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Osteoporosis （OP） is a common bone disease affecting the quality of life and causing huge medical burden to the patients and society. The occurrence of OP is mainly caused by excessive bone resorption and insufficient bone formation， which are directly influenced by external calcium ion balance. Calcium imbalance can impair bone integrity， reduce the calcium supply to the bone， and lower the calcium content in the bone， thus triggering OP. Drugs are the main anti-OP therapy in modern medicine， which， however， may cause adverse reactions and drug dependence. Chinese medicines have good clinical effects and high safety in treating OP， being suitable for long-term use. Recent studies have shown that Chinese medicines can alleviate estrogen deficiency， regulate bone cell and calcium metabolism， which is crucial for the formation and development of OP. The transient receptor potential cation channel superfamily V members 5 and 6 （TRPV5 and TRPV6， respectively） affect bone homeostasis by mediating the transmembrane calcium ion transport in the intestine （TRPV6） and kidney （TRPV5）. Therefore， TRPV5/6 is one of the key targets to understand the anti-OP mechanisms of the effective parts of Chinese medicines， which is worthy of further study. This paper summarizes the research results about the anti-OP effects of Chinese medicines in the last two decades， especially the mechanism of regulating calcium metabolism， aiming to provide new ideas for the basic research， clinical application， and drug development of OP treatment.
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OBJECTIVE To compare anti-ischemic stroke （IS） effect of different extraction parts from Gastrodia elata， and to provide reference for screening the anti-IS effective parts of G. elata. METHODS G. elata was extracted and separated by ethanol reflux extraction and ethyl acetate extraction. The rat model of diffuse cerebral thrombosis was induced by internal carotid artery injection of arachidonic acid （AA）； the anti-IS effect of G. elata powder， ethanol extract of G. elata， residue of ethanol extract of G. elata， ethyl acetate extract of G. elata， residue of ethyl acetate extract of G. elata， gastrodin and aspirin （positive control drug） were investigated with the content of Evans blue （EB） in the ischemic brain tissue as index. RESULTS Compared with model group， aspirin， ethanol extract of G. elata and ethyl acetate extract of G. elata could significantly decrease the content of EB in the ischemic brain tissue of model rats （P＜0.05）. G. elata powder had the tendency to reduce the content of EB in the ischemic brain tissue of model rats， without statistical significance （P＞0.05）. The residue of ethanol extract of G. elata， residue of ethyl acetate extract of G. elata and gastrodin had little effect on the content of EB in the ischemic brain tissue of model rats. CONCLUSIONS Both ethanol extract of G. elata and ethyl acetate extract of G. elata have anti-IS effects， which are stronger than that of G. elata powder.
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OBJECTIVE To screen the effective anti-depressant part from Coreopsis tinctoria and study its mechanism. METHODS The anti-depressant effects of 30％，50％，70％ and 90％ ethanol elution fractions from 75％ ethanol extract of C. tinctoria（CCTE）were investigated by tail suspension test and forced swimming test. Mice head-drop test ，reserpine antagonistic test，yohimbine toxicity enhancement test and in vitro monoamine oxidase （MAO） inhibition test were used to explore the mechanism of the relationship between the effective parts and 5-hydroxytryptamine （5-HT） and norepinephrine （NE） nerves. RESULTS The 50％ and 70％CCTE could significantly shorten the accumulative immobility time in tail suspension test and forced swimming test （P＜0.05 or P＜0.01），increase the number of head-shaking times （P＜0.01），reverse the eyelid ptosis ， hypothermia and immobility caused by hematopin （P＜0.05 or P＜0.01），and increase the number of dead mice caused by yohimbine toxicity （P＜0.01）. IC 50 of okanin （CCT-6），isookanin（CCT-7）and taxifolin （CCT-8）against MAO were 8.71，37.89 and 67.07 µmol/L，respectively. CONCLUSIONS The 50％ and 70％CCTE are the effective anti-depressant parts of C. tinctoria . Its anti-depressant effect may be related to the reinforcement of 5-HT and the activation of NE nerves. The inhibition of CCT- 6， CCT-7 and CCT- 8 against MAO may be one of the anti-depressant mechanism of C. tinctoria .
