基于经典剂型科学表征的中药制剂创新策略

挖掘和表征中药经典制剂的剂型特征是中药现代制剂创新的基础。本文通过对近10年国家自然科学基金委员会（NSFC）在中药制剂学科立项情况、国内外中药制剂研究文献以及中药新药注册申报情况等大数据的梳理统计,发现中药经典制剂的研究项目大幅度缩减,中药经典剂型的市场份额逐年萎缩。“中药西制”模式下的现代制剂占有市场主导地位,但因其疗效“降格”致竞争力较弱。因此,借助国家政策推动下的经典剂型研究浪潮,加快加深中药经典制剂的研究,既有助于促进中药药剂学的学科发展、提升经典医药文化素养,也能促进经典医药非遗的保护和传承。     

Flavonoids in myocardial ischemia–reperfusion injury: Therapeutic effects and mechanisms

Ischemic heart diseases are one of the major causes of death worldwide. Effective restoration of blood flow can significantly improve patients’ quality of life and reduce mortality. However, reperfusion injury cannot be ignored. Flavonoids possess well-established antioxidant properties;They also have other benefits that may be relevant for ameliorating myocardial ischemia-reperfusion injury(MIRI). In this review,we focus on flavonoids with cardiovascular-protection function and emphasize their pharmacological effects. The main mechanisms of flavonoid pharmacological activities against MIRI involve the following aspects: a) antioxidant, b) anti-inflammatory, c) anti-platelet aggregation, d) anti-apoptosis, and e)myocardial-function regulation activities. We also summarized the effectiveness of flavonoids for MIRI.     

Combined antihypertensive effect of luteolin and buddleoside enriched extracts in spontaneously hypertensive rats

Ethnopharmacological relevance

Flos Chrysanthemi is used in a variety of diseases in traditional Chinese medicine including hypertension, and the total flavonoids (rich in luteolin (LUT) and buddleoside (BUD)) of Flos Chrysanthemi is known to modulate vascular functions and reduce the blood pressure. However, the active flavonoids and their synergistic effects on anti-hypertension are still unclear. To investigate the combined anti-hypertension effects of LUT and BUD enriched extracts on spontaneously hypertensive rats (SHR), as well as the anti-hypertensive mechanism of LUT&BUD mixture.

Materials and methods

CODA Mouse & Rat Tail-Cuff Blood Pressure System was used to measure the systolic blood pressure (SBP) and diastolic blood pressure (DBP) of SHR after treated with extracts contains with LUT and/or BUD. The expressions of Ang II, PRA, ALD, ET, PGI₂ and TXB₂ were investigated by ELASA. Serum NO concentration was measured by the method of Nitric acid reductase.

Results

A single administration of LUT, BUD, or LUT:BUD=1:1 significantly reduced SBP by about 3.35 mmHg, 4.39 mmHg and 15.42 mmHg, respectively. Chronic administration of LBM (at 60 mg/kg; p.o. for 30 days) reduced both SBP and DBP by 4.04% and 5.24% of the vehicle group, respectively. Oral administration of LBM at 60 mg/kg inhibited the serum levels of ANG, ALD and ET, but increased serum NO concentration.

Conclusion

This study shows the synergistic anti-hypertension effects of LUT and BUD in SHR. The effects of LBM on blood pressure are associated with RAAS and endothelial system. Thus, our experiments suggest that the combination of luteolin and buddleoside from Flos Chrysanthemi are potentially useful for the therapeutic treatments for hypertension.     

