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An in vitro study of anti-inflammatory activity of standardised Andrographis paniculata extracts and pure andrographolide

机译:标准化穿心莲提取物和纯穿心莲内酯抗炎活性的体外研究

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Background The anti-inflammatory activity of Andrographis paniculata (Acanthaceae), a traditional medicine widely used in Asia, is commonly attributed to andrographolide, its main secondary metabolite. Commercial A. paniculata extracts are standardised to andrographolide content. We undertook the present study to investigate 1) how selective enrichment of andrographolide in commercial A. paniculata extracts affects the variability of non-standardised phytochemical components and 2) if variability in the non-standardised components of the extract affects the pharmacological activity of andrographolide itself. Methods We characterized 12 commercial, standardised (≥30% andrographolide) batches of A. paniculata extracts from India by HPLC profiling. We determined the antioxidant capacity of the extracts using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, oxygen radical antioxidant capacity (ORAC) and a Folin-Ciocalteu (FC) antioxidant assays. Their anti-inflammatory activity was assessed by assaying their inhibitory effect on the release of tumor necrosis factor alpha (TNF-α) in the human monocytic cell line THP-1. Results The andrographolide content in the samples was close to the claimed value (32.2?±?2.1%, range 27.5 to 35.9%). Twenty-one non-standardised constituents exhibited more than 2-fold variation in HPLC peak intensities in the tested batches. The chlorogenic acid content of the batches varied more than 30-fold. The DPPH free radical scavenging activity varied ~3-fold, the ORAC and FC antioxidant capacity varied ~1.5 fold among batches. In contrast, the TNF-α inhibitory activity of the extracts exhibited little variation and comparison with pure andrographolide indicated that it was mostly due to their andrographolide content. Conclusions Standardised A. paniculata extracts contained the claimed amount of andrographolide but exhibited considerable phytochemical background variation. DPPH radical scavenging activity of the extracts was mostly due to the flavonoid/phenlycarboxylic acid compounds in the extracts. The inhibitory effect of andrographolide on the release of TNF-α was little affected by the quantitative variation of the non-standardised constituents.
机译:背景技术穿心莲(Acanthaceae)(一种在亚洲广泛使用的传统药物)的抗炎活性通常归因于穿心莲内酯(其主要的次要代谢产物)。商业化的沙棘提取物标准化了穿心莲内酯的含量。我们进行了本研究,以调查1)穿心莲内酯在市售A. paniculata提取物中的选择性富集如何影响非标准化植物化学成分的可变性,以及2)如果提取物中非标准化成分中的可变性影响穿心莲内酯本身的药理活性。方法我们通过HPLC分析表征了印度的12种商业标准化(≥30%穿心莲内酯)批次的沙棘提取物。我们使用2,2-二苯基-1-picylhydrazyl(DPPH)自由基清除,氧自由基抗氧化剂能力(ORAC)和Folin-Ciocalteu(FC)抗氧化剂测定法确定了提取物的抗氧化剂能力。通过测定其对人单核细胞系THP-1中肿瘤坏死因子α(TNF-α)释放的抑制作用来评估其抗炎活性。结果样品中穿心莲内酯的含量接近要求的值(32.2±±2.1%,范围为27.5至35.9%)。在测试批次中,二十一种非标准化成分的HPLC峰强度变化超过2倍。批次中的绿原酸含量变化超过30倍。在批次之间,DPPH自由基清除活性变化约3倍,ORAC和FC抗氧化能力变化约1.5倍。相反,提取物的TNF-α抑制活性几乎没有变化,与纯穿心莲内酯的比较表明,这主要归因于穿心莲内酯的含量。结论标准化的人参沙棘提取物含有声称含量的穿心莲内酯,但表现出相当大的植物化学背景变化。提取物的DPPH自由基清除活性主要归因于提取物中的类黄酮/苯甲酸化合物。穿心莲内酯对TNF-α释放的抑制作用几乎不受非标准化成分定量变化的影响。

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