辣木（Moringa oleifera Lam.）又名鼓槌树和牛奶树，因其树根部位有辛辣味得“辣木”之名[1]，于20世纪60年代引入我国，因中巴两国辣木合作研究而名声大噪，并迅速在国内掀起研究浪潮。辣木的大部分植物器官均有药用价值[2-3]，其中活性成分在医疗保健用品、化妆品、食品等领域均有使用，具有十分广阔的开发前景和极其重要的研究意义。
随着生活水平的提高，人们的目光已经逐渐转向饮食健康和对各种威胁人体健康的慢性疾病的预防上，辣木叶随之走进大众和学者视野。目前辣木叶研究主要集中在诸多活性成分的提取工艺和药理活性探究上。本文对相关研究成果进行总结并归纳，以期为辣木叶在今后相关各领域的研究和使用提供科学依据。
辣木叶干粉的蛋白含量约为30%，与大豆中的蛋白质的含量相近，且含有人体所需的7种必需氨基酸（含量约占总氨基酸量的32.6%），因此在一些地区被用作儿童和婴儿的营养补充剂[4-5]。蛋白营养质量高低取决于食用的蛋白中8种人体必需氨基酸的绝对含量和相对含量以及消化吸收后的生物利用度[6]。大多数植物中蛋白含硫氨基酸含量低，要摄取多种植物蛋白才能满足人体生长发育所需。植物中的非蛋白的成分（鞣酸、植酸）和蛋白成分（蛋白酶抑制剂、凝集素）均会影响蛋白在人体胃肠道消化和吸收过程[7]。虽然植物蛋白的吸收利用受一定限制，但其广阔的开发前景不容忽视。
辣木叶中优质蛋白除了给人食用和用作饲料给动物补充蛋白外[8-9]，还可用来酶解得到具有较强的清除自由基能力和修复氧化损伤的抗氧化肽[10]。Paula等[11]从辣木叶中获得一种辣木叶蛋白质（Moringa oleifera leaf protein isolate，Mo-LPI），该蛋白不仅刺激糖尿病小鼠的胰岛素分泌，还能通过降低丙二醛水平和增加过氧化氢酶活性来有效降低糖尿病小鼠的氧化应激，同时Mo-LPI在浓度为2 500 mg/kg下不会对小鼠造成急性毒性，因此辣木叶蛋白Mo-LPI是治疗糖尿病的替代品或补充剂。
吕晓亚等[12]采用超声-微波协同萃取方法提取辣木叶水溶性蛋白，在料液比1∶160（g/mL），提取时间127 s，微波功率40 W，pH值为11时，辣木叶蛋白最高得率为40.11 mg/g。施娅楠等[13]报道了酶解法提取辣木叶非水溶性蛋白，在碱性蛋白酶用量1.8%，温度55℃，提取时间70 min条件下，蛋白提取率约34 mg/g。
辣木叶中的总黄酮含量为62mg/g（折合异槲皮素），检测出的主要有槲皮素、异槲皮素、山奈酚、异鼠李素等，并多以苷的结合形式存在[14-16]。研究表明，槲皮素通过抑制环加氧酶和脂氧合酶活性对炎症有抑制作用[17]，山奈酚和异鼠李素有抗癌疗效是食品衍生的预防癌症的化合物和抗癌的潜在候选药物[18-19]。
Wang等[20]使用亚临界乙醇在126.6℃，2.05 h条件下的辣木叶黄酮化合物提取率为2.6%，与传统乙醇回流法相比，产率提高了26.7%。Dadi等[21]试验发现用超声波辅助对辣木叶中的总黄酮和总酚的提取有较大的帮助，超声波能加速有效物质从植物细胞中释放和扩散。研究对比微波辅助提取与加压萃取2种不同的提取方法，加压萃取能够提取具有更多羟基类取代基的酚类化合物，如山奈酚二糖苷及其乙酰基衍生物和对高温敏感的硫代葡萄糖苷或氨基酸，而微波辅助提取可以更好地提取山奈酚、槲皮素及其葡糖苷衍生物，应根据要分离的目标化合物选择提取方法[22]。
董竹平等[23]选取3种分别来自亚洲与非洲的辣木叶，测得多糖含量分别为6.84%、4.67%和3.78%。辣木叶中的多糖含量除了受品种影响外，还与采收时间和采收部位有关[24-25]。因结构复杂多样，多糖已成为生命体中除蛋白质和核酸之外能承担起复杂生理功能需求的生物大分子[26]。关于辣木多糖类物质，目前研究发现有抗氧化、抗炎、降血糖、降血脂、免疫增强、抗病毒[27-32]等作用。
