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黔產(chǎn)昆明山海棠化學(xué)成分及其抑菌活性研究

2019-09-10 05:28李江李??穆淑珍張仕林王莉云郝小江鄧璐璐
廣西植物 2019年11期

李江 李?? 穆淑珍 張仕林 王莉云 郝小江 鄧璐璐

摘?要:該研究采用硅膠柱色譜、Sephadex LH-20 凝膠柱色譜、半制備型高效液相色譜和重結(jié)晶等方法分離純化,從黔產(chǎn)昆明山海棠乙醇提取物中分離得到11個化合物,并采用96孔板微量稀釋法對化合物進(jìn)行抑菌活性測定。結(jié)果表明:利用 NMR,MS 等現(xiàn)代波譜技術(shù)以及化合物的理化性質(zhì)并結(jié)合參考文獻(xiàn)分別鑒定為3-O-乙?;R墩果酸(1),雷酚萜(2),3-氧代齊墩果酸(3),β-谷甾醇(4),木栓酮(5),β-谷甾醇棕櫚酸酯(6),雷公藤紅素(7),大黃素(8),雷公藤內(nèi)酯甲(9),雷藤二萜醌 B(10),ent-kauran-16 β,19-diol(11)。抑菌活性結(jié)果顯示,化合物3、7和8具有較好的抑菌作用,MIC值為2~16 μg·mL-1。其中,化合物6、11為首次從該植物中分離得到,化合物11為首次從雷公藤屬植物中分離得到,且首次發(fā)現(xiàn)了化合物3、7對綠膿桿菌和青枯菌具有明顯的抑制作用。

關(guān)鍵詞:昆明山海棠, 雷公藤屬, 雷公藤紅素, 雷藤二萜醌 B, 抑菌作用

中圖分類號:Q946.91

文獻(xiàn)標(biāo)識碼:A

文章編號:1000-3142(2019)11-1505-07

Abstract:Eleven compounds were isolated and purified from ethanol extract of Tripterygium hypoglaucum from Guizhou Province by silica gel column chromatography, Sephadex LH-20 gel column chromatography, semi-prepared HPLC and recrystallization. Their antibacterial activity were determined by 96-well plate microdilution method. The results were as follows:The structures were identified as 3-O-acetyloleanolicacetic anhydride(1), triptonoterpene(2), 3-Oxo-olean-12-en-28-oic acid(3), β-sitosterol(4), friedelin(5), β-sitosteryl palmitate(6), celastrol(7), emodin(8), wilforlide A(9), triptoquinone B(10), and ent-kauran-16 β, 19-diol(11) by NMR, MS, physicochemical properties and some reported data. Based on the results of antibacterial activity, compounds 3, 7 and 8 showed potential activity, and their MIC values were 2-16 μg·mL-1. Compounds 6 and 11 were isolated from this plant for the first time, and meanwhile compound 11 was also isolated from the genus of Tripterygium for the first time. Furthermore it was found firstly that compounds 3 and 7 had significant inhibitory effects on Pseudomonas aeruginosa and Rastonia solanacearum.

Key words:Tripterygium hypoglaucum, Tripterygium, celastrol, triptoquinone B, antibacterial activity

昆明山海棠(Tripterygium hypoglaucum),又名紫金皮、大方藤、洋道藤、粉背雷公藤、九團(tuán)花、火把花等,是衛(wèi)矛科(Celastraceae)雷公藤屬(Tripterygium)有毒木質(zhì)藤本植物。產(chǎn)于貴州、湖南、云南、廣西、江西等地,貴州主要分布在梵凈山、雷公山、臺江、龍里、興仁、興義等地。目前臨床上相關(guān)藥品及制劑主要作為免疫抑制劑,用于治療類風(fēng)濕性關(guān)節(jié)炎、慢性腎炎、麻風(fēng)反應(yīng)、白血病和紅斑狼瘡等多種膠元性疾病及自身免疫性疾病,且療效確切,效果良好(國家中醫(yī)藥管理局《中華本草》編委會,1999)。近年來藥理學(xué)研究表明昆明山海棠還具有抗生育作用(周激文等,1991;Zhen et al., 1995)。

目前,針對昆明山海棠,國內(nèi)外均以抗腫瘤方面的研究為主,而其抑菌活性少見報道。為開發(fā)利用該植物資源,探索昆明山海棠的化合物結(jié)構(gòu)及其活性成分,本文對黔產(chǎn)昆明山海棠抑菌活性明顯的乙酸乙酯萃取部位化學(xué)成分進(jìn)行初步研究。該研究進(jìn)一步豐富了昆明山海棠的化學(xué)研究,為綜合利用昆明山海棠資源奠定了基礎(chǔ)。

