Serine Protease Inhibitors and Activators From Dalbergia Tonkinensis Species
Serine Protease Inhibitors and Activators From Dalbergia Tonkinensis Species
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东京黄檀物种的丝氨酸蛋白酶抑制剂和激活剂
DOI：
10.1007/s11418-019-01347-y
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发表时间：
2020
期刊：
影响因子：
--
通讯作者：
Fukuyama Y
中科院分区：
文献类型：
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作者：
Son N;Suenaga M;Matsunaga Y;Chinh L;Kubo M;Harada K;Cuong N;Fukuyama Y
脆弱的黄檀是越南的稀有物种。在生物活性植物的研究过程中，我们进行了丝氨酸蛋白酶的筛选。结果表明，在25 ~ 250 ng/mL浓度下，叶根甲醇提取物、根乙醇提取物及其二氯甲烷组分、心木水煎提取物均可作为刺激胰蛋白酶活性的有效来源。此外，叶和茎皮的水煎提取物可能解释未知的民族药理学，因为在使用胰蛋白酶，凝乳胰蛋白酶和弹性酶的酶测定中具有高抑制作用。在23个分离化合物和2个半合成衍生物中，槲皮素（17）抑制胰蛋白酶和凝乳胰蛋白酶活性的IC509.7µM。黄酮类化合物被分类为黄酮、异黄酮、黄酮类、异黄酮类、前棕榈碱类、金酮类和新黄酮类，它们具有不同的活性。一些取代与蛋白酶的作用密切相关，包括黄酮中C-3和C-3′和异黄酮中C-5和C-3′的羟基化，黄酮中C-3、C-5和C-3′的羟基化，C-6和C-8的羧基化和7取代；异黄酮中C-3′的7-取代和甲氧基化新黄酮中的内酯环开口。在酪蛋白裂解评估中，25 ng/mL剂量下，叶水煎提物对胰蛋白酶裂解酪蛋白有抑制作用，而乙醇和甲醇提取物对胰蛋白酶裂解酪蛋白有激活作用。
The vulnerable plantDalbergia tonkinensisPrain is a rare species in Vietnam. In the course of our studies on biologically active plants, we performed serine protease enzyme screenings. The results suggest that at concentrations of 25–250 ng/mL, methanol extracts of leaf and root, root ethanol extract and its dichloromethane fraction, and heartwood water decoction extract can serve as useful sources to stimulate trypsin enzyme activity. In addition, water decoction extracts of leaf and stem bark may explain unknown ethno-pharmacology due to the high inhibitory effects in enzyme assays using trypsin, chymotrypsin, and elastase. Among 23 isolated compounds and two semi-synthetic derivatives tested, quercetin (17) inhibits the activities of trypsin and chymotrypsin with IC509.7 µM. Flavonoids categorized as flavanone, isoflavanone, flavone, isoflavone, pretocarpan, aurone, and neoflavanone demonstrated variable activities. Several substitutions are closely correlated with protease actions, including hydroxylation at C-3 and C-3′ in flavone and C-5 and C-3′ in isoflavone, hydroxylation at C-3, C-5 and C-3′, carboxylation at C-6 and C-8, and 7-substitution in flavanone; 7-substitution and methoxylation at C-3′ in isoflavanone; and lactone ring opening in neoflavanone. In the assessment of casein cleavage, at a dose of 25 ng/mL, leaf water decoction extract demonstrates an inhibitory effect on casein cleavage by trypsin, whereas ethanol and methanol extracts of the root caused activation.