黄槿化学成分的研究

目的 研究黄槿Hibiscus tiliaceus枝叶的化学成分。方法 采用硅胶柱色谱、Sephadex LH-20柱色谱分离化合物,并通过理化数据测定和波谱技术分析鉴定化合物的结构。结果 从黄槿枝叶70%乙醇提取物中分离得到14个化合物,分别鉴定为木栓酮（1）、β-谷甾醇（2）、香草醛（3）、syriacusin A（4）、hibiscolactone（5）、莨菪亭（6）、臭矢菜素C（7）、反式丁烯二酸（8）、山柰酚（9）、槲皮素（10）、胡萝卜苷（11）、壬二酸（12）、丁二酸（13）、芦丁（14）。结论 化合物7、9、10为首次从该属植物中分离得到,化合物3～5、8、12～14为首次从该植物中分离得到。     

柿叶中黄酮类化合物及提取工艺研究进展

柿叶来源于柿科柿属植物柿Diospyros kaki的干燥叶。柿叶中的主要化学成分有黄酮、三萜等,其中黄酮类化合物是中药制剂脑心清片的主要活性成分,在脑心清片治疗心脑血管疾病的过程中起关键作用,因此柿叶中的黄酮类成分具有较高的经济和药用价值。针对柿叶中的黄酮类化合物结构类型及柿叶黄酮的不同提取工艺进行综述,以期为柿叶中黄酮成分的深入开发和应用提供参考依据。     

Hepatoprotective effects of kaempferol 3-O-rutinoside and kaempferol 3-O-glucoside from Carthamus tinctorius L. on CCl4-induced oxidative liver injury in mice

Safflower (Carthamus tinctorius L.) is a traditional medicinal and edible herb with a long history of use in China. In this study, a model of hepatotoxicity induced by carbon tetrachloride (CCl₄) in mice was used to investigate the hepatoprotective effects of kaempferol 3-O-rutinoside (K-3-R) and kaempferol 3-O-glucoside (K-3-G), two kaempferol glycosides isolated from C. tinctorius L. K-3-R and K-3-G, at doses of 200 mg/kg and 400 mg/kg, were given orally to male mice once/d for 7 days before they received CCl₄ intraperitoneally. Our results showed that K-3-R and K-3-G treatment increased the level of total protein (TP) and prevented the CCl₄-induced increases in serum aspartate aminotransferase (AST), serum alkaline phosphatase (ALP), and hepatic malondialdehyde (MDA) levels. Additionally, mice treated with K-3-R and K-3-G had significantly restored glutathione (GSH) levels and showed normal catalase (CAT) and superoxide dismutase (SOD) activities, compared to CCl₄-treated mice. K-3-R and K-3-G also mitigated the CCl₄-induced liver histological alteration, as indicated by histopathological evaluation. These findings demonstrate that K-3-R and K-3-G have protective effects against acute CCl₄-induced oxidative liver damage.     

Kaempferol Inhibits P. intermedia Lipopolysaccharide‐Induced Production of Nitric Oxide Through Translational Regulation in Murine Macrophages: Critical Role of Heme Oxygenase‐1‐Mediated ROS Reduction

Background: Nitric oxide (NO) could be a potential target for the development of new therapeutic approaches to the treatment of periodontal disease because this molecule plays a significant role in the tissue destruction observed in periodontitis. In this study, the authors investigate the effect of kaempferol on the production of NO by murine macrophage‐like RAW264.7 cells stimulated with lipopolysaccharide (LPS) from Prevotella intermedia, a pathogen implicated in periodontal disease, and try to determine the underlying mechanisms of action. Methods: NO production was assayed by measuring the accumulation of nitrite in culture supernatants. Real‐time polymerase chain reaction was performed to quantify inducible NO synthase (iNOS) and heme oxygenase‐1 (HO‐1) mRNA expression. iNOS and HO‐1 protein expression and phosphorylation of c‐Jun N‐terminal kinase and p38 were characterized via immunoblot analysis. Reactive oxygen species (ROS) production was measured using the redox‐sensitive fluorescent probe 2′,7′‐dichlorodihydrofluorescein diacetate. Results: Kaempferol significantly inhibited NO production and expression of iNOS protein in P. intermedia LPS‐stimulated RAW246.7 cells without affecting iNOS mRNA expression. Kaempferol upregulated HO‐1 expression in LPS‐activated cells. Inhibition of HO‐1 activity by tin protoporphyrin IX (SnPP) abolished the suppressive effect of kaempferol on NO production. In addition, kaempferol significantly attenuated P. intermedia LPS‐induced increase of intracellular ROS, and SnPP blocked this reduction. Treatment with antioxidants downregulated the production of LPS‐induced NO. Conclusions: Kaempferol inhibits NO production and iNOS protein expression in P. intermedia LPS‐stimulated RAW264.7 cells at the translational level via HO‐1‐mediated ROS reduction and could be an efficient modulator of host response in the treatment of periodontal disease.     