1?材料、儀器與試劑

1.1 材料

昆明山海棠2016年10月采集于貴州省雷山縣,經(jīng)貴陽中醫(yī)學(xué)院孫慶文教授鑒定為昆明山海棠(Tripterygium hypoglaucum)的根,標(biāo)本存放于省部共建藥用植物功效與利用國家重點實驗室中。

金黃色葡萄球菌(Staphyloccus aureus)、綠膿桿菌(Pseudomonas aeruginosa)、枯草芽孢桿菌(Bacillus subtilis)、青枯菌(Rastonia solanacearum)由省部共建藥用植物功效與利用國家重點實驗室李老師提供。

1.2 儀器與試劑

儀器:恒溫振蕩器HZQ-F160A(上海一恒科學(xué)儀器有限公司),立式壓力蒸汽滅菌鍋LDZX-50KBS(上海申安醫(yī)療器械廠),SW-CJ-2FD型雙人單面凈化工作臺(蘇州凈化設(shè)備有限公司),電子天平FA2204B(上海精科天美科學(xué)儀器有限公司),INOVA-400 MHz 核磁共振波譜儀,Bruker AM-400和DRX-500 核磁共振儀(TMS為內(nèi)標(biāo),瑞士Bruker公司),Si-HPLC 半制備色譜儀(美國Waters公司)。材料:Sephadex LH-20 凝膠(40~70 μm)(瑞士Amersham Pharmacia Biotech AB 公司),柱層析硅膠(200~300目和300~400目),硅膠H(10~40 μm)和薄層層析用硅膠GF254(0.20~0.25 mm)(青島海洋化工廠)。

試劑:本實驗所用HPLC試劑均為色譜純試劑,二氯甲烷、石油醚、乙酸乙酯、甲醇、乙醇(分析純,上海泰坦科技股份有限公司),氯仿(工業(yè)級,使用前經(jīng)重蒸處理),其余試劑為國產(chǎn)分析純。LB培養(yǎng)基:胰蛋白胨10.0 g ·L-1,酵母提取物5.0 g ·L-1,NaCl 10.0 g ·L-1,pH=7.4,在高壓下121 ℃濕熱滅菌21 min。陽性對照藥:環(huán)丙沙星(薩恩化學(xué)技術(shù)有限公司)。

2?研究方法

2.1 提取和分離

取昆明山海棠干燥根19.4 kg,用無水乙醇提取3次,時間分別為4、3、2 h,合并提取液,用水乙醇提取液=11減壓回收乙醇至無醇味,得到昆明山海棠水溶液;用乙酸乙酯萃取上述水溶液3次,濃縮乙酸乙酯層萃取液得到浸膏275 g,經(jīng)常壓硅膠柱層析, 以石油醚-乙酸乙酯、 氯仿-甲醇溶劑系統(tǒng)梯度洗脫,得到Fr. 1-7。Fr. 2(9.4 g)經(jīng)硅膠柱層析,以石油醚∶乙酸乙酯=200∶1洗脫,并通過重結(jié)晶得到化合物5(18 mg)和6(56 mg)。Fr. 5(69.2 g)經(jīng)硅膠柱層析,以石油醚-乙酸乙酯、氯仿-甲醇溶劑系統(tǒng)梯度洗脫,得到Fr. 5.1-5.5。Fr.5.1經(jīng)硅膠柱層析,以石油醚∶乙酸乙酯=30∶1洗脫以及 Sephadex LH-20 凝膠柱色譜分離(甲醇),得到化合物1(39 mg)、2(5 mg)、3(563 mg)、4(803 mg)和8(12 mg)。Fr. 5.2經(jīng)硅膠柱層析,以氯仿∶甲醇=40∶1洗脫,Si-HPLC(甲醇水=8812)以及 Sephadex LH-20 凝膠柱色譜(氯仿甲醇=11,甲醇),分離得到化合物7(140 mg)、9(9 mg)、10(22 mg)和11(16 mg)。

2.2 最小抑菌濃度(MIC)的測定

2.2.1 菌懸液的制備?將活化的各供試菌種分別接種3~5個單菌落于30 mL LB培養(yǎng)基的100 mL三角瓶中,增殖6 h,再另取提前裝好3 mL LB培養(yǎng)基用于稀釋菌液至1.5×108個·mL-1,再用LB 培養(yǎng)基稀釋1 000倍即為1.5×105個·mL-1備用。

