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采用 NMR、LC-MS 对提取物进行分析，鉴定作为 LDLR 和 PCSK9 调节剂的天然产物。

NMR, LC-MS Characterization of Extracts, Identification of Natural Products Acting as Modulators of LDLR and PCSK9.

机构信息

Department of Pharmaceutical and Pharmacological Sciences, University of Padova, 35122 Padova, Italy.

Department of Agriculture, Minab Higher Education Center, University of Hormozgan, Bandar Abbas 79177, Iran.

出版信息

Molecules. 2022 Mar 30;27(7):2256. doi: 10.3390/molecules27072256.

DOI:10.3390/molecules27072256
PMID:35408655
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9000307/
Abstract

(Briq.) Scheen and V.A.Albert (Lamiaceae) is used in Iranian traditional medicine to treat malaria, diabetes, hyperlipidemia, rheumatism and cardiovascular diseases. NMR and LC-DAD-MS analyses were used to establish extract composition and phenylethanoid, flavonoid glycosides, lignans, labdane diterpenes and iridoids were identified and quantified. The main constituents were isolated, and structures were elucidated based on NMR, polarimetric and MS measurements. A new natural compound, ent-labda-8(17),13-dien-18-glucopyranosyl ester-15,16-olide is described here. The effects of ent-labda-8(17),13-dien-18-oic acid-15,16-olide (), ent-labda-8(17),13-dien-18-glucopyranosyl es-ter-15,16-olide (), antirrhinoside (), echinacoside (), verbascoside (), and apigenin 6,8-di-C-glucoside (), on the low-density lipoprotein receptor (LDLR) and proprotein convertase subtilisin/kexin type 9 (PCSK9), were studied in the human hepatocarcinoma cell line Huh7. Among the six constituents, () showed the strongest induction of the LDLR (3.7 ± 2.2 fold vs. control) and PCSK9 (3.2 ± 1.5 fold vs. control) at a concentration of 50 µM. The in vitro observations indicated a potential lipid lowering activity of () with a statin-like mechanism of action.

摘要

(Briq.) Scheen 和 V.A.Albert（唇形科）在伊朗传统医学中用于治疗疟疾、糖尿病、高脂血症、风湿病和心血管疾病。使用 NMR 和 LC-DAD-MS 分析来建立提取物成分，并鉴定和定量苯乙醇苷、黄酮苷、木脂素、裂环烯醚萜和环烯醚萜。主要成分被分离出来，并根据 NMR、旋光和 MS 测量确定了结构。描述了一种新的天然化合物，ent-labda-8(17),13-dien-18-葡萄糖苷-15,16-内酯。研究了 ent-labda-8(17),13-dien-18-酸-15,16-内酯 ()、ent-labda-8(17),13-dien-18-葡萄糖苷-15,16-内酯 ()、antirrhinoside ()、echinacoside ()、verbascoside () 和 apigenin 6,8-di-C-葡萄糖苷 () 对人肝癌细胞系 Huh7 中低密度脂蛋白受体 (LDLR) 和前蛋白转化酶枯草溶菌素/激肽释放酶 9 (PCSK9) 的影响。在这六种成分中，()在 50µM 浓度下对 LDLR（3.7±2.2 倍对照）和 PCSK9（3.2±1.5 倍对照）的诱导作用最强。体外观察表明 ()具有他汀类药物作用机制的潜在降脂活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/cf17df872482/molecules-27-02256-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/49ee3daf6bcc/molecules-27-02256-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/0d34813b3828/molecules-27-02256-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/25f55037e730/molecules-27-02256-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/8c32b0d40b08/molecules-27-02256-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/1bca8012f466/molecules-27-02256-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/30ca197648a0/molecules-27-02256-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/cf17df872482/molecules-27-02256-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/49ee3daf6bcc/molecules-27-02256-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/0d34813b3828/molecules-27-02256-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/25f55037e730/molecules-27-02256-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/8c32b0d40b08/molecules-27-02256-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/1bca8012f466/molecules-27-02256-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/30ca197648a0/molecules-27-02256-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b04/9000307/cf17df872482/molecules-27-02256-g007.jpg

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