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OBJECTIVE: To study the metabolic differences of the effective fractions of total glycosides of Jinkui Shenqi Pills in liver homogenate and blood by high performance liquid chromatography-electrospray ion trap mass spectrometry (HPLC-ESI/MSn). METHODS: The in vitro metabolism of the glycosides was studied using rat liver homogenate and the in vivo metabolism was investigated in rats. The metabolites were detected by HPLC-ESI/MS/MS. According to the molecular ion peak in negative ion mode, the molecular weight information of the compound was obtained. RESULTS: A total of 13 chemical components were detected in the rat liver homogenate after incubation for 20 min. Eight prototype components were detected in both liver homogenate and plasma while pentagalloylglucose was only found in the liver homogenate. A total of nine metabolites were detected in plasma, and only four metabolites were found in the liver, which were shared by those in plasma. CONCLUSION: The four common metabolites are produced through liver metabolism of the total glycosides. The RESULTS of this study have important implications for revealing the metabolic mechanisms of the total glycoside constituents in vitro and in vivo.
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Aims To study single dose toxicity of poly-phenols effective parts from Punica granatum,to eval-uate their safety,and thus to provide a theoretical basis for drug development and clinical use.To observe their protective effect on ethanol-induced gastric ulcer in rats.Methods 50 healthy Kunming mice were ran-domly divided into five groups and given different doses of polyphenols’effective parts from Punica granatum via intragastric administration.Toxicity and death in each group of mice were observed and recorded after administration for 14 d.The median lethal dose was calculated by Bliss method.70 rats were randomly di-vided into normal group,model group(constant volume of normal saline),sanjiuweitai particles(1 850 mg· kg-1 )group,colloidal bismuth subcitrate (33 mg · kg-1 )group and polyphenols effective parts from Puni-ca granatum low-dose,medium-dose,high-dose(430, 852,1 704 mg·kg-1 )groups.On the 9th day of 10 days’gavage,all except the normal group were fed ethanol (1.5 mL/only)to induce gastric mucosal inju-ry in rats with acute gastric ulcer.Gastric ulcer index, the rate of ulcer inhibition were calculated for each group.The morphological changes of gastric mucosa were observed.The gastric mucosa levels of PGE2 , NO,SOD and MDA were determined.Results The LD50 and 95%confidence limit of the polyphenols’ef-fective parts from Punica granatum were 8 520.9 mg· kg-1 and 7 291.2 ~9 914.4 mg·kg-1,respectively. Pathology showed that the organs receiving dose of 16 000 mg · kg-1 had different degrees of damage . Compared with the model group,the extract from Puni-ca granatum significantly repaired the gastric mucosa, and significantly increased the gastric mucosa levels of NO and reduced MDA content,and improved SOD content and the levels of PGE2 .Conclousion The dose of 5 063 mg · kg-1 of polyphenols effective part from Punica granatum showed no death.The dose of 16 000 mg · kg-1 of polyphenols effective parts from Punica granatum could cause varying degrees of dam-age in heart,liver,lung,kidney or the death of mice. The LD50 and 95% confidence limit of the polyphenols effective parts from Punica granatum were 8 520.9 mg ·kg-1 and 7 291.2 ~9 914.4 mg·kg-1,respective-ly.The extract from Punica granatum plays a protective role against gastric mucosa damage induced by absolute ethanol,and the mechanism may be related to promo-ting ulcer epithelial cells synthesis,enhancing mucosal regeneration function,regulating NO content and en-hancing antioxidant capacity.
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Objective To establish a qualitative and quantitative method for controlling the quality of Radix Puerariae and its preparation. Methods The qualitative fingerprint of effective part (extract part of ethyl acetate) was obtained by using RP-HPLC with methanol-water (42∶58) as mobile phase and UV detection at 250 nm . The quantitative measurement of effective components (puerarin and daidzein) was finished under the above chromatographic conditions. And the 11 kinds of different samples of Radix Puerariae were analyzed by the method. Results Under the qualitative conditions, the 5 common peaks in RP-HPLC fingerprint of the effective part could be used as index peaks for qualitative identification. In RP-HPLC quantitative analysis, the recoveries of the method were 98.0% with RSD of 1.30% for puerarin and 95.4% with RSD of 1.61% for daidzein, respectively. The amount of puerarin and daidzein in Radix Puerariae was 0.213%～3.626% and 0.012%～ 0.049% , respectively. Conclusion The analytical method with qualitative fingerprint of effective part and quantitative measurement of effective components of Radix Puerariae can be accurately used for controlling its quality.