在保证辣木叶多糖的总提取率尽量高的前提下，同时要考虑兼顾到提取温度、提取时间及提取的pH值等因素，以保证多糖的空间结构和生物活性不会降低甚至丧失。王振西[33]通过响应面优化试验获得超声协同纤维素酶提取法的最佳工艺参数：料液比1 ∶50（g/mL）、pH 5.17、超声功率 210 W、提取时间35 min、提取温度75℃，纤维素酶1 800 U/mg，辣木多糖的提取率为33.11%。该试验优化的超声波加酶的提取法比吴玲雪等[34]的传统热水提取法提取率高一倍，温度低5℃，时间减少85 min，同时比彭凌[35]的超声波辅助法的提取率高三分之一，但所用的时间长，温度更加高，还需高效纤维素酶辅助。
目前从不同品种的辣木叶中分离鉴定出的化合物包括甾体、脂肪酸、酯、醇等，其活性物质主要有β-谷甾醇、豆甾醇、羊毛甾醇、维生素E、植醇、棕榈酸、香草乙酮、香芹酚、β-紫罗酮等[36-39]。辣木叶挥发油对金黄色葡萄球菌、铜绿假单胞菌、大肠杆菌和蜡状芽孢杆菌等细菌，以及桔青霉、指状青霉、毛癣菌、表皮癣菌等真菌均有不同程度的抑制作用[39-41]。Otunola等[42]报道了辣木叶挥发油通过抑制蛋白质变性提升红细胞膜的稳定性，且IC50值为0.2 mg/mL。
从辣木叶中提取挥发油，袁明焱等[37]用正己烷萃取法的产率为0.88%，分离出43种化合物；蔡彩虹等[39]用水蒸气蒸馏法的产率为0.53%，分离出34种化合物；Zhao等[43]用超临界流体萃取法的产率为6.34%，分离出12种化合物。因此正己烷萃取法是目前比较合适的提取方法，同时兼顾了提取效率和化合物数量。
辣木叶中含有的三萜类、黄酮和多糖等物质可以通过抑制肿瘤细胞变态生长、诱导癌症细胞凋亡和抑制癌症细胞抗氧化等多种途径来治疗癌症[44]。Jintana等[45]通过柱层析法从辣木叶（Moringaoleiferaleaf，MOL）提取物得到连续组分 MOL1、MOL2、MOL3、MOL4。研究表明，MOL2、MOL 3和MOL 4均以浓度依赖性方式抑制人结肠癌HCT116细胞生长，且抑制作用是由胞外信号调节激酶1/2磷酸化下调介导的。Madi等[46]研究了用辣木叶水提取物能促使人肺癌A549细胞凋亡，提取物能让细胞能量代谢发生障碍，诱发重要蛋白酶和DNA氧化损伤，还促进胱天蛋白酶活化和促凋亡蛋白表达增加。辣木叶水提取物中含有对人乳腺癌细胞MCF-7细胞具有细胞毒性作用的异硫氰酸苄酯，该物质能激活p38丝裂原活化蛋白激酶信号通路来促进细胞凋亡[47]。Berkovich等[48]体外实验发现人胰腺癌细胞Panc-1细胞暴露于2mg/mL辣木叶水提取物后，细胞活力的降低达到100%，免疫印迹分析发现提取物可以显著减少细胞核转录因子κB信号传导途径中的细胞核转录因子RelA（p65），细胞核转录因子κB抑制蛋白α和磷酸化细胞核转录因子κB抑制蛋白α的表达，因细胞核转录因子κB信号传导途径的抑制导致Panc-1细胞的存活能力下降。
随着糖尿病的发病率逐渐升高，有研究表明辣木叶具有降血糖疗效，对辣木叶提取物降糖机理相关研究日益深入[49-50]。Irfan等[51]研究发现辣木叶乙醇提取物对Ⅰ型糖尿病大鼠有急性抗高血糖活性，同时鉴定出具有潜在的降糖物质可能是乙醇提取物中的隐绿原酸、槲皮素-3-β-D-葡萄糖苷和山奈酚-3-O-葡萄糖苷。Olayaki等[52]在治疗糖尿病小鼠过程中发现，辣木叶甲醇提取物能够提高胰岛素分泌水平，进而增强肝脏细胞和肌肉细胞对葡萄糖摄取及糖原合成来降血糖。除了增加胰岛素分泌水平外，胰腺β细胞的保护和再生，肝组织中糖异生途径中的丙酮酸羧化酶的mRNA表达正常化，抑制α-淀粉酶和α-葡萄糖苷酶的活性等途径也是辣木叶提取物治疗糖尿病小鼠的重要途径[53-55]。
高脂血症是常见慢性心血管疾病的发病因素之一，易引发动脉粥样硬化、冠心病和外周血管病变等代谢性疾病，也会增加Ⅱ型糖尿病和脂肪肝的发病率。辣木叶中的植物固醇、2-腈苷、3-芥子糖苷等物质能降低胆固醇的吸收，可用作开发治疗高脂血症的药物[56]。有研究报道了喂食辣木叶粉可降低高脂血症大鼠的胆固醇、甘油三酯、低密度脂蛋白水平与抑制丙二醛和丙氨酸氨基转移酶活性，表明辣木叶有较好的降血脂功效[57]。
