An overview of Pu-erh tea and its health-promoting effects of lipid-lowering and anti-obesity

Eric Wei Chiang Chan, Siu Kuin Wong, Hung Tuck Chan

2021, 30(8): 623-633. DOI: 10.5246/jcps.2021.08.050

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As a dark tea, Pu-erh tea (PET) is produced from sun-dried leaves of Camellia sinensis var. assamica mainly in Yunnan Province of China. Many microorganisms are involved in the fermentation of PET. Among them, Aspergillus niger is most important. It is believed that the longer the preservation period, the better is the quality and taste of PET, which is commercially available as loose, compressed or instant tea leaves. Chemical components of PET include flavones, flavanols, flavonols, phenolic acids, alkaloids and methylxanthines. In this overview, the lipid-lowering and anti-obesity effects of PET were discussed based on animal models and human trials, and our study provided some insights into possible mechanisms of bioactive compounds, such as theabrownin, catechins, lovastatin and gallic acid. Other bioactivities of PET and some information on Fuzhuan brick tea were also included. Sources of information cited were from Google Scholar, PubMed, PubMed Central, Science Direct, J-Stage, PubChem, Directory of Open Access Journals (DOAJ), and China National Knowledge Infrastructure (CNKI).

Synthesis, cytotoxicity assay, and molecular docking study of hydroxychalcone derivatives as potential tyrosinase inhibitors

Aris Stiawan, Eti Nurwening Sholikhah, Yehezkiel Steven Kurniawan, Yoga Priastomo, Jumina

2021, 30(8): 634-644. DOI: 10.5246/jcps.2021.08.051

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In this work, we studied the synthesis, cytotoxicity assay, and molecular docking of hydroxychalcone derivatives as tyrosinase inhibitors. Synthesis of chalcone derivatives was carried out through a Claisen-Schmidt condensation reaction between acetophenone and benzaldehyde derivatives under alkaline conditions for 48 h. The synthesized products were characterized by using Fourier transform infrared (FTIR), gas chromatography-mass spectrometry (GC-MS), proton and carbon nuclear magnetic resonance (¹H and ¹³C NMR) spectrometer. The in vitro inhibitory activity was evaluated against tyrosinase enzyme by employing L-3,4-dihydroxyphenylalanine (L-DOPA) as the substrate. We successfully synthesized 4-hydroxychalcone (HC) and 4-hydroxy-3-methoxychalcone (HMC) with a yield of 60% and 76%, respectively. While the tyrosinase inhibitory test of HC and HMC gave the IC₅₀ value of 64.35 and 21.56 μg/mL, respectively, demonstrating that their inhibitory activities against tyrosinase enzyme were better compared with kojic acid and hydroquinone as the positive controls. We also found that HC gave 2025 μg/mL as the IC₅₀ value against Vero cells, confirming that it was not toxic to the normal cell line. The molecular docking study gave the root-mean-square deviation value of less than 2 ?. Furthermore, the binding energies of hydroxychalcone derivatives were found as –30.13 and –31.38 kJ/mol, showing that those compounds could be potentially used as the alternative tyrosinase inhibitors in medical application.

白术内酯II在人肝微粒体中与CYP450酶之间的相互作用研究

陈绪龙, 廖正根, 李成, 黄国勇, 宋云燕, 董伟, Abid Naeem, 梁新丽

2021, 30(8): 645-656. DOI: 10.5246/jcps.2021.08.052

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本研究旨在探讨白术内酯II在人肝微粒体中与CYP450酶之间的相互作用情况, 为预测白术内酯II在药物联用时可能产生的相互作用奠定理论基础。采用特异性抑制剂进行化学抑制实验, 阐明影响白术内酯II代谢的CYP450亚型; 以IC₅₀和K_i等相关数据为评价指标, 采用人肝微粒体系统的基于探针的测定方法, 研究白术内酯II对CYP450酶系抑制机理、动力学和抑制类型。结果显示白术内酯II代谢受CYP1A2、CYP2C9和CYP3A4抑制剂的影响, 最高抑制率分别为41.35%、41.97%和82.45%; 白术内酯II对P450五种亚型CYP2C9、CYP1A2、CYP2C19、CYP3A4和CYP2D6的IC₅₀值分别为69.7、84.3、92.4、173.8和190.1 μmol/L, K_i值分别为190.6、179.1、> 200、72.2和66.8; 白术内酯II对CYP1A2为非竞争性抑制, 对CYP2C9和3A4为竞争性抑制, 对CYP2C19和2D6为混合型抑制。研究结果表明, CYP1A2、CYP2C9和CYP3A4是参与白术内酯II代谢的CYP亚型, 白术内酯II对5种CYP450亚型具有不同的抑制机制和抑制强度。

钩藤碱小鼠急性毒性试验及评价

胡岚岚, 张惠静, 张乐, 汤建林

2021, 30(8): 657-665. DOI: 10.5246/jcps.2021.08.053

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钩藤碱作为钩藤的主要生物碱成分, 具有抗高血压和神经保护作用, 近年来受到广泛关注。尽管如此, 其毒性的研究仍较少。本研究通过口服给药钩藤碱, 观察其对昆明小鼠的急性毒性反应。昆明小鼠随机分组后分别灌服给药520.00、442.00、375.70、319.34、271.44 mg/kg剂量的钩藤碱, 观察14天, 记录小鼠的一般行为、体重变化、毒性反应和死亡情况, 计算半数致死量(LD₅₀), 并对死亡小鼠进行主要脏器的病理学检查。与对照组相比, 单次给药钩藤碱后小鼠体重未见明显变化, 但是钩藤碱给药后小鼠出现明显的异常症状和死亡率。毒性试验的LD₅₀为308.08 mg/kg, 病理学结果显示钩藤碱高剂量组对小鼠的脑、肝、肺、肾有较明显的毒性作用。本研究表明, 钩藤碱不可长时间或高剂量使用, 本研究可为下一步的临床研究提供有力的依据。

