Maurer H R
Department of Biochemistry, Molecular Biology and Biotechnology, Institute of Pharmacy, Freie Universität Berlin, Germany.
Cell Mol Life Sci. 2001 Aug;58(9):1234-45. doi: 10.1007/PL00000936.
Bromelain is a crude extract from the pineapple that contains, among other components, various closely related proteinases, demonstrating, in vitro and in vivo, antiedematous, antiinflammatory, antithrombotic and fibrinolytic activities. The active factors involved are biochemically characterized only in part. Due to its efficacy after oral administration, its safety and lack of undesired side effects, bromelain has earned growing acceptance and compliance among patients as a phytotherapeutical drug. A wide range of therapeutic benefits has been claimed for bromelain, such as reversible inhibition of platelet aggregation, angina pectoris, bronchitis, sinusitis, surgical traumas, thrombophlebitis, pyelonephritis and enhanced absorption of drugs, particularly of antibiotics. Biochemical experiments indicate that these pharmacological properties depend on the proteolytic activity only partly, suggesting the presence of nonprotein factors in bromelain. Recent results from preclinical and pharmacological studies recommend bromelain as an orally given drug for complementary tumor therapy: bromelain acts as an immunomodulator by raising the impaired immunocytotoxicity of monocytes against tumor cells from patients and by inducing the production of distinct cytokines such as tumor necrosis factor-a, interleukin (Il)-1beta, Il-6, and Il-8. In a recent clinical study with mammary tumor patients, these findings could be partially confirmed. Especially promising are reports on animal experiments claiming an antimetastatic efficacy and inhibition of metastasis-associated platelet aggregation as well as inhibition of growth and invasiveness of tumor cells. Apparently, the antiinvasive activity does not depend on the proteolytic activity. This is also true for bromelain effects on the modulation of immune functions, its potential to eliminate burn debris and to accelerate wound healing. Whether bromelain will gain wide acceptance as a drug that inhibits platelet aggregation, is antimetastatic and facilitates skin debridement, among other indications, will be determined by further clinical trials. The claim that bromelain cannot be effective after oral administration is definitely refuted at this time.
菠萝蛋白酶是从菠萝中提取的粗提物，除其他成分外，还含有多种密切相关的蛋白酶，在体外和体内均表现出抗水肿、抗炎、抗血栓形成和纤维蛋白溶解活性。所涉及的活性因子仅部分得到了生化特性鉴定。由于口服后有效、安全且无不良副作用，菠萝蛋白酶作为一种植物治疗药物在患者中越来越被接受和依从。菠萝蛋白酶具有广泛的治疗益处，如可逆性抑制血小板聚集、治疗心绞痛、支气管炎、鼻窦炎、手术创伤、血栓性静脉炎、肾盂肾炎以及增强药物尤其是抗生素的吸收。生化实验表明，这些药理特性仅部分取决于蛋白水解活性，这表明菠萝蛋白酶中存在非蛋白质因子。临床前和药理学研究的最新结果推荐菠萝蛋白酶作为口服药物用于辅助肿瘤治疗：菠萝蛋白酶通过提高单核细胞对患者肿瘤细胞受损的免疫细胞毒性以及诱导产生不同的细胞因子如肿瘤坏死因子-α、白细胞介素（Il）-1β、Il-6和Il-8来发挥免疫调节作用。在最近一项针对乳腺肿瘤患者的临床研究中，这些发现得到了部分证实。特别有前景的是关于动物实验的报告，称其具有抗转移功效，可抑制与转移相关的血小板聚集以及抑制肿瘤细胞的生长和侵袭性。显然，抗侵袭活性不取决于蛋白水解活性。菠萝蛋白酶对免疫功能调节的作用、清除烧伤碎片和加速伤口愈合的潜力也是如此。菠萝蛋白酶是否会作为一种抑制血小板聚集、具有抗转移作用并有助于皮肤清创等用途的药物而被广泛接受，将由进一步的临床试验来确定。目前，菠萝蛋白酶口服无效的说法已被明确驳斥。