2.2.2 最小抑菌濃度(MIC)的測定?在無菌操作臺上將滅菌后的LB培養(yǎng)基,加入100 μL于96孔板每個孔中,A,B,C 3排的第1孔加入配制的藥液A(濃度為1 024 μg·mL-1)100 μL;D,E,F(xiàn) 3排的第1孔加入配制的藥液B(濃度為1 024 μg·mL-1)100 μL,用移液槍對A~F排充分吹打使藥液與培養(yǎng)基混勻,然后進(jìn)行2倍稀釋,照此重復(fù)至第12孔,第12孔混勻后吸100 μL棄去;將配制的菌懸液加100 μL于96孔板中,重復(fù)3次(A,B,C 3排樣品);在同一96孔板上的G排為空白對照(空白培養(yǎng)基)和F排為陰性對照(菌液和培養(yǎng)基),于37 ℃恒溫培養(yǎng)18~24 h,96孔板中沒有混濁的最后1孔的最低藥液濃度為該化合物的最小抑菌濃度(μg ·mL-1),分別記錄實驗結(jié)果。

3?結(jié)果與分析

3.1 結(jié)構(gòu)鑒定

化合物1?白色粉末,EI-MS(m/z):498[M]+,分子式為C32H50O4。1H-NMR(400 MHz,CDCl3) δ:5.27(1H,t,J=4.0 Hz,H-12),4.49(1H,t,J=8.0 Hz,H-3),2.83(1H,dd,J=13.8,4.6 Hz,H-18),2.05(3H,s,Me-OAc),1.12(3H,s,Me),0.94(3H,s,H-30),0.93(3H,s,H-29),0.90(3H,s,H-25),0.86(3H,s,H-23),0.85(3H,s,H-24),0.74(3H,s,H-26);13C-NMR(100 MHz,CDCl3) δ:38.0(C-1),23.4(C-2),80.9(C-3),37.7(C-4),55.2(C-5),18.1(C-6),32.4(C-7),39.2(C-8),47.5(C-9),36.9(C-10),22.8(C-11),122.5(C-12),143.6(C-13),41.5(C-14),27.6(C-15),23.5(C-16),45.8(C-17),40.8(C-18),46.5(C-19),30.6(C-20),33.7(C-21),32.5(C-22),28.0(C-23),16.6(C-24),15.4(C-25),17.1(C-26),25.9(C-27),184.2(C-28),23.6(C-29),33.0(C-30),171.1(C=O),21.3(C-CH3)。以上數(shù)據(jù)與Carvalho et al.(1993)的報道一致,故鑒定化合物1為3-O-乙?;R墩果酸。

化合物2?白色結(jié)晶,EI-MS(m/z):300[M]+,分子式為C20H28O2。1H-NMR(400 MHz,CDCl3) δ:7.04(1H,d,J=8.3 Hz,H-12),6.86(1H,d,J=8.3 Hz,H-11),4.69(1H,s,-OH),3.12(1H,sept,J=7.0 Hz,H-15),2.89(1H,m,H-5),2.70(2H,m,H-7),2.58(2H,m,H-2),1.92(2H,m,H-1),1.87(2H,m,H-6),1.33(3H,s,H-20),1.27(3H,s,H-19),1.25(3H,s,H-18),1.17(3H,d,J=7.0 Hz,H-16),1.14(3H,d,J=7.0 Hz,H-17);13C-NMR(100 MHz,CDCl3) δ:37.1(C-1),34.7(C-2),217.2(C-3),47.3(C-4),50.0(C-5),19.5(C-6),24.6(C-7),120.8(C-8),146.4(C-9),37.6(C-10),117.3(C-11),123.6(C-12),130.3(C-13),150.1(C-14),26.9(C-15),22.5(C-16),22.7(C-17),24.4(C-18),26.6(C-19),21.2(C-20)。以上數(shù)據(jù)與(Kutney & Han, 1996)的報道一致,故鑒定化合物2為雷酚萜。

