Chemical Components And Biological Activity From The Roots Of Aphanamixis Grandifolia BL

Objective In order to study the chemical ingredients and biological activity from the roots of Aphanamixis grandifolia Bl..Methods The roots of Aphanamixis grandifolia were extracted by refluxing with 95% EtOH three times, the EtOH distillate was concentrated in vacuum to obtain a crude residue, which was partitioned with PE(petroleum ether), EtOAc and n-BuOH, successively. The EtOAc fraction was separated over a whole series of methods(CC on silica gel, MCI, Sephadex LH-20, RP-C18 gel and so on) and purified by recrystallization to yield pure compounds. The structures were identified by the modern spectrum analysis technology(IR, UV, EI-MS, ESI-MS, HR-ESI-MS, 1H NMR, 13 C NMR, DEPT, 1H-1H COSY, HSQC, HMBC and so on) and the physico-chemical method. All compounds evaluated their antimicrobial activities against pathogenic bacteria of human, pathogenic fungi of agriculture, Ralstonia solanacearum by the paper-disc method. The antitumor activity of all compounds were measured by using MTT method. Acetylcholinesterase inhibitory activity of all compounds were also measured. The extractions of PE, EtOAc and n-BuOH were screened for their insecticidal activities against the method of mixing toxicity. The extraction of PE, EtOAc and n-BuOH were further evaluated their antimicrobial activities against C. gloeosporioides by using plate growth rate method.Results Thirty five compounds were isolated from the roots of Aphanamixis grandifolia, twenty one compounds were identified as aphanamolide E(1), dregeana-1(2), 6,6-dimethoxy-7α-hydroxy-stigmast-4-en-3-one(3), schleicheol 1(4), schleicheol 2(5), β-rosasterol(6), Stigmasterol(7), β-sitosterol(8), daucosterol(9), fregenedadiol(10), 7-hydroxycadalene(11), 6-deoxyjacareubin(12), isojacareubin(13), 4-oxopinoresinol(14), 4-ketopinoresinol(15), syringaresinol(16), episyringaresinol(17), graminone A(18), sylvatesmin(19), methyl-Z-6-nonadecenoate(20), palmitic acid(21). Compound 4 showed growth inhibitory activity of Fusarium oxysporum f.sp. niveum, and compound 11 showed growth inhibitory activity of Staphylococcus aureus and Ralstonia solanacearum. Compounds 4, 5, 6, 11 and 12 possessed inhibitory activity against SGC-7901 cell line, and compounds 11 and 12 showed inhibition of the proliferation of K562 cell line. None of inhibition of acetylcholinesterase activity to all compounds. The extractions of PE, EtOAc and n-BuOH from the roots of Aphanamixis grandifolia possessed little insecticidal activities against cotton leafworm. The extractions of PE and EtOAc from the roots of Aphanamixis grandifolia displayed moderate activities against C. gloeosporioides, and the extractions of n-BuOH showed moderate to weak activities against C. gloeosporioides.Conclusions Isolation and identification of the types of compounds from the roots of Aphanamixis grandifolia involved triterpenoids, steroids, diterpenes, sesquiterpenes, lignans, etc. Compound 1 was a new triterpenoid,and compound 3 was a new steroid. Compounds 1-6,10-15 and 18-20 were isolated from the genus Aphanamixis for the first time, and the 13 C NMR spectral data of compound 11 was reported for the first time. The activity studies shown that the roots of Aphanamixis grandifolia have well activity of antibacterial, antitumor and insecticidal.