HPLC指纹图谱结合化学模式识别评价舒筋活血制剂的整体质量

目的建立舒筋活血制剂(舒筋活血胶囊、舒筋活血片)HPLC指纹图谱的方法,为其整体质量评价提供参考。方法色谱柱为Agilent Poroshell 120 SB-C18(150 mm×4.6 mm,2.7μm),以乙腈-0.2%甲酸水溶液为流动相,进行梯度洗脱;体积流量0.5mL/min,检测波长277nm,柱温30℃。采用"中药色谱指纹图谱相似度评价系统"(2012版)考察23批舒筋活血制剂的相似度,结合主成分分析(principal component analysis,PCA)、聚类分析(cluster analysis,CA)以及正交偏最小二乘判别分析(orthogonal partial least squares discriminant analysis,OPLS-DA)对舒筋活血制剂进行整体质量评价。结果舒筋活血制剂的HPLC指纹图谱中18批样品(S1～S17和S23)的相似度0.900,通过PCA、CA和OPLS-DA,23批样品聚成3类,S1～S16来自同一厂家为一类;S23和S17为一类;S18～S22为一类,并从10个共有峰中确定差异较大的4个共有峰,分别为1、3(5-羟甲基糠醛)、6(苯乙酸)和10(4-甲氧基水杨醛)号峰。结论所建立的指纹图谱结合化学模式识别方法稳定、简单,可用于评价舒筋活血制剂质量。     

消抗汤治疗免疫性反复自然流产抗心磷脂抗体阳性46例

目的:观察消抗汤治疗免疫性反复自然流产抗心磷脂抗体阳性的临床疗效。方法:将65例免疫性反复自然流产抗心磷脂抗体阳性的患者,根据随机法按2:1分为试验组(46例,采用消抗汤加减治疗)和对照组(19例,采用阿斯匹林治疗),治疗8周后观察2组患者症状调查问卷评分和抗心磷脂抗体检验变化情况。结果:试验组46例,抗体转阴29例,有效率63.04%;对照组19例,抗体转阴6例,有效率31.58%;试验组治疗后的症状调查问卷平均积分与治疗前相比有显著下降,对照组治疗后的症状调查问卷平均积分与治疗前相比无显著差异。试验组总疗效明显优于对照组(P<0.05)。结论:通过临床试验观察表明,中药消抗汤对免疫性反复自然流产患者抗心磷脂抗体的转阴以及症状的改善具有显著的疗效,明显优于阿斯匹林的治疗效果。     

增免抑瘤颗粒剂干预卵巢癌大剂量化疗后免疫及骨髓抑制的实验研究

目的探讨增免抑瘤颗粒剂对卵巢癌SKOV3荷瘤小鼠顺铂（DDP）化疗后免疫及骨髓抑制的改善情况。方法建立卵巢癌SKOV3荷瘤小鼠模型,测定小鼠单次腹腔注射DDP的LD50。取40只造模成功的荷瘤鼠,随机分为DDP组、ZMYL高、中、低剂量合并DDP组,每组10只,各组均予DDP LD50值单次腹腔注射。注射后次日开始灌胃给药,ZMYL高、中、低剂量组的给药剂量分别为24.0g/kg、12.0g/kg、6.0g/kg,DDP组灌以等量的0.9%NaC l溶液,共干预8天。观察荷瘤小鼠存活时间、存活率、脾脏指数及骨髓DNA含量、血常规等指标变化情况,应用荧光标记的单克隆抗体染色结合流式细胞仪测定外周血T淋巴细胞亚群比例。结果①DDP腹腔注射LD50为16.36 mg/kg,95%可信限为13.22mg/k-20.39 mg/kg。②各组生存时间以及存活率差异均无统计学意义（P〉0.05）。③与DDP组比较,各剂量ZMYL＋DDP组均可提高荷瘤小鼠脾脏指数,中高剂量组还可提高骨髓DNA含量,差异均有统计学意义（P〈0.05）。④与DDP组比较,各剂量ZMYL＋DDP组均可提高荷瘤小鼠外周血中白细胞数,差异均有统计学意义（P〈0.05）。⑤与DDP组比较,各剂量ZMYL＋DDP组的CD3、CD4、CD8及CD4/CD8差异无统计学意义（P〉0.05）。结论 ZMYL对顺铂大剂量化疗引起的荷瘤小鼠外周血白细胞减少及骨髓DNA含量、脾脏指数的降低有明显的升高作用,能调节机体紊乱的免疫功能,改善骨髓抑制。     

Louki Zupa decoction attenuates the airway inflammation in acute asthma mice induced by ovalbumin through IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway

ContextAsthma is a common respiratory system disease. Louki Zupa decoction (LKZP), a traditional Chinese medicine, presents a promising efficacy against lung diseases.ObjectiveTo investigate the pathogenic mechanism of asthma and reveal the intervention mechanism of LKZP.Materials and methodsForty-eight female Balb/c mice were randomly divided into 6 groups: normal control group (NC), ovalbumin (OVA)/saline asthma model group, OVA/LL group, OVA/LM group, OVA/LH group and OVA/DEX group (n = 8 per group). The asthmatic mice were modelled through intraperitoneal injecting and neutralizing OVA. LKZP decoction was administrated by gavage at the challenge stage for seven consecutive days (2.1, 4.2 and 8.4 g/kg/day). We investigated the change in lung function, airway inflammation, mucus secretion and TH-1/TH-2-related cytokines. We further verify the activated status of the IL-33/ST2/NF-κB/GSK3β/mTOR signalling pathway.ResultsLKZP was proved to improve asthmatic symptoms, as evidenced by the down-regulated airway resistance by 36%, 58% and 53% (p < 0.01, p < 0.001 vs. OVA/saline group), up-regulated lung compliance by 102%, 114% and 111%, decreased airway inflammation and mucus secretion by 33%, 40% and 33% (p < 0.001 vs. OVA/saline group). Moreover, the content of cytokines in BALF related to airway allergy (such as IgE) and T helper 1/T helper 2 cells (like IL-2, IL-4, IL-5, IL-13, TNF-α and IFN-γ), were also markedly reduced by 13–65% on LKZP intervention groups compared with model group. Mechanistic research revealed that the IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway was activated in the OVA/saline group and LKZP significantly down-regulated this pathway.Discussion and conclusionLKZP improves lung function, airway inflammation, mucus secretion and correct immune imbalance by intervening with the IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway, presenting a promising therapeutic choice for asthma.     

Perspectives on developing small molecule inhibitors targeting HIV-1 integrase

HIV-1 integrase (IN) is a crucial enzyme in the life cycle of HIV-1 and also a validated target for developing anti-HIV inhibitors. Recent progress in drug design has significantly accelerated the development of anti-AIDS IN inhibitors. A large amount of novel inhibitors that interact specifically with IN were developed along with the expanding and application of methods to drug design. This article reviewed the anti-HIV IN inhibitors discovered by the rational drug design approaches in the recent 5-year.     

Design,Synthesis, Biological Evaluation,and Molecular Docking of Novel Benzopyran and Phenylpyrazole Derivatives as Akt Inhibitors

By inspiration of good Akt1 inhibitory and cytotoxic activity of our previously screened hits 1 and 2 , a series of novel benzopyrans 3a – c , 4 and phenylpyrazoles 5a – c , 6a – b , and 7 were designed, synthesized, and biologically evaluated for their in vitro Akt1 inhibitory and cytotoxic activity. The results revealed that all of these compounds showed moderate‐to‐excellent antiproliferative effects against the tested cancer cell lines (i.e. HL‐60, OVCAR, PC‐3, and HepG2). Among them, compounds 3a and 3c exhibited preferable Akt1 inhibitory activities (IC₅₀ of 3a and 3c are 6.18 and 5.28 μm , respectively), while compounds 4 , 5a – c , 6a – b , and 7 only showed weak Akt1 inhibitory activities. Consequently, we used molecular docking and dynamic simulation to propose a mode of binding between Akt1 and the 3c compound.     

18β-glycyrrhetinic acid inhibits migration and invasion of human gastric cancer cells via the ROS/PKC-α/ERK pathway

Journal of Natural Medicines - 18β-glycyrrhetinic acid (18β-GA) is a bioactive component of licorice root which exerts pharmacological activities including anti-inflammatory, antiviral,...     

一个新的醌类化合物的结构鉴定

醌类化合物是一类优良的光敏剂 ,有特殊的化学和生物学特性。含　醌类化合物的一些真菌的代谢产物和植物在民间用于治疗胃痛、风湿性关节炎、跌打损伤等症 ,近来发现　醌类化合物不仅可治疗某些皮肤病 ,而且有光敏杀伤肿瘤细胞和抑制爱滋病病毒的作用[1,2 ] 。作者从云南省西北部山区采集到一株丝状真菌 ,由云南大学生物系杨发蓉教授鉴定为子囊菌纲、肉座菌科、菌寄生菌属真菌(ＡｓｃｏｍｙｃｅｔｅｓＨｙｐｏｃｒｅａｃｅａｅＨｙｐｏｍｙｃｅｓ (Ｆｒ .)Ｔｕｌ.ｓｐ .) ,经驯化 ,实验室内培养成功。本文从该菌固态发酵的菌丝体中分得一新…     

Decoupling location specificity from perceptual learning of orientation discrimination

Perceptual learning of orientation discrimination is reported to be precisely specific to the trained retinal location. This specificity is often taken as evidence for localizing the site of orientation learning to retinotopic cortical areas V1/V2. However, the extant physiological evidence for training improved orientation turning in V1/V2 neurons is controversial and weak. Here we demonstrate substantial transfer of orientation learning across retinal locations, either from the fovea to the periphery or amongst peripheral locations. Most importantly, we found that a brief pretest at a peripheral location before foveal training enabled complete transfer of learning, so that additional practice at that peripheral location resulted in no further improvement. These results indicate that location specificity in orientation learning depends on the particular training procedures, and is not necessarily a genuine property of orientation learning. We suggest that non-retinotopic high brain areas may be responsible for orientation learning, consistent with the extant neurophysiological data.