化合物3?白色粉末,EI-MS(m/z):454[M]+,分子式為C30H46O3。1H-NMR(400 MHz,CDCl3) δ:5.30(1H,t,J=4.0 Hz,H-12),2.83(1H,dd,J=13.7,4.1 Hz,H-18),2.54(1H,m,H-2),2.36(1H,m,H-2),1.14(3H,s,CH3),1.08(3H,s,H-30),1.04(3H,s,H-29),1.03(3H,s,H-25),0.93(3H,s,H-23),0.91(3H,s,H-24),0.81(3H,s,H-26);13C-NMR(100 MHz,CDCl3) δ:39.1(C-1),34.1(C-2), 217.8(C-3),46.6(C-4),55.3(C-5),19.5(C-6),32.1(C-7),39.2(C-8),47.4(C-9),36.8(C-10),22.9(C-11),122.3(C-12),143.6(C-13),41.7(C-14),27.7(C-15),23.6(C-16),46.9(C-17),41.0(C-18), 45.8(C-19),30.7(C-20),33.1(C-21),32.4(C-22),21.4(C-23),26.4(C-24),15.0(C-25),17.0(C-26), 25.8(C-27),183.9(C-28),33.8(C-29),23.5(C-30)。以上數(shù)據(jù)與Sun et al.(2008)的報道一致,故鑒定化合物3為3-氧代齊墩果酸。

化合物4?白色針晶,EI-MS(m/z):414[M]+,分子式為C29H50O。1H-NMR(500 MHz,CDCl3) δ:5.30(1H,br d,H-6),3.65(1H,m,H-3),0.96(3H,s,H-19),0.88(3H,d,J=6.6 Hz,H-21),0.82(3H,t,J=7.5 Hz,H-29),0.80(3H,d,J=6.8 Hz,H-27),0.77(3H,d,J=6.8 Hz,H-26),0.64(3H,s,H-18);13C-NMR(125 MHz,CDCl3) δ:37.2(C-1),31.4(C-2),71.6(C-3),42.1(C-4),140.8(C-5),121.6(C-6),31.8(C-7),31.8(C-8),50.0(C-9),36.4(C-10),21.0(C-11),39.7(C-12),42.2(C-13),56.7(C-14), 24.2(C-15),28.2(C-16),55.9(C-17),11.8(C-18),19.3(C-19),36.1(C-20),18.9(C-21),33.8(C-22), 29.0(C-23),45.7(C-24),25.9(C-25),18.7(C-26),19.7(C-27),23.0(C-28),11.8(C-29)。以上數(shù)據(jù)與Li et al.(2008)的報道一致,故鑒定化合物4為 β-谷甾醇。

化合物5?白色針晶,EI-MS(m/z):426[M]+,分子式為C30H50O。1H-NMR(500 MHz,CDCl3) δ:2.31(1H,m,H-2),2.25(1H,m,H-4),1.18(3H,s,H-28),1.05(3H,s,H-27),0.98(3H,s,H-26),0.99(6H,d,J=5.1 Hz,H-29,30),0.95(3H,s,H-25),0.87(3H,s,H-23),0.72(3H,s,H-24);13C-NMR(125 MHz,CDCl3) δ:22.3(C-1),41.5(C-2),213.3(C-3),58.2(C-4),42.1(C-5),41.3(C-6),18.2(C-7), 53.1(C-8),37.4(C-9),59.5(C-10),35.6(C-11),30.5(C-12),38.3(C-13),39.7(C-14),32.4(C-15), 36.0(C-16),30.0(C-17),42.8(C-18),35.3(C-19),28.2(C-20),32.8(C-21),39.2(C-22),6.8(C-23), 14.7(C-24),17.9(C-25),20.3(C-26),18.7(C-27),32.1(C-28),35.0(C-29),31.8(C-30)。以上數(shù)據(jù)與Ageta et al.(1995)的報道一致,故鑒定化合物5為木栓酮。

化合物6?白色晶體,EI-MS(m/z):653[M]+,分子式為C45H80O2。1H-NMR(500 MHz,CDCl3) δ:5.37(1H,d,J=4.6 Hz,H-6),4.62(1H,t,J=5.5 Hz,H-3),2.31(2H,m,H-4),2.27(2H,t,J=7.5 Hz,H-2′),1.85(2H,m,H-2),1.26,1.62(2H,m,H-3′),1.02(3H,s,H-19),0.92(2H,d,J=6.5 Hz, H-24),0.89(2H,m,H-21),0.84(2H,m,H-26),0.82(3H,s,H-29),0.68(3H,s,H-18);13C-NMR(125 MHz,CDCl3) δ:37.0(C-1),27.8(C-2),73.7(C-3),38.2(C-4),139.7(C-5),122.6(C-6),31.9(C-7),31.9(C-8),50.0(C-9),36.6(C-10),21.0(C-11),39.7(C-12),42.3(C-13),56.7(C-14),24.3(C-15),28.2(C-16),56.0(C-17),11.8(C-18),19.3(C-19),36.2(C-20),18.8(C-21),33.9(C-22),26.1(C-23),45.8(C-24),29.1(C-25),19.8(C-26),19.0(C-27),23.1(C-28),12.0(C-29),173.3(C-1′),34.7(C-2′),25.1(C-3′),29.3(C-4′),29.4(C-5′),29.5(C-6′),29.6(C-7′),29.7(C-8′),29.7(C-9′),29.7(C-10′),29.7(C-11′),29.7(C-12′),29.7(C-13′),31.9(C-14′),22.7(C-15′),14.1(C-16′)。以上數(shù)據(jù)與孫紅祥等(2002)的報道一致,故鑒定化合物6為 β-谷甾醇棕櫚酸酯。