UPLC-Q-Orbitrap HRMS法同时测定秦艽炮制前后8种成分

目的建立一种UPLC-Q-Orbitrap HRMS定量分析方法,同时测定秦艽炮制前后8种化学成分(龙胆苦苷、马钱苷酸、獐牙菜苦苷、獐牙菜苷、木犀草素、异牡荆素、芹菜素、山柰酚)含量的变化。方法采用Waters Acquity UPLC BEH C_(18)(100 mm×2.1 mm,1.7μm)色谱柱,以甲醇-0.1%甲酸水溶液为流动相进行梯度洗脱,体积流量0.3 mL/min,柱温35℃。质谱采用负离子检测模式进行检测。结果秦艽经清炒、酒炙后环烯醚萜类含量均明显升高,且清炒后龙胆苦苷和马钱苷酸含量具有统计学差异。黄酮类在清炒和酒炙后含量变化不大。2类成分总的含量变化为环烯醚萜类成分含量清炒酒炙生品;黄酮类成分含量生品酒炙清炒。结论建立的UPLC-Q-Orbitrap HRMS同时测定秦艽炮制前后8种成分的方法准确、稳定,为进一步研究秦艽炮制前后主要成分的变化奠定了基础。     

委陵菜HPLC指纹图谱及多指标含量测定研究

目的建立委陵菜的指纹图谱及多指标含量测定方法,为委陵菜的质量标准提升提供实验依据。方法采用HPLC法,色谱柱Diamonsil C18(250 mm×4.6 mm,5μm),以乙腈-0.1%磷酸水为流动相,梯度洗脱;体积流量1.0 mL/min;柱温25℃;进样量10μL;检测波长260 nm;建立10批委陵菜的指纹图谱,用中药色谱指纹图谱相似度评价系统软件(2004版)进行评价,聚类分析将10批药材分为2类;建立同时测定委陵菜药材中没食子酸、槲皮素及山柰酚3种成分的含量测定方法。结果建立了委陵菜的HPLC指纹图谱,共标定了12个共有峰;没食子酸、槲皮素和山柰酚线性关系良好,相关系数(r)均大于0.999。精密度、稳定性、重复性的RSD均小于3%,平均回收率分别为97.44%、97.64%、99.19%。结论建立的委陵菜的指纹图谱及多指标含量测定方法专属性强、重复性好,能有效地控制委陵菜的内在质量,为提高委陵菜的质量评价方法提供参考。     

四逆散干预焦虑症作用机制的网络药理学分析

目的探讨四逆散干预焦虑症的功效作用网络及药效作用机制。方法运用网络药理学方法,多个数据库联合分析四逆散和焦虑症的作用靶点,通过Cytoscape筛选靶点并对其基因功能和信号通路进行分析,运用Bio GPS数据库对所得靶点进行器官定位。结果分析结果表明槲皮素、山柰酚、芍药苷等成分作用于SRC、EGFR、PIK3R1等靶点,通过ERBB2信号通路、EGFRv III信号通路、VEGFA-VEGFR2信号通路等共同发挥作用,器官定位结果表明作用的核心病位为肝。结论四逆散干预焦虑症体现了中药多成分、多靶点、多通路的作用特点。     

Bauhinia forficata in the treatment of diabetes mellitus: a patent review

Introduction: Diabetes Mellitus has been considered an epidemic by the World Health Organization, with a high risk of morbidity and mortality. The treatment of this pathology consists in glycemic control, which can be done by oral hypoglycemic agents, insulin therapy, dietary guidance, regular physical activity, and psychosocial support. In addition, other adjuvant treatments are employed, such as phytotherapic, and one of the most used plants is Bauhinia forficata.

Areas covered: In the current review, patents using Bauhinia forficata for the Diabetes Mellitus treatment have been analyzed. There were 03 patents in WIPO, 01 in Espacenet, 01 in USPTO, and 02 in INPI.

Expert opinion: Patents on the adjuvant treatment of Diabetes Mellitus by Bauhinia forficata are discussed. Although there are some phytotherapy products containing this medicinal plant which has hypoglycemic effect here is still a need for the development of more products based on natural resources, for the treatment of this pathology, without side effects and with other benefits, to assist in the glycemia control in diabetic patients, and to improve their quality of life.     

高效液相色谱法测定复方矮地茶止咳合剂中的槲皮素和山奈酚含量

目的建立高效液相色谱法测定复方矮地茶止咳合剂中槲皮素和山奈酚的含量。方法采用SUPELCO Discovery C18（4．6mm×250nm,5μm）色谱柱,流动相：甲醇-0．4％磷酸溶液（50：50）,流速：1．0mL·min^-1,检测波长：370nm,柱温：40℃,进样量：10μL。结果槲皮素和山奈酚分别在6．484-155．6μg·mL^-1、5．708～137．0μg·mL^-1与峰面积线性关系良好,低、中、高3个剂量组的平均回收率分别为93．6％、97．2％、98．2％与95．2％、94．9％、100．2％。结论所建立的方法准确可靠、灵敏度高、专属性强,可有效控制复方矮地茶止咳合剂的质量。     

Therapeutic effects of kaempferol affecting autophagy and endoplasmic reticulum stress

Regulated cell death (RCD) guarantees to preserve organismal homeostasis. Apoptosis and autophagy are two major arms of RCD, while endoplasmic reticulum (ER) as a crucial organelle involved in proteostasis, promotes cells toward autophagy and apoptosis. Alteration in ER stress and autophagy machinery is responsible for a great number of diseases. Therefore, targeting those pathways appears to be beneficial in the treatment of relevant diseases. Meantime, among the traditional herb medicine, kaempferol as a flavonoid seems to be promising to modulate ER stress and autophagy and exhibits protective effects on malfunctioning cells. There are some reports indicating the capability of kaempferol in affecting autophagy and ER stress. In brief, kaempferol modulates autophagy in noncancerous cells to protect cells against malfunction, while it induces cell mortality derived from autophagy through the elevation of p‐AMP‐activated protein kinase, light chain‐3‐II, autophagy‐related geness, and Beclin‐1 in cancer cells. Noteworthy, kaempferol enhances cell survival through C/EBP homologous protein (CHOP) suppression and GRP78 increment in noncancerous cells, while it enhances cell mortality through the induction of unfolding protein response and CHOP increment in cancer cells. In this review, we discuss how kaempferol modulates autophagy and ER stress in noncancer and cancer cells to expand our knowledge of new pharmacological compounds for the treatment of associated diseases.