Moretó M, Goñalons E, Mylonakis N, Giráldez A, Torralba A
Arzneimittelforschung. 1979;29(10):1561-4.
The disodium salt of the sulphuric diester of 3,3-bis-(4-hydroxyphenyl)-7-methyl-2-indolinone (sodium sulisatin, Laxitex), a synthetic laxative with two phenolic groups esterified with sulfate, has been studied in order to find out if its laxative properties may be attributed to the unaltered compound or to its diphenolic derivative BHMI. We first studied the effect of homogenates of the gastrointestinal tract of rats and of rat cecal content of the hydrolysis of sulfate ester bonds of sulisatin. Results show that sulisatin can be hydrolyzed by cecal content while homogenates of stomach, small intestine and large intestine have no hydrolytic effect. Sulisatin is also a substrate of arylsulfate sulphohydrolase obtained from the snail Helix pomatia. The unaltered drug has no effect on the intestinal motility since it does not change the intestinal transit speed in rats pretreated with neomycin sulfate. Sulisatin (1.5, 3 and 6 mg) is unable to inhibit water absorption in rat colon while small amounts of BHMI (15 and 30 micrograms) may inhibit it significantly. It is concluded that sulisatin passes unaltered through the small intestine and is hydrolyzed in the large intestine by the intestinal microflora to its diphenolic derivative BHMI, which is responsible for the laxative activity of the drug.
3,3 - 双 -（4 - 羟苯基）- 7 - 甲基 - 2 - 吲哚酮硫酸二酯的二钠盐（舒立酸二钠，Laxitex）是一种合成泻药，其两个酚羟基被硫酸酯化。为了确定其泻下特性是归因于未改变的化合物还是其双酚衍生物BHMI，我们进行了研究。我们首先研究了大鼠胃肠道匀浆以及大鼠盲肠内容物对舒立酸硫酸酯键的水解作用。结果表明，舒立酸可被盲肠内容物水解，而胃、小肠和大肠的匀浆没有水解作用。舒立酸也是从蜗牛Helix pomatia获得的芳基硫酸酯硫酸水解酶的底物。未改变的药物对肠道运动没有影响，因为它不会改变用硫酸新霉素预处理的大鼠的肠道转运速度。舒立酸（1.5、3和6毫克）不能抑制大鼠结肠对水的吸收，而少量的BHMI（15和30微克）可能会显著抑制它。结论是，舒立酸未经改变地通过小肠，并在大肠中被肠道微生物群水解为其双酚衍生物BHMI，后者是该药物泻下活性的原因。