化合物7?紅色結(jié)晶,ESI-MS(m/z):473[M+Na]+,分子式為C29H38O4。1H-NMR(500 MHz,CDCl3) δ:7.06(1H,d,J=5.2 Hz,H-6),6.49(1H,br s,H-1),6.32(1H,d,J=6.3 Hz,H-7),2.21(3H,s,H-23),1.43(3H,s,H-24),1.27(3H,s,H-28),1.24(3H,s,H-25),1.09(3H,s,H-27),0.58(3H,s,H-26);13C-NMR(125 MHz,CDCl3) δ:120.4(C-1),178.3(C-2),147.0(C-3),120.5(C-4),127.5(C-5),135.4(C-6),118.3(C-7),172.7(C-8),43.1(C-9),165.0(C-10),33.8(C-11),29.3(C-12),39.3(C-13),45.3(C-14),28.7(C-15),36.3(C-16),30.6(C-17),44.2(C-18),31.0(C-19),39.9(C-20),29.5(C-21), 34.5(C-22),10.5(C-23),38.3(C-24),21.4(C-25),18.7(C-26),31.5(C-27),182.5(C-28),32.4(C-29)。以上數(shù)據(jù)與倪慧艷等(2014)的報道一致,故鑒定化合物7為雷公藤紅素。

化合物8?黃色粉末,ESI-MS(m/z):269[M-H]-,分子式為C15H10O5。1H-NMR(500 MHz,CDCl3) δ:7.52(1H,br s,H-4),7.18(1H,d,J=3.2 Hz,H-5),7.03(1H,d,J=1.8 Hz,H-2),6.57(1H,d,J=3.2 Hz, H-7),2.43(3H,s,H-11);13C-NMR(125 MHz,CDCl3) δ:165.8(C-1),124.9(C-2),148.8(C-3),121.5(C-4),133.9(C-4a),109.8(C-5),166.8(C-6),108.9(C-7),162.8(C-8),114.3(C-8a),191.0(C-9), 110.2(C-9a),183.1(C-10),136.0(C-10a),22.2(C-11)。以上數(shù)據(jù)與Kim et al.(2016)的報道一致,故鑒定化合物8為大黃素。

化合物9?無色針狀晶體,ESI-MS(m/z):477[M+Na]+,分子式為C30H46O3。1H-NMR(500 MHz,CDCl3) δ:5.30(1H,t,J=3.7 Hz,H-12),4.14(1H,d,J=5.4 Hz,H-22),3.21(1H,m,H-3),1.20(3H,s,H-30),1.07(3H,s,H-27),0.99(3H,s,H-23),0.94(3H,s,H-25),0.93(3H,s,H-26),0.86(3H,s,H-28),0.78(3H,s,H-24);13C-NMR(125 MHz,CDCl3) δ:38.6(C-1),27.2(C-2),78.9(C-3),38.8(C-4),55.2(C-5),18.3(C-6),33.1(C-7),42.5(C-8),47.5(C-9),37.0(C-10),23.5(C-11),124.7(C-12), 140.2(C-13),39.3(C-14),25.2(C-15),24.3(C-16),35.3(C-17),43.4(C-18),39.8(C-19),39.5(C-20), 33.9(C-21),83.2(C-22),28.1(C-23),15.7(C-24),15.7(C-25),17.0(C-26),24.1(C-27),25.0(C-28), 182.5(C-29),21.0(C-30)。以上數(shù)據(jù)與Wang KW & Wang SW(2014)的報道一致,故鑒定化合物9為雷公藤內(nèi)酯甲。

