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OBJECTIVE To explore the improvement effect and potential mechanism of Baicao fuyanqing suppository on bacterial vaginitis （BV） in rats. METHODS The female SD rats were randomly divided into normal group， model group， metronidazole group （positive control， 0.03 g/kg）， Baicao fuyanqing suppository low-dose， medium-dose and high-dose groups （0.18， 0.36， 0.72 g/kg）， with 8 rats in each group. Except for the normal group， the rats in other groups were injected subcutaneously with 0.2 g of Estradiol benzoate injection+20 μL of Escherichia coli suspension （2×108～3×108 cfu/mL） through the vaginal opening to establish the BV rat model. Administration groups were given relevant medicine vaginally， while the normal group and the model group were given normal saline， once a day， for 6 consecutive days. Twenty-four hours after the last administration， the vaginal appearance score and vaginal pH were measured for each group of rats. The levels of cytokines [interleukin-1β （IL-1β）， IL-2， IL-13， immunoglobulin A （IgA）] in vaginal lavage fluid were determined. The morphology of the uterus and accessories， and pathological changes in the vaginal tissue were observed. The expressions of Toll-like receptor 2 （TLR2）， TLR4 and nuclear factor-κB （NF-κB） in vaginal tissues were determined. RESULTS Compared with the normal group， the uterus edema， the irregular shape of uterus and accessories， the vaginal mucosa hyperplasia， and the massive desquamation of epithelial cells were observed in the model group， complicating with massive infiltration of inflammatory cells； vaginal opening redness and swelling score and secretion score， vaginal pH， the levels of proinflammatory cytokine IL-1β and IL-2， the protein expressions of TLR2， TLR4 and NF- κB were all increased or up-regulated， while the levels of IgA and anti-inflammatory cytokine IL-13 decreased significantly （P＜0.05 or P＜0.01）. Compared with the model group， varying cn degrees of improvement in uterine and accessories， and vaginal tissue lesions in rats were observed in administration groups， and most of the quantitative indicators mentioned above showed significant improvement （P＜0.05 or P＜0.01）. CONCLUSIONS Baicao fuyanqing suppository has a certain improvement effect on inflammatory symptoms in BV rats， and its mechanism may be related to the inhibition of the TLR/NF-κB signaling pathway.
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OBJECTIVE To analyze quality maker （Q-marker） of Ka nggongyan soft capsule （KSC）. METHODS The fingerprints of 20 batches of KSC were established by ultra high performance liquid chromatography （UPLC）method. Similarity Evaluation System of TCM Chromatographic Fingerprint （2012 edition）were used to evaluate the similarity and confirm common peaks. The contents of norisoboldine ，leonurine hydrochloride ，forsythoside B ，acteoside，poliumoside and isoacteoside were determined by the same UPLC method. Targets and pathways related to KSC in the treatment of cervicitis were screened and analyzed by network pharmacology and molecular docking method to construct a “component-target-pathway”network，and analyze its potential Q-marker. RESULTS Twelve common peaks were identified in the fingerprints of 20 batches of KSC ，and the similarity was greater than 0.99. Six common peaks were identified ，including norisoboldine ，leonurine hydrochloride ，forsythoside B，acteoside，poliumoside and isoacteoside. The contents of the above 6 components were 1.336-1.774，0.093-0.143，4.970-5.888， 0.505-0.623，5.206-6.226 and 0.785-0.895 mg/g，respectively. By network pharmacology analysis ，14 key targets and 94 pathways were obtained ，and their binding energies to the core targets （protein kinase B 1，tumor necrosis factor ）were all less than －6.4 kJ/cal. CONCLUSIONS Six components such as norisoboldine and leonurine hydrochloride are potential Q-marker of KSC.
