Li Rui-yu, Feng Wu-wen, Li Xiao-fei, Zhang Ding-kun, Li Chun-yu, Meng Ya-kun, Bai Zhao-fang, Song Hai-bo, Du Xiao-xi, Xia Hou-lin, Wang Jia-bo, Xiao Xiao-he
Yao Xue Xue Bao. 2016 Jan;51(1):116-21.
Decoction is one of the most commonly used dosage forms of traditional Chinese medicine. The stability of chemical constituents in decoction is closely related to the clinical efficacy and safety. There were few reports about the influence of metal ions in the stability of chemical constituents in traditional Chinese medicine. However, there is no evidence that metal ions in decoction water need to be controlled. In this study, 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside (THSG), one of the main constituents in Polygoni Multiflori Radix was studied. Ordinary tap water, deionized water, and water containing different metal ions were used to investigate and compare the influence on THSG. The results showed that after storage in a dark place at the room temperature for 10 days, the degradation of THSG was 7% in deionized water, while undetectable in tap water. The content of THSG could be decreased by different kinds of metal ions, and the effect was concentration-dependent. Moreover, Fe3+ and Fe2+ showed the greatest influence at the same concentration; and our study has shown that THSG decreased more than 98% in Fe and Fe2+ solutions at 500 ppm concentration. In the same time we found out p-hydroxybenzaldehyde (molecular weight: 122.036 7) and 2,3,5-trihydroxybenzaldehyde-2-O-glycoside (molecular weight: 316.079 4) were the main degradation products of THSG in tap water and water containing Cu2+, Ca2+, Zn2+, Mg2+ and Al3+. The product of THSG dimer with a water molecule was found in water containing Fe3+ and Fe2+. The above results showed that the metal ions in water could significantly influence the stability of THSG in water, indicating that the clinical efficacy and safety of decoction would be affected if the metal ions in water were not under control. It's suggested that deionized water should be used in the preparation of decoction containing Polygoni Multiflori Radix in the clinic to avoid degradation of THSG. Meanwhile, decoction prepared by tap water should be taken by patients in a short time. Our investigation provides important information and reference about the influence of metal ions on the stability of decoctions in other traditional Chinese medicine that have unstable groups such as hydroxyls and unsaturated bonds, etc.
汤剂是中药最常用的剂型之一。汤剂中化学成分的稳定性与临床疗效和安全性密切相关。关于金属离子对中药化学成分稳定性的影响报道较少。然而,目前尚无证据表明需要控制汤剂水中的金属离子。本研究以何首乌主要成分之一的2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(THSG)为研究对象。采用普通自来水、去离子水以及含有不同金属离子的水来研究并比较对THSG的影响。结果表明,在室温暗处储存10天后,THSG在去离子水中的降解率为7%,而在自来水中未检测到降解。不同种类的金属离子会使THSG含量降低,且呈浓度依赖性。此外,在相同浓度下,Fe3+和Fe2+的影响最大;我们的研究表明,在500 ppm浓度的Fe3+和Fe2+溶液中,THSG的降解率超过98%。同时我们发现,对羟基苯甲醛(分子量:122.036 7)和2,3,5-三羟基苯甲醛-2-O-糖苷(分子量:316.079 4)是THSG在自来水以及含有Cu2+、Ca2+、Zn2+、Mg2+和Al3+的水中的主要降解产物。在含有Fe3+和Fe2+的水中发现了THSG二聚体与一个水分子的产物。上述结果表明,水中的金属离子会显著影响THSG在水中的稳定性,这表明如果水中的金属离子不受控制,汤剂的临床疗效和安全性将受到影响。建议临床制备含何首乌的汤剂时使用去离子水,以避免THSG降解。同时,用自来水制备的汤剂患者应尽快服用。我们的研究为金属离子对其他含有羟基和不饱和键等不稳定基团的中药汤剂稳定性的影响提供了重要信息和参考。