中药杂志

This study aimed to investigate the inhibitory effect of total C-21 steroidal glycoside (TCSG) from Baishouwu on the proliferation, invasion and apoptosis of human hepatoma HepG2 cells in vitro and the relevant molecular mechanism. The experiment was divded into control group, TCSG groups (25, 60, 150 mg·L⁻¹) and positive control cisplatin group (1.33 mg·L⁻¹). Human hepatocyte L-02 cells and hepatoma HepG2 cells were treated with different concentrations of TCSG. Then, the inhibitory effect of TCSG on the proliferation of HepG2 cells was detected by CCK-8 method. Cell cycle, cell apoptosis and mitochondrial membrane potential were detected by flow cytometry. The apoptotic morphology was observed by Hoechst 33258 staining. Cell migration and invasion abilities were analyzed by Transwell chamber model. The protein expressions of Bcl-2, Bax, caspase 3, cleaved caspase 3 and Cyt C (cytosolchondrial) were detected by Western blot. Compared with the control group, the proliferation of HepG2 cells was significantly inhibited after treatment with different concentrations of TCSG for 48 h in a dose-dependent manner(<0.01), but no obvious effect was observed on the proliferation of L-02 cells. After treatment with TCSG for 48 h, apoptotic morphology such as nuclear shrinkage, fragmentation and semilunar or circular was observed; migration and invasion abilities of cells were significantly decreased, cell cycle was blocked in the G₀/G₁ phase(<0.01), mitochondrial membrane potential was remarkably decreased(<0.01), and so did the ratio of apoptosis(<0.01).Western blot results showed that the protein expressions of Bax, caspase 3, cleaved caspase 3, and Cyt C were significantly up-regulated(<0.05, <0.01), while the Bcl-2 protein was significantly down-regulated(<0.05, <0.01). Furthermore, the ratio of Bax/Bcl-2 was increased (<0.01). The results suggested that TCSG could inhibit the proliferation and invasion of HepG2 cells, and induce the apoptosis of HepG2 cells. The potential mechanism may be related to the blocking of cell cycle and the regulation of the expressions of apoptosis-related proteins by activating mitochondrial pathway.

Two new C steroidal glycosides isolated from Cynanchum komarovii / 中国天然药物

The present study was designed to further investigate the C steroidal glycosides in Cynanchum plants. Two new steroidal glycosides based on a 13, 14:14, 15-disecopregnane-type aglycone, komaroside P (1) and komaroside Q (2), together with three known compounds (3-5) were isolated from the whole herbs of Cynanchum komarovii. The aglycones of compounds 1 and 2 were two new disecopregnane. Their structures were elucidated on the basis of 1D, 2D NMR spectroscopic data and acid hydrolysis. All the compounds (1-5) showed potent inhibitory activities against human leukemia cell lines (HL-60) with IC values ranging from 16.6 to 26.3 μmol·L, compared to the positive control 5-fluorouracil (6.4 μmol·L).