Antioxidant, anti-semicarbazide-sensitive amine oxidase, and anti-hypertensive activities of geraniin isolated from Phyllanthus urinaria

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• 作者：Shyr-Yi Lin ; Ching-Chiung Wang ; Yeh-Lin Lu ; Wen-Chun Wu ; Wen-Chi Hou
• 关键词：Antihypertensive activity ; Angiotensin converting enzyme (ACE) ; Antioxidant ; Geraniin ; Phyllanthus urinaria ; Semicarbazide-sensitive amine oxidase (SSAO)
• 刊名：Food and Chemical Toxicology
• 出版年：2008
• 期刊代码：20_02786915
• 类别：pha
• 出版时间：July 2008
• 卷：46
• 期：7
• 页码：2485-2492
• 文件大小：306 K

摘要

The wrinkle-fruited leaf flower (Phyllanthus urinaria L.) (Euphorbiaceae) is widely used as a traditional folk medicine for inflammatory relief. Geraniin, the hydrolysable tannin, was purified by a series of chromatographic processes from the 70%aqueous acetone extracts of P. urinaria and identified by NMR [¹H (500 MHz) and ¹³C NMR (126 MHz)] spectra and mass spectroscopy. The scavenging activities of geraniin against DPPH radicals (half-inhibition concentration, IC₅₀, were 0.92 and 1.27 μM, respectively, for pH 4.5 and pH 7.9), hydroxyl radicals (IC₅₀ was 0.11 μM by deoxyribose method and 1.44 μM by electron spin resonance method), and superoxide radicals (IC₅₀ were 2.65 μM) were determined in comparison with positive controls. The inhibitory activities against xanthine oxidase (IC₅₀ were 30.49 μM) were measured. Geraniin also showed dose-dependent inhibitory activities against semicarbazide-sensitive amine oxidase (SSAO, IC₅₀ were 6.58 μM) and against angiotensin converting enzyme (ACE, IC₅₀ were 13.22 μM). For kinetic property determinations, geraniin showed competitive inhibitions against SSAO (the apparent inhibition constant, K_i, was 0.70 μM) and mixed noncompetitive inhibitions against ACE. Spontaneously hypertensive rats (SHR, 10-week age) were orally administered to once (5 mg geraniin/kg SHR), and changes of systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured over 24 h and compared with the positive control of captopril (2 mg/kg SHR). The geraniin showed antihypertensive activity in lowering SBP and DBP and showed a significant difference from the blank (distilled water) at 2, 4, 6, 8, and 24 h. Healthy food products could use geraniin for antioxidant protection and therapeutic effects in the future.