化合物10?無定形粉末,ESI-MS(m/z):353[M+Na]+,分子式為C20H26O4。1H-NMR(500 MHz,CDCl3) δ:6.35(1H,d,J=1.0 Hz,H-12),4.03(1H,d,J=11.4 Hz,H-19),3.44(1H,d,J=11.4 Hz,H-19), 2.98(1H,sept,d,J=6.9,1.2 Hz,H-15),2.82(1H,m,H-7),2.78(1H,m,H-1),2.67(1H,m,H-2), 2.46(1H,ddd,J=15.7,9.0,5.9 Hz,H-2),2.27(1H,m,H-7),1.99(1H,dd,J=13.0,2.2 Hz,H-5), 1.86(1H,m,H-6),1.79(1H,m,H-7),1.44(1H,m,H-1),1.32(3H,s,18-Me),1.26(3H,s,20-Me), 1.09(6H,dd,J=6.9,1.7 Hz,16,17-Me);13C-NMR(125 MHz,CDCl3) δ:34.4(C-1),34.2(C-2),220.6(C-3),50.2(C-4),51.6(C-5),17.8(C-6),25.4(C-7),142.5(C-8),147.5(C-9),37.0(C-10),187.3(C-11),131.8(C-12),153.3(C-13),187.5(C-14),26.3(C-15),21.3(C-16),21.2(C-17),22.5(C-18), 65.5(C-19),21.1(C-20)。以上數(shù)據(jù)與張彥文等(2007)的報道一致,故鑒定化合物10為雷藤二萜醌 B。

化合物11?無色針狀晶體,ESI-MS(m/z):329[M+Na]+,分子式為C20H34O2。1H-NMR(600 MHz,CDCl3) δ:1.82(1H,m,H-13),1.55(2H,s,H-15),1.38(3H,s,H-17),1.03(3H,s,H-20),0.97(1H,d,J=6.2 Hz,H-9),0.95(3H,s,H-18),0.91(1H,t,J=11.2 Hz,H-5);13C-NMR(150 MHz,CDCl3) δ:40.4(C-1),18.3(C-2),35.7(C-3),39.2(C-4),56.8(C-5),20.7(C-6),42.4(C-7),45.3(C-8),57.0(C-9),38.7(C-10),18.0(C-11),26.8(C-12),49.0(C-13),37.5(C-14),57.9(C-15),79.3(C-16),24.5(C-17),27.1(C-18),65.5(C-19),18.3(C-20)。以上數(shù)據(jù)與Rocha et al.(2009)的報道一致,故鑒定化合物11為ent-kauran-16β,19-diol。

3.2 化合物抗菌活性結(jié)果

以金黃色葡萄球菌、綠膿桿菌、青枯菌、枯草芽孢桿菌等4種菌株對分離鑒定的11個化合物進(jìn)行抗菌活性篩選,結(jié)果表明化合物3、7、8和10對金黃色葡萄球菌、綠膿桿菌、青枯菌有抑制作用,尤其是化合物3、7和8對金黃色葡萄球菌、綠膿桿菌、青枯菌有較強(qiáng)的抗菌作用,MIC值為2~16 μg ·mL-1(表1)。

4?結(jié)論

昆明山海棠和雷公藤是雷公藤屬植物中的兩個種,二者藥理作用很相似,均具有顯著的抗炎、抗腫瘤等活性,但其毒性要低于雷公藤。目前,針對雷公藤的相關(guān)研究及文獻(xiàn)報道非常多,相比之下,對昆明山海棠的化學(xué)成分及其生物活性研究就顯得比較少。通過對黔產(chǎn)昆明山海棠化學(xué)成分及其抑菌活性的研究,共分離鑒定化合物11個,其中化合物6、11為首次從該種植物中分離得到,且化合物11為首次從雷公藤屬植物中分離得到。抑菌活性結(jié)果顯示,化合物3、7、8和10對金黃色葡萄球菌、綠膿桿菌、青枯菌有抑制作用,并首次發(fā)現(xiàn)了化合物3、7對綠膿桿菌和青枯菌具有明顯的抑制作用。從抑菌結(jié)果可以推測昆明山海棠的抑菌活性成分主要為萜類化合物,后續(xù)還需對分離得到的其他同類化合物進(jìn)行抑菌活性測定,并對其構(gòu)效關(guān)系進(jìn)行研究,為設(shè)計和改造具有更高活性的化合物提供思路。另外,針對化合物3、7的毒性、其對綠膿桿菌抗藥性方面的研究,以及對青枯菌的抑菌作用機(jī)理也有待進(jìn)一步探究。

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