Abstract

Nepeta bracteata Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the aim of this study was to screen for compounds with anti-inflammatory activities in N. bracteata Benth. Using silica gel, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, 10 compounds were separated from N. bracteata Benth. extract, including four new diterpenoids (1–4), one amide alkaloid (5), and five known diterpenoids (6–10). The structures of all the isolates were elucidated by HR-ESI-MS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, we investigated the anti-inflammatory activities of compounds 1–10. It is worth noting that all were able to inhibit nitric oxide (NO) production with IC50 values < 50 μM and little effect on RAW 264.7 macrophage viability. Compounds 2 and 4 displayed remarkable inhibition with IC50 values of 19.2 and 18.8 μM, respectively. Meanwhile, screening on HCT-8 cells demonstrated that compounds 2 and 4 also had moderate cytotoxic activities with IC50 values of 36.3 and 41.4 μM, respectively, which is related to their anti-inflammatory effects.

Highlights

  • Inflammation, a common clinical pathological process, is closely related to many diseases such as arthritis, psychosis, cardiovascular and cerebrovascular diseases, and cancer [1,2,3,4]

  • While modern pharmacology has shown that its extract has significant anti-inflammatory activity, no related research has been conducted to characterize its chemical components [10,11,12]

  • With the aim of screening for anti-inflammatory active compounds in N. bracteata Benth., a 95% ethanol extract shown that its extract has significant anti-inflammatory activity, no related research has been conducted to characterize its chemical components [10,11,12]

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Summary

Introduction

Inflammation, a common clinical pathological process, is closely related to many diseases such as arthritis, psychosis, cardiovascular and cerebrovascular diseases, and cancer [1,2,3,4]. Belongs to the genus Nepeta of the Lamiaceae family and is mainly distributed in Pakistan, Nepal, Iran, and other countries It is a folk medicine used by Xinjiang Uyghurs and a medicinal material imported for use in the Xinjiang Uygur hospital, with the Uyghur name “Zufa” [7]. While modern pharmacology has shown that its extract has significant anti-inflammatory activity, no related research has been conducted to characterize its chemical components [10,11,12]. With the aim of screening for anti-inflammatory active compounds in N. bracteata Benth., a 95% ethanol extract shown that its extract has significant anti-inflammatory activity, no related research has been conducted to characterize its chemical components [10,11,12]. With the aim of screening for anti-inflammatory active compounds in N. bracteata Benth., a 95% ethanol extract was investigated, and 10 compounds—four new diterpenoids, nepetabrates A–D (1–4), was investigated, and

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