Jing等[58]报道辣木叶石油醚提取物以剂量依赖性方式抑制小鼠3T3-L1脂肪细胞中的脂肪形成，并在高剂量下对细胞存活率没有影响。进一步实验证实该提取物能显著下调3T3-L1脂肪细胞中的脂肪生成过程中相关蛋白表达和抑制脂肪酸合成酶活性来抑制脂肪酸的合成，上调3T3-L1脂肪细胞中脂代谢途径相关蛋白的表达。高脂小鼠动物实验发现，该提取物在高剂量下显着降低了血清总胆固醇、低密度脂蛋白胆固醇和天冬氨酸转氨酶的水平，在小鼠肝和附睾脂肪组织中下调了与脂肪生成相关的蛋白的表达，并上调了与脂解相关的蛋白表达，并增加脂代谢途径中限速酶即腺嘌呤核糖核苷酸的蛋白激酶α表达以抑制脂肪细胞释放脂肪酸及促进脂肪酸降解。
人工合成多种抗生素因容易获得、价格合适和疗效好已在许多领域内广泛使用。虽然已推行联合用药减缓耐药菌株的产生速度，但耐药菌株的出现是不可避免的，植物源“抗生素”成为较好的解决方案[59]。
Rahman等[60]报道出新鲜辣木叶乙醇提取物对志贺氏菌、铜绿假单胞菌、蜡状芽孢杆菌、枯草杆菌等均有一定抑制作用。辣木叶甲醇提取物对金黄色葡萄球菌和鼠伤寒沙门氏菌有抑制活性[61]；辣木叶乙醇提取物对耐甲氧西林金黄色葡萄球菌的细胞壁有破坏作用以及能显著影响两种管家蛋白的产生来抗菌[62]；辣木叶乙酸乙酯提取物对烟曲霉、黑曲霉和白色念珠菌等真菌有体外抑制活性，并分析出单宁是主要活性物质[63]。Khatun等[64]直接从辣木叶中分离得到了3种凝集素（糖蛋白）SLL-1、SLL-2和SLL-3。在3种常见的致病菌的抑制活性试验中观察到SLL-1表现出最高抗菌活性。试验还通过卤虫（Artemia salina L.）测得凝集素的细胞毒性，三者 LC50值分别为 15.8、17.78、14.12 μg/mL。
胃溃疡是一种消化道常见且多发的疾病，逐渐呈年轻化的趋势。其诱因主要有幽门螺旋杆菌感染、胃酸分泌异常、非甾体药物刺激、不良的生活习惯等。Verma等[65]实验发现，辣木叶乙醇提取物以剂量依赖方式减少大鼠的幽门结扎胃溃疡模型、应激胃溃疡模型、阿司匹林诱导胃溃疡模型等的胃溃疡面积，抗溃疡的机制是通过代谢脂质过氧化物和清除内源性H2O2等抗氧化途径实现。经辣木叶水提取物治疗后的胃溃疡小鼠的肠嗜铬细胞密度增加，5-羟色胺含量增加，黏膜厚度增加，显示出对胃黏膜的保护作用[66]。辣木叶水提取物能帮助阿司匹林诱导的胃溃疡小鼠的环氧合酶-1基因的表达水平与胃的黏膜黏蛋白数量接近正常值，同时还促使炎症因子中的肿瘤坏死因子-α、转化生长因子-β和环氧合酶-2基因表达下调2.7、2.3、4.1倍[67]。辣木叶对胃溃疡的多重疗效相对于中和、抑制胃酸分泌药物和抗生素的联合使用有其独特的治疗优势。
研究结果表明，辣木叶中含有的蛋白、多酚、糖类等成分均有抗氧化活性，抗氧化能力受到品种提取工艺、生长时间、品种等因素影响[68-69]。辣木叶的抗氧化成分能通过直接清除自由基和络合金属离子，提高抗氧化相关的酶系统基因的表达，激活核因子E2相关因子2/血红素加氧酶-1途径调节氧化应激等方式实现抗氧化[70-72]。
辣木叶蛋白含量高且含有多种人体必需氨基酸能满足生长需求，黄酮类物质能抗氧化延缓衰老和预防癌症，多糖类物质能抗病毒和增强免疫力，挥发油能抑制多种有害细菌和真菌的生长繁殖。辣木叶营养价值丰富，生物学药理活性突出，能够治疗和预防多种疾病。然因辣木的种植技术和品种改良研究不够深入限制了辣木叶的产量，活性物质提取工艺的提取效率较低，辣木叶的其它药理功能，如抗溃疡、保肝、通便等研究较少，药理功能的物质基础与治病机理的探究有待进一步加深。
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Research Progress on the Pharmacological Functions of Active Components in Moringa oleifera Leaves
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