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因为黄连素对绿脓杆菌几乎无效,不宜单独作为烧伤用药,而且单味黄连素易产生抗药性(特别是对痢疾杆菌、金黄色葡萄球菌、溶血性链球菌等),故常要求配成复方。文献报道(江苏新医学院:中药大辞典,上册,763页,1977),原儿茶酸对痢疾杆菌、大肠杆菌、金黄色葡萄球菌和绿脓杆菌均有抑制作用,抑菌浓度0.1～0.15%,其2%水溶液 pH 约为3,若调节至近中性,则两个相邻酸羟基易氧化而变色,同时它的水溶液能使创面及皮肤染成棕黑色。为克服上两种药物的缺点,我们将黄连素和原儿茶酸化合成盐,制成一种药物前体(prodrug)——味儿茶酸黄连素,并对它作了抑菌试验,现报道如下。
Because berberine is almost ineffective against Pseudomonas aeruginosa, it should not be used alone as a burn drug, and single-flavor berberine is easy to produce drug resistance (especially for Shigella, Staphylococcus aureus, hemolytic streptococcus, etc.), so it is often required to be compounded. Literature reports (Jiangsu New Medical College: Dictionary of Traditional Chinese Medicine, Volume 1, 763, 1977). Protocatechuic acid has inhibitory effects on Shigella, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The antibacterial concentration is 0.1 to 0.15%. The 2% aqueous solution has a pH of about 3. If it is adjusted to near neutrality, the two adjacent acid hydroxyl groups are easily oxidized and discolored. At the same time, the aqueous solution can dye the wound surface and skin brownish-black. In order to overcome the shortcomings of the above two drugs, we synthesized berberine and protocatechuic acid to form a drug prodrug, flavonol berberine, and it was tested for antibacterial activity. The report is as follows.