束缚所致肝郁证动物模型肝组织蛋白质组的差异表达研究

目的：通过运用组织蛋白质组学技术和方法,寻找肝郁证动物模型肝组织差异表达蛋白质.方法：以束缚制动法制备肝郁证大鼠模型,采用组织溶解方法分步抽提大鼠肝脏组织蛋白质,对获得的蛋白质进行二维凝胶电泳（2-DE）分离、胶体染色,分析模型组和对照组蛋白质分子的差异表达,并以基质辅助激光解吸电离飞行时间质谱（MALDI-TOF-MS）检测肽质量指纹,在数据库中检索出相应的蛋白质.结果：在大鼠肝组织胶体考染的2-DE图谱上,约能辨识出300余个清晰的蛋白质斑点,共找出3个与肝郁证辨证相关的肝组织差异表达蛋白,质谱出峰率达100%,检索结果分别为芳基硫基转移酶、烯酰辅酶A水合酶和转甲状腺素蛋白.结论：肝主疏泄功能的正常可能和实体肝组织中的特异表达蛋白质--芳基硫基转移酶、烯酰辅酶A水合酶和转甲状腺素蛋白的不同表达密切相关.     

高效液相色谱法测定红宝散中欧前胡素的含量

目的采用高效液相色谱法测定红宝散中欧前胡素的含量。方法采用HPLC法,Apollo-C18（250mm×4．6mm,5μm）色谱柱,流动相为甲醇一水（55：45）,流速为1．0mL·min-1,紫外检测波长为300nm,柱温为室温。结果欧前胡素进样量在0．0300-0．2000ug线性关系良好,r=0．9999,平均回收率99．68％,RSD=0．35％。结论本方法准确、简便、快速,可作为红宝散中欧前胡素的含量测定。     

人参皂苷Rg1对大脑皮质神经细胞生物膜的影响

目的:研究人参皂苷Rg1对原代培养正常大鼠大脑皮质神经细胞生物膜的影响。方法:采用细胞培养技术,运用比色法、硫代巴比妥酸法、黄嘌呤氧化酶法(羟胺法)和微量酶标法测定人参皂苷Rg1对细胞内ACP活力、MDA含量、SOD活力及LDH释放量的影响。结果:1mg/ml、2 mg/ml及4 mg/ml人参皂苷Rg1作用30min可不同程度增加正常培养神经细胞的LDH释放量和细胞内SOD活力,降低细胞内ACP活力及MDA含量。结论:1mg/ml、2 mg/ml及4 mg/ml人参皂苷Rg1作用30min对正常培养大脑皮质神经细胞生物膜具有显著影响,其中对溶酶体膜有保护作用,对生物膜的脂质过氧化反应有抑制作用,能减轻自由基对生物膜的攻击及损伤,但对细胞膜可能有一定的损伤作用。     

胆囊结石术后胃肠功能紊乱的针刺研究

目的:观察不同针刺刺激量对胆囊结石术后胃肠功能紊乱患者胃肠功能的恢复以及血管活性肠肽(VIP)的影响。方法:将32例患者分为四组,分为提插强刺激组、提插弱刺激组、捻转强刺激组、捻转弱刺激组,观察给予不同针刺刺激后四组患者的胃肠功能和血管活性肠肽(VIP)的变化。结果:统计学处理后,对于肠鸣音恢复时间,提插强刺激组和捻转弱刺激组之间的比较有统计学意义;对于术后排气时间,提插强刺激与捻转强刺激、捻转弱刺激之间,提插弱刺激与捻转弱刺激之间均有统计学意义(P<0.05),其余无统计学意义;术后排便时间统计结果无差异(P>0.05)。对于VIP,四组病人术前血管活性肠肽无差异(P>0.05),具有可比性;术后第2天四组病人血浆血管活性肠肽含量治疗后均有回升趋势,提插弱刺激组和捻转弱刺激组病人血浆VIP含量在治疗后与提插强刺激组和捻转强刺激组比较均有明显差异(P<0.05)。结论:强刺激对血管活性肠肽的变化的影响较弱刺激好,同样的刺激量下提插较捻转的对血管活性肠肽的变化影响大,提插强刺激对于胃肠功能恢复的作用由于其他三种。     

Exploring the mechanism of Buyang Huanwu decoction in the treatment of lumbar disc herniation based on network pharmacology and molecular docking

