栀子花的生理活性

栀子花(Gardenia,Gardenia jasminoides)

  茜草科(Rubiaceae)栀子属(Gardenia)

  英文名:Gardenia jasminoides、Gardenia jasminoides Ellis、Fructus gardeniae、Cape jasmine

  中文名:栀子花、山黄栀、黄栀子

  栀子开白或黄花,香气馥郁#3,主要分布中国各地,其他像越南、台湾、日本、缅甸或印度等地也常见#4,东方国家早有将果实作为天然食用色素和染料的纪录,习惯应用在面类或甜点,赋予黄、蓝和红等色彩#1-2,5-6。

【生理活性】

  栀子果实富含环烯醚萜类(iridoids)#1,例如:京尼平(genipin)、栀子苷(geniposide)和异栀子苷(gardenoside),摄取进入体内的栀子苷会在消化道藉由β-D-糖苷酵素(β-D-glycosidase)转换成京尼平#7。有研究描述#8,使用51.3%酒精、70.4℃和28.6分钟萃取栀子果实,可达到最佳萃取效果,分别获得10.9%栀子苷和2.497%总多酚含量。果实中还含有属于类胡萝卜素的藏花素(crocin)及其他键结衍生物#1,它也是番红花的主要活性成分,已有大量研究证明藏花素具有多种健康功效。

  栀子花有环烯醚萜类、黄酮类、二萜类、三萜类、酚酸类和有机酸酯类等成分#9-14。其精油、石油醚原精和生鲜花朵的主要成分皆含有芳樟醇(linalool,21.49-38.23%)、α-金合欢烯(α-farnesene,17.54-23.35%)、z-3-惕恪酸叶醇酯(z-3-hexenyl tiglate,12.67-16.27%)和反式-β-罗勒烯(trans-β-ocimene,2.61-9.50%),精油萃取率约0.02%(体积/生鲜重)#15,其他研究也有类似结果#16-18。根据152位志愿者参与的感官评测#16,脂吸法(enfleurage)使用鲸蜡和棕榈油萃取的栀子花原精香气如同刚摘下时花香,予人放松和净化感。

民俗疗法

  干燥的栀子熟果是传统中药,可泻火除烦、清热利湿、凉血散瘀,主治热病心烦、黄疸尿赤、火毒疮疡#19。文献纪载曾添加于治疗发炎、头痛、水肿、发烧、肝功能异常和高血压等药方#4。

抗氧化

  栀子果实的酒精和水萃取物,证实能消除多种自由基或超氧化物(superoxide),是多功能的抗氧化物质,其中水萃取物效果又优于酒萃物。藏花素于浓度20 ppm预防油脂过氧化的能力和常用抗氧化剂BHA(butylated hydroxyanisole)相似。#20

  1毫升栀子花精油消除阳离子自由基能力,约等同2.56 mg的水性维他命E;1公克石油醚原精则约为29.71 mg#15。

抗菌

  栀子花精油和石油醚原精能抑制金黄色葡萄球菌和表皮葡萄球菌,但对伤寒沙门氏菌(Salmonella typhi)、绿脓杆菌皆无效,精油另可抑制大肠杆菌、曲状杆菌(Campylobacter jejuni)和李斯特菌(Listeria monocytogenes)#15,21。另篇研究结果表示#13,栀子花二氯乙烷萃取物能抑制白色念珠菌,轻微抑制大肠杆菌、绿脓杆菌、金黄色葡萄球菌和须癣毛癣菌(Trichophyton mentagrophytes),对枯草杆菌(Bacillus subtilis)和黑霉菌(Aspergillus niger)则无效。

改善糖尿病

  第二型糖尿病主要发病机制源于胰岛素的分泌异常和抗性,胰岛素抗性(insulin-resistant)是指细胞无法对正常分泌的胰岛素有足够反应,导致葡萄糖和油脂异常的代谢,且胰岛素抗性是罹患第二型糖尿病的征兆之一,提早表现5-10年#22-24。

  口服200 mg/kg的栀子水萃物60分钟后可明显改善大鼠因类固醇诱发的胰岛素抗性、胰岛素敏感性和血糖值#22,进一步实验显示反应机转可能跟参与胰岛素讯息传递的两种蛋白质相关,受体底物1(insulin receptor substrate-1,IRS-1)和过氧化物酶体增殖物活化受体γ(peroxisome proliferator-activated receptor,PPARγ)两种蛋白质在口服后活化讯号明显放大。

  每日1次腹腔注射25 mg/kg京尼平于年迈大鼠持续12天#25,能有效改善因老化而导致的全身及肝胰岛素抗性,并缓解高胰岛素血症、高血脂和脂肪肝,减少肝脏氧化压力和粒线体失能。

抗忧郁

  越鞠丸是能行气解郁的传统中药,主要由苍术、香附、川芎、神麴、栀子等成分组成。在习得无助(learned helplessness)忧郁症动物模型#26,经灌胃0.8 g/kg栀子酒萃物的小鼠,于2、6和24小时后,皆能显著表现抗忧郁功效,而其他成分的效果并不明显,证明栀子在越鞠丸的快速抗忧郁功效可能扮演重要角色,另BDNF(Brain-derived neurotrophic factor)蛋白质的表现也显著增加,近年多项研究表示BDNF表现量和抗忧郁效果正相关#27,间接支持栀子有缓和忧郁的潜力。

顾胃

  栀子酒精萃取物及其内含成分─熊果酸(ursolic acid)和京尼平,能缓解大鼠因盐酸/酒精诱发的胃炎,实验发现这些物质可使酸中和、抗氧化并抑制幽门杆菌(Helicobacter pylori)的生长,且在体外细胞实验显示栀子酒萃物和熊果酸也有杀死人类胃癌细胞的能力#28。

保护神经

  腹腔注射100 mg/kg栀子苷于因药物诱发急性帕金森氏症的小鼠持续8天,能有效改善症状,结果发现小鼠的运动迟缓和平衡问题减少、移动和探索活动增加,而在后续实验也证实,栀子苷能重建TH-positive多巴胺神经元(tyrosine hydroxylase(TH)positive dopaminergic neuron),并促进生长因子Bax讯息传递、减少凋亡因子Bcl-2表现#29。

舒缓皮肤过敏

  因尘螨诱发皮肤过敏的小鼠,在涂抹栀子乙酸乙酯萃取物后,可减少过敏症状,并阻止发炎细胞反应、减少血液中IgG和组织胺浓度,同时降低发炎因子和黏附分子(adhesion molecules)表现。再将萃取物做成分分析,发现栀子苷可抑制肥大细胞释放组织胺,但藏花素无效,因此栀子苷具有开发治疗皮肤过敏用药的潜力。#30

可能风险

  24.3 mg/kg剂量以上的栀子苷会使大鼠肝脏承受氧化压力产生急性肝毒性#31-32。京尼平在枯草菌重组检定(rec-assay)和姊妹染色体交换(sister chromatid exchange)试验显示具有基因毒性,可能损伤DNA#33。

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