Northeast Asia Research Institute of Traditional Chinese Medicine, Changchun University of Chinese Medicine, Changchun 130117, China.
Molecules. 2023 Oct 9;28(19):7001. doi: 10.3390/molecules28197001.
The enzymatic transformation of the sugar moiety of the gypenosides provides a new way to obtain more pharmacologically active components. A gene encoding a family 1 glycosyl hydrolase from was cloned and expressed in . The recombinant enzyme was purified, and its molecular weight was approximately 44 kDa. The recombinant BdbglB exhibited an optimal activity at 35 °C and pH 5.4. The purified recombinant enzyme, exhibiting β-glucosidase activity, was used to produce gypenoside XVII (Gyp XVII) via highly selective and efficient hydrolysis of the outer glucose moiety linked to the C-3 position in ginsenoside Rb1 (G-Rb1). Under the optimal reaction conditions for large scale production of gypenoside XVII, 40 g ginsenoside Rb1 was transformed by using 45 g crude enzyme at pH 5.4 and 35 °C for 10 h with a molar yield of 100%. Furthermore, the anti-inflammatory effects of the product gypenoside XVII and its conversion precursor ginsenoside Rb1 were evaluated by using lipopolysaccharide (LPS)-induced murine RAW 264.7 macrophages and the xylene-induced acute inflammation model of mouse ear edema, respectively. Gypenoside XVII showed improved anti-inflammatory activity, which significantly inhibited the generation of TNF-α and IL-6 more effectively than its precursor ginsenoside Rb1. In addition, the swelling inhibition rate of gypenoside XVII was 80.55%, while the rate of its precursor was 40.47%, the results also indicated that gypenoside XVII had better anti-inflammatory activity than ginsenoside Rb1. Hence, this enzymatic method would be useful in the large-scale production of gypenoside XVII, which may become a new potent anti-inflammatory candidate drug.
糖基的酶促转化为绞股蓝皂苷提供了获得更多具有药理活性成分的新方法。从 克隆并在 中表达了一个编码家族 1 糖苷水解酶的基因。重组酶被纯化，其分子量约为 44 kDa。重组 BdbglB 在 35°C 和 pH 5.4 下表现出最佳活性。纯化的重组酶具有β-葡萄糖苷酶活性，可通过高度选择性和高效水解人参皂苷 Rb1（G-Rb1）C-3 位连接的外葡萄糖基来生产绞股蓝皂苷 XVII（Gyp XVII）。在大规模生产绞股蓝皂苷 XVII 的最佳反应条件下，在 pH 5.4 和 35°C 下，使用 45 g 粗酶在 10 h 内将 40 g 人参皂苷 Rb1 转化，摩尔收率为 100%。此外，通过使用脂多糖（LPS）诱导的鼠 RAW 264.7 巨噬细胞和二甲苯诱导的小鼠耳肿胀急性炎症模型，分别评估了产物绞股蓝皂苷 XVII及其转化前体人参皂苷 Rb1 的抗炎作用。绞股蓝皂苷 XVII 显示出改善的抗炎活性，其对 TNF-α和 IL-6 的生成的抑制作用明显优于其前体人参皂苷 Rb1。此外，绞股蓝皂苷 XVII 的肿胀抑制率为 80.55%，而其前体的抑制率为 40.47%，结果表明绞股蓝皂苷 XVII 比人参皂苷 Rb1 具有更好的抗炎活性。因此，这种酶促方法将有助于大规模生产绞股蓝皂苷 XVII，它可能成为一种新的有效的抗炎候选药物。