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OBJECTIVE：To isolate and purify baicalin metabolites from rat bile ，and to study its effect on the proliferation of liver cancer HepG 2 cells. METHODS ：Totally of 6 SD rats were collected ，anesthetized and then intubated with bile ducts. They were given baicalin （168 mg/kg）intragastrically after the rats were awake as well as the bile sample 1 was collected during 24 h after intragastric administration. After processed ，bile sample 1 was preliminarily analyzed by HPLC. Another 5 SD rats were anesthetized and intubated in the same way as above ，and then given baicalin intragastrically （400 mg/kg）. The bile sample 2 was collected during 48 h after intragastric administration. After processed ，the bile sample 2 was isolated and purified by semi-preparative HPLC. The isolated metabolites were identified by using UV ，IR，MS and NMR ，as well as based on physical and chemical properties. MTT method combined with high content cell imaging analysis system was used to study the effect of the metabolites on the proliferation of HepG 2 cells. RESULTS ：Baicalin was mainly metabolized into metabolite 1 and metabolite 2 through bile. After isolation and purification ， they were identified as oroxylin A- 7-O-β-D-glucuronide and 2726719792@qq.com baicalein 6-O-β-D-glucuronide. The results of MTT assay showed that the metabolite 2 had a significant inhibitory effect 分析。E-mail：gaoxl@gmc.edu.cn on the proliferation of HepG 2 cells，and its IC 50 was 90 µg/mL；the results of high content cell imaging analysis showed that at a certain concentration metabolite 2 may inhibit proliferation by changing the mitochondrial distribution and membrane permeability of HepG 2 cells（studies on the pharmacological activities of metabolism 1 had been reported ，it was skipped in this study ）. CONCLUSIONS ：In this study ，two baicalin bile metabolites were successfully isolated and identified ，of which baicalein 6-O-β-D-glucuronide has a significant inhibitory effect on the proliferation of HepG 2 cells.
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OBJECTIVE： Compare the contents of free ellagic acid and total ellagic acid in fruits， roots and levels of Rosa roxburghii， and to evaluate the in vitro anti-oxidant activity of ethanol extract of three medicinal parts of R. roxburghii. METHODS： Free ellagic acid and total ellagic acid were obtained from different medicinal parts of R. roxburghii by ultrasonic extraction and acid hydrolysis， respectively. The contents of them were determined by UPLC. Using half-clearance value （IC50） as anti-oxidant evaluation index， free radical scavenging test of 1，1-diphenyl-2-trinitrophenylhydrazine （DPPH） and 2，2′ -binitro-bis（3-ethylbenzothiazoline-6-sulfonic acid） （ABTS） were conducted for ethanol extract of different medicinal part， using vitamin C （VC） as positive control. RESULTS： There were significant differences in the content of free ellagic acid and total ellagic acid in different medicinal parts of R. roxburghii. The content level of free ellagic acid was in descending order： R. roxburghii leaves （38.49 mg/g）＞R. roxburghii fruits （20.59 mg/g）＞R. roxburghii roots （11.35 mg/g）； the content level of total ellagic acid was in descending order： R. roxburghii leaves （197.08 mg/g） ＞ R. roxburghii fruits （49.36 mg/g） ＞ R. roxburghii roots （21.86 mg/g）. The contents of total ellagic acid in the fruits and roots of R. roxburghii were twice as much as that of free ellagic acid in corresponding parts； the contnets of total ellagic acid in the leaves of R. roxburghii were five times higher than that of free ellagic acid in corresponding parts. In the DPPH free radical scavenging test and ABTS free radical scavenging test， the order of antioxidant activity was VC ＞ R. roxburghii leaves＞R. roxburghii fruits＞R. roxburghii roots. There was no statistical significance in the effects of R. roxburghii leaves [IC50 to DPPH free radical and ABTS free radical were （4.57±0.70）、（115.99±2.21） μg/mL] and R. roxburghii fruits [IC50 to DPPH free radical and ABTS free radical were （5.12±0.24）、（127.61±3.31） μg/mL]， compared with the effects of VC [IC50 to DPPH free radical and ABTS free radical were （4.47±0.38）、（121.42±2.65） μg/mL] （P＞0.05）. CONCLUSIONS： Among fruits， roots and leaves of R. roxburghii， the content of free （total） ellagic acid is the highest in the R. roxburghii leaves and in vitro anti-oxidant activity of its ethanol extract is the strongest.
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Object To develop and utilize a folk-medicine of Yunnan Province, Lethariella cladonioides (Nyl.) Krog. Methods The constituents were extracted with 80% ethanol and isolated with silica gel column chromatography. The structures were identified by physicochemical properties and spectral analysis. Results Two unknown constituents were elucidated from the extract as 3-aldehyde-6-methyl-2, 4-dihydroxy-ethyl-benzoate (Ⅰ), and 4-methyl-2, 6-dihydroxy-benzaldehyde (Ⅱ). Conclusion They are both new constituents obtained firstly.