辣椒素对多柔比星耐药的乳腺癌细胞的耐药逆转作用

周毅, 王婷, 赵佳佳, 蒋学华

2021, 30(8): 666-674. DOI: 10.5246/jcps.2021.08.054

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肿瘤细胞高表达P糖蛋白(P-gp)会抑制化疗的疗效, 导致肿瘤耐药, 而P-gp抑制剂可逆转P-gp介导的肿瘤耐药。辣椒素是辣椒的主要活性成分, 也是P-gp抑制剂。本研究旨在初步探讨辣椒素对多柔比星(DOX)耐药的乳腺癌MCF-7/DOX细胞的耐药逆转作用。细胞毒性研究结果表明, 长期处理72 h后, 辣椒素(50 μM)可以逆转MCF-7/DOX细胞对多柔比星的耐药(逆转倍数为4.68倍), 并浓度依赖性地下调MDR1基因mRNA的表达。在短期培养3 h后, 辣椒素可逆地、浓度依赖性地增加了DOX在MCF-7/DOX细胞中的蓄积, 对DOX在细胞内亚细胞分布的影响不同于阳性对照药维拉帕米。辣椒素也能浓度依赖性地抑制线粒体生成ATP。综上所述, 辣椒素能够逆转MCF-7/DOX细胞对DOX的耐药, 可成为一种很有前途的逆转多药耐药的先导化合物。

Diaporisoindole B通过抑制MyD88/NF-κB/MAPKs通路对LPS诱导的RAW 264.7巨噬细胞发挥抗炎作用

刘红菊, 李静, 谢慧仪, 王玲玲, 张志珍, 闫冲

2021, 30(8): 675-685. DOI: 10.5246/jcps.2021.08.055

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Diaporisoindole B(DPB)是从红树内生真菌Diaporthe sp. SYSU-HQ3的次级代谢产物中分离得到的一种异吲哚类衍生物。前期研究表明DPB可抑制LPS诱导的RAW 264.7巨噬细胞产生NO, 说明其具有潜在的抗炎活性。本文进一步研究了DPB对LPS诱导的RAW 264.7巨噬细胞的抗炎活性及可能的作用机制。DPB(3.125、6.25、12.5和25 μM)可显著性抑制LPS引起的RAW 264.7小鼠巨噬细胞中PGE2的水平, 及iNOS和COX-2的表达, 并呈剂量依赖性。DPB也可显著抑制LPS引起的RAW 264.7小鼠巨噬细胞中细胞因子TNF-α, IL-1β和IL-6的表达。此外, 我们还研究了DPB发挥抗炎作用的机制。DPB可通过下调上游MyD88 蛋白水平抑制NF-κB信号通路的激活。此外, DPB还能够抑制MAPKs三个亚型(包括ERK 1/2、JNK和p38)的磷酸化。因此, DPB可能通过下调RAW 264.7巨噬细胞中MyD88蛋白的水平抑制NF-κB和MAPKs的表达, 从而达到抗炎的作用。

新生儿无乳链球菌脑膜炎的抗感染治疗方案分析及停药指征探讨

武海艳, 王涛, 王倩, 唐琳

2021, 30(8): 686-691. DOI: 10.5246/jcps.2021.08.056

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新生儿GBS脑膜炎的临床表现为: 非特异性、住院时间长、易引起神经系统并发症和后遗症。临床药师参与一例停药时脑脊液仍异常的新生儿无乳链球菌脑膜炎的抗感染治疗。根据抗菌药物PK/PD特性、血脑屏障通透性、抗生素的剂量调整, 分析脑脊液细胞数在使用万古霉素治疗后先降低后上升的原因, 分析利奈唑胺治疗新生儿细菌性脑膜炎的疗效, 探讨脑脊液异常时停药的适应症, 以提高新生儿细菌性脑膜炎用药的安全性和有效性。

利格列汀对初诊2型糖尿病患者炎症因子和动脉硬化的影响

李睿, 孔燕茹

2021, 30(8): 692-698. DOI: 10.5246/jcps.2021.08.057

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研究旨在探讨利格列汀对初诊2型糖尿病(T2DM)合并颈动脉硬化性疾病(CAD)患者的血液炎症因子水平和颈动脉内膜中层厚度(CIMT)的影响。我们将326例初诊T2DM合并CAD患者随机分为2组, 对照组163例二甲双胍单药治疗, 实验组163例在二甲双胍基础上联合利格列汀治疗。彩色超声多普勒测量治疗前后CIMT, ELISA法检测治疗前后IL-6和IL-1β数值, 比较两组治疗前后炎症因子水平和CIMT厚度, 并分析IL-6和IL-1β与CIMT的相关性。治疗24周后, 结果显示实验组的炎症因子水平和CIMT均显著低于对照组(P < 0.01), IL-6和IL-1β的水平与CIMT呈正相关。通过本研究得出利格列汀对初诊T2DM合并CAD患者的血液炎症因子水平和CIMT均有改善作用, IL-6、IL-1β可能通过影响CIMT参与CAD的发生和发展。

夏青课题组利用基因密码子扩展技术治疗无义突变罕见病

北京大学药学院天然药物及仿生药物国家重点实验室

2021, 30(8): 699-700.

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