Buyang Huanwu decoction (BYHWD), as one of the traditional Chinese medicine formulas, is widely used in the clinical treatment of lumbar disc herniation (LDH) with curative effect. It has the characteristics of multi-component, multi-target, and mutual synergy, but the mechanism of action is often unclear. It needs some research to explore the molecular mechanism of BYHWD in the treatment of LDH based on network pharmacology and molecular docking. Screen the active compounds of BYHWD and predict drug-related gene/protein targets, which could determine the specific target of BYHWD in the treatment of LDH. Construct the “Drugs-Compounds-Targets” network and search for the core targets. Use Gene Ontology functional enrichment analysis, Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis, and molecular docking verification to explore the possible molecular mechanism. Eighty-two effective compounds and 666 targets of BYHWD, 187 targets for LDH treatment, and 20 core candidate targets were excavated. A total of 3414 entries were identified by Gene Ontology enrichment analysis, 173 related signal pathways were identified by Kyoto Encyclopedia of Genes and Genomes enrichment analysis, and 5 core compounds were identified by molecular docking, which had a good affinity with core genes STAT3, JUN, AKT1, MAPK1, RELA, and PIK3CA. BYHWD may play the role of analgesic and improving function by synergistic anti-inflammatory and analgesic compounds, regulating cell metabolic differentiation, regulating immunity, and anticoagulation. BYHWD in the treatment of LDH may play a role in analgesia and improve function through multiple signaling pathways, including PI3K-Akt, mitogen-activated protein kinase, tumor necrosis factor, and interleukin-17. The PI3K-Akt signaling may be one of the key mechanisms.     

Assessment of endometrial receptivity during implantation window in women with unexplained infertility

Abstract

This study aimed to assess the endometrial receptivity during implantation window in women with unexplained infertility. A prospective study recruited 168 women with unexplained infertility and 169 fertile women. Ultrasonic parameters and biomarkers in the uterine fluid were detected. The endometrial vascularization index (VI), flow index (FI) and vascularization flow index (VFI) were significantly higher in fertile women as compared with unexplained infertile women, and the integrin αvβ3, vascular endothelial growth factor (VEGF), tumor necrosis factor alpha (TNF-α), and leukemia inhibitory factor (LIF) levels in uterine fluid were significantly higher in fertile women. The biochemical pregnancy rate, clinical pregnancy rate, and ongoing pregnancy rate in fertile women were 20.12%, 18.34%, and 17.75%, respectively, which were significantly higher compared with unexplained infertile women (7.14%, 5.36%, and 4.17%, respectively). Endometrial thickness (ET), endometrial volume (EV), VI, FI, and VFI measured by ultrasound, and the integrin αvβ3, VEGF, TNF-α, and LIF levels in uterine fluid were all significantly higher in pregnant women as compared with nonpregnant women. The best parameters of ultrasonic indicators for predicting endometrial receptivity in women with unexplained infertility were FI(AUC = 0.894, sensitivity 93.8%, and specificity 83.1%). Integrin αvβ3 had the best predictive value for endometrial receptivity among biomarkers in the uterine fluid (AUC = 0.921, sensitivity 96.7%, and specificity 89.5%). Women with unexplained infertility present declined endometrial receptivity. Endometrial ultrasonic parameters detected by three-dimensional power Doppler and biomarkers in the uterine fluid may be effective indicators to predict endometrial receptivity.     

复方芪芍合剂的质量控制

目的建立复方芪芍合剂的质量控制方法。方法应用薄层色谱法对复方芪芍合剂中黄芪、赤芍进行定性鉴别,并用紫外分光光度法对复方芪芍合剂中总皂苷进行含量测定。结果测得复方芪芍合剂中总皂苷量平均为0.436 3 g.L-1,RSD为8.59%,加样回收率为88.32%。结论本方法专属性强,操作简便,结果准确,可用于复方芪芍合剂的质量控制。