Bonaterra Gabriel Alejandro, Kelber Olaf, Weiser Dieter, Metz Jürgen, Kinscherf Ralf
Centre for Biomedicine and Biomedical Technology Mannheim, University of Heidelberg, Mannheim, Germany.
Arzneimittelforschung. 2010;60(6):330-5. doi: 10.1055/s-0031-1296296.
The well-known anti-inflammatory and analgesic effects of the phytopharmacon willow bark extract have been attributed to the content of salicin; however, pharmacological studies have shown that salicin alone, despite being involved in its therapeutic action, cannot fully explain its clinical efficacy. In addition to reducing inflammation and pain, acetylsalicylic acid (ASA, CAS 50-78-2), like other synthetic non-steroidal anti-inflammatory drugs (NSAIDs), has been shown to exert anti-proliferative effects and to induce apoptosis in a variety of cell lines, e.g., colon, stomach, and prostate cancer cells. To investigate the mechanism of action and possible anti-proliferative and proapoptotic effects of willow bark, a water extract (STW 33-I) and a polyphenol rich fraction (fraction E) have been tested by using the colon-carcinoma cell line HT-29. Both, STW 33-I and its fraction E showed significant anti-proliferative and (1) Introduction The most well-known component of willow bark extract is salicin, which is metabolized in vivo to salicylic acid. The standardized aqueous willow bark extract STW 33-I, which is an effective analgesic and anti-inflammatory drug, contains 23-26% total salicin derivatives and additionally flavonoids, condensed tannins and polyphenols. Typical representatives of the flavonoids are glycosides of naringenin, isosalipurpuroside or eriodictyol. In vitro experiments have demonstrated for pro-apoptotic effects on HT-29 cancer cells. Related to the salicin content of the willow bark extract, a higher dosage of ASA was needed. Furthermore, compared to ASA and to diclofenac (Diclo, CAS 15307-79-6), the COX-1 and COX-2 mRNA expressions were influenced differently by STW 33-I and fraction E. ASA and Diclo inhibited both the COX-1 and COX-2 mRNA expressions, whereas STW 33-I and its fraction E increased the COX-1 mRNA expression. In addition to the already well-known anti-inflammatory and analgesic effects, willow bark extract has been found to possess anti-proliferative and pro-apoptotic effects similar to NSAIDs. The different influence of willow bark on the COX-1 and COX-2 mRNA expressions in comparison to NSAIDs might be relevant, e.g., for prevention of undesirable side effects such as gastric erosions.
植物药柳树皮提取物具有抗炎和镇痛作用，这一作用通常归因于其所含的水杨苷；然而，药理学研究表明，尽管水杨苷参与了其治疗作用，但仅靠它并不能完全解释其临床疗效。除了减轻炎症和疼痛外，乙酰水杨酸（ASA，CAS 50-78-2）与其他合成非甾体抗炎药（NSAIDs）一样，已被证明在多种细胞系中具有抗增殖作用并能诱导凋亡，例如结肠、胃和前列腺癌细胞。为了研究柳树皮的作用机制以及可能的抗增殖和促凋亡作用，采用结肠癌细胞系HT-29对柳树皮水提取物（STW 33-I）和富含多酚的组分（组分E）进行了测试。STW 33-I及其组分E均显示出显著的抗增殖和（1）引言柳树皮提取物最著名的成分是水杨苷，它在体内代谢为水杨酸。标准化的柳树皮水提取物STW 33-I是一种有效的镇痛和抗炎药物，含有23%-26%的总水杨苷衍生物，此外还含有黄酮类、缩合单宁和多酚。黄酮类的典型代表是柚皮苷、异水苏苷或圣草酚的糖苷。体外实验已证明其对HT-29癌细胞有促凋亡作用。与柳树皮提取物中的水杨苷含量相关，需要更高剂量的ASA。此外，与ASA和双氯芬酸（Diclo，CAS 15307-79-6）相比，STW 33-I和组分E对COX-1和COX-2 mRNA表达的影响不同。ASA和双氯芬酸均抑制COX-1和COX-2 mRNA表达，而STW 33-I及其组分E则增加COX-1 mRNA表达。除了已为人熟知的抗炎和镇痛作用外，柳树皮提取物还被发现具有与NSAIDs类似的抗增殖和促凋亡作用。柳树皮与NSAIDs相比，对COX-1和COX-2 mRNA表达的不同影响可能与预防不良副作用（如胃糜烂）有关。
