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由黄连((Goetgh.))、生姜(Roscoe.)和红花(L.)组成的新型草药配方对抑制HepG2细胞中PCSK9表达以上调LDLR表达的胆固醇调节作用。

The Cholesterol-Modulating Effect of the New Herbal Medicinal Recipe from Yellow Vine ( (Goetgh.)), Ginger ( Roscoe.), and Safflower ( L.) on Suppressing PCSK9 Expression to Upregulate LDLR Expression in HepG2 Cells.

作者信息

Ongtanasup Tassanee, Prommee Nuntika, Jampa Onkamon, Limcharoen Thanchanok, Wanmasae Smith, Nissapatorn Veeranoot, Paul Alok K, Pereira Maria de Lourdes, Wilairatana Polrat, Nasongkla Norased, Eawsakul Komgrit

机构信息

School of Medicine, Walailak University, Nakhon Si Thammarat 80160, Thailand.

Research Excellence Center for Innovation and Health Products (RECIHP), Walailak University, Nakhon Si Thammarat 80160, Thailand.

出版信息

Plants (Basel). 2022 Jul 13;11(14):1835. doi: 10.3390/plants11141835.

Abstract

PCSK9 is a promising target for developing novel cholesterol-lowering drugs. We developed a recipe that combined molecular docking, GC-MS/MS, and real-time PCR to identify potential PCSK9 inhibitors for herb ratio determination. Three herbs, , , and were used in this study. This work aimed to evaluate cholesterol-lowering through a PCSK9 inhibitory mechanism of these three herbs for defining a suitable ratio. Chemical constituents were identified using GC-MS/MS. The PCSK9 inhibitory potential of the compounds was determined using molecular docking, real-time PCR, and Oil red O staining. It has been shown that most of the active compounds of and inhibit PCSK9 when extracted with water, and has been shown to yield tetraacetyl-d-xylonic nitrile (27.92%) and inositol, 1-deoxy-(24.89%). These compounds could inhibit PCSK9 through the binding of 6 and 5 hydrogen bonds, respectively, while the active compound in is 2-Formyl-9-[.beta.-d-ribofuranosyl] hypoxanthine (4.37%) inhibits PCSK9 by forming 8 hydrogen bonds. These results suggest that a recipe comprising three parts , two parts , and one part is a suitable herbal ratio for reducing lipid levels in the bloodstream through a PCSK9 inhibitory mechanism.

摘要

前蛋白转化酶枯草溶菌素9(PCSK9)是开发新型降胆固醇药物的一个有前景的靶点。我们开发了一种结合分子对接、气相色谱-串联质谱(GC-MS/MS)和实时定量聚合酶链反应(real-time PCR)的方法,以鉴定用于确定草药比例的潜在PCSK9抑制剂。本研究使用了三种草药,[此处三种草药名称缺失]。这项工作旨在通过这三种草药的PCSK9抑制机制来评估降胆固醇作用,以确定合适的比例。使用GC-MS/MS鉴定化学成分。使用分子对接、实时定量聚合酶链反应和油红O染色来确定化合物的PCSK9抑制潜力。结果表明,[此处两种草药名称缺失]的大多数活性化合物用水提取时可抑制PCSK9,并且[此处草药名称缺失]已被证明可产生四乙酰基-D-木糖腈(27.92%)和1-脱氧肌醇(24.89%)。这些化合物可分别通过6个和5个氢键的结合来抑制PCSK9,而[此处草药名称缺失]中的活性化合物2-甲酰基-9-[β-D-呋喃核糖基]次黄嘌呤(4.37%)通过形成8个氢键来抑制PCSK9。这些结果表明,由三份[此处草药名称缺失]、两份[此处草药名称缺失]和一份[此处草药名称缺失]组成的配方是通过PCSK9抑制机制降低血液中脂质水平的合适草药比例。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/06c0/9318486/c0bba187bc54/plants-11-01835-g001.jpg

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