Advances in Pharmacological Studies of Calycosin-7-O-β-D-glucoside

The isoflavone compound Calycosin-7-O-β-D-glucoside (CG) is an active monomer component extracted from the dry roots of the leguminous plant Astragalus mongolicus and Astragalus. It is also one of the main active ingredients in the Astragalus that is a commonly used traditional herb. CG has obvious effects of anti-oxidation, anti-virus, inhibition of melanin formation, and immunosuppression. With the advancement of modern technology, it has become a pivotal subject that the adjuvant therapy or even substitute for the synthetic drug of monomer of Chinese herb in medical field. In recent years, with the deepening of research on the mechanism of action of CG, which has been found that its pharmacological effects are very extensive, such as the anti-tumor effect and the effect on cerebrovascular diseases of CG. This review summarizes the pharmacological effects and the latest research progress of CG.

Mechanisms of Apigenin-7-glucoside As a Hepatoprotective Agent

Ixeris chinesis (Thunb.) Ankai has been used as a Chinese folk medicine, but only scanty information is available on the physiological and biochemical functions of the compounds extracted from I. chinesis. In the present study the effects of apigenin -7-glucoside (APIG) isolated from I. chinesis against liver injury caused by carbon tetrachloride (CCl4) were investigated. Methods The contents of malondialdehyde (MDA), glutamic pyruvic transaminase (GPT), glutamic oxaloacetic transaminase (GOT), and reduced glutathione (GSH) were evaluated by spectrophotography. The content of 8-Hydroxydeoxyguanosine (8-OHdG) was measured with high-performance liquid chromatography (HPLC) equipped with electrochemical and UV detection methods. The antioxidant activity of APIG was evaluated using chemiluminescence single photon counting technology. Results CCl4 significantly increased the enzyme activities of GPT and GOT in blood serum, as well as the level of MDA and 8-OHdG in liver tissue, and decreased the levels of GSH. Pretreatment with APIG was able not only to suppress the elevation of GPT, GOT, MDA and 8-OHdG, and inhibit the reduction of GSH in a dose-dependent manner in vivo, but also to reduce the damage of hepatocytes in vitro. On the other hand, we also found that APIG had strong antioxidant activity against reactive oxygen species (ROS) in vitro in a concentration-dependent manner. Conclusion The hepatoprotective activity of APIG is possibly due to its antioxidant properties, acting as scavengers of ROS. These results obtained in vivo and in vitro suggest that APIG has protective effects against hepatic oxidative injury induced by chemicals. Further studies on the pharmaceutical functions and immunological responses of APIG may help its clinical application.

Calycosin-7-O-β-D-glucopyranoside stimulates osteoblast differentiation through regulating the BMP/WNT signaling pathways

The iso fl avone calycosin-7-O-β-D-glucopyranoside(CG) is a principal constituent of Astragalus membranaceus(AR) and has been reported to inhibit osteoclast development in vitro and bone loss in vivo. The aim of this study was to investigate the osteogenic effects of CG and its underlying mechanism in ST2 cells. The results show that exposure of cells to CG in osteogenic differentiation medium increases ALP activity, osteocalcin(Ocal) m RNA expression and the osteoblastic mineralization process. Mechanistically, CG treatment increased the expression of bone morphogenetic protein 2(BMP-2), p-Smad 1/5/8, β-catenin and Runx2, all of which are regulators of the BMP- or wingless-type MMTV integration site family(WNT)/β-catenin-signaling pathways. Moreover, the osteogenic effects of CG were inhibited by Noggin and DKK-1 which are classical inhibitors of the BMP and WNT/β-catenin-signaling pathways, respectively. Taken together, the results indicate that CG promotes the osteoblastic differentiation of ST2 cells through regulating the BMP/WNT signaling pathways. On this basis, CG may be a useful lead compound for improving the treatment of bone-decreasing diseases and enhancing bone regeneration.

HPLC-DAD-MS研究黄芪的化学成分

目的建立HPLC-DAD-MS快速分离分析黄芪Astragali Radix化学成分的方法。方法色谱柱为Thermo Hypersil-Hypurity C18(150 mm×2.1 mm,5μm)分析柱,柱温40℃,流动相水-甲醇(梯度洗脱),体积流量0.25 mL/min。二极管阵列扫描范围200～370 nm。质谱采用大气压化学电离(APCI+)离子源,扫描范围m/z 100～650。结果通过与已有文献报道的质谱、紫外光谱和保留行为比较可以初步定性5个化合物,分别为calycosin-7-O-β-D-glycoside、ononin、calycosin、formononetin、(3R)-7,2′-dihydroxy-3′,4′-dimethoxyisoflavan。结论因为能够同时提供相对分子质量、紫外光谱和保留行为,所以HPLC-DAD-MS是一种分析中药化学成分的有力方法。

云南沉香果壳的化学成分研究

目的研究云南沉香Aquilaria yunnanensis果壳的化学成分。方法采用硅胶、Sephadex LH-20柱色谱和半制备HPLC技术进行分离、纯化,结合理化性质和波谱数据鉴定化合物的结构。结果从云南沉香果壳的95%乙醇提取物的醋酸乙酯萃取部位中分离得到13个化合物,分别鉴定为trans-linalool-3,6-oxide-7-O-β-D-(6′-O-acetyl)-glucoside(1)、苯乙基-8-O-β-D-(6′-O-乙酰基)-葡萄糖苷(2)、芒果苷(3)、鸢尾酚酮-3,5-C-β-D-二葡萄糖苷(4)、山柰酚-3-O-β-D-葡萄糖苷(5)、木犀草素-7-O-β-D-葡萄糖苷(6)、异鼠李素-3-O-β-D-葡萄糖苷(7)、山柰酚-3-O-β-D-(6″-对-香豆酰基)-葡萄糖苷(8)、香叶醇-1-O-β-D-葡萄糖苷(9)、3-[2-甲酰基-5-(羟甲基)-1H-吡咯-1-基]戊二酸(10)、大麻酰胺D(11)、淫羊藿次苷D2(12)、松柏苷(13)。结论化合物1为新的单萜苷类化合物,命名为云南沉香苷C,化合物2为新天然产物,7、9~13为首次从沉香属植物中分离得到,所有化合物均为首次从该植物中分离得到。