Kwak Hee Jae, Park SeonJu, Kim Nanyoung, Yoo Guijae, Park Jun Hyung, Oh Youngse, Nhiem Nguyen Xuan, Kim Seung Hyun
a College of Pharmacy , Yonsei Institute of Pharmaceutical Sciences, Yonsei University , Incheon , Korea.
b Institute of Marine Biochemistry , Vietnam Academy of Science and Technology , Hanoi , Vietnam.
Nat Prod Res. 2018 Sep;32(17):2111-2115. doi: 10.1080/14786419.2017.1365067. Epub 2017 Aug 17.
Rhinacanthus nasutus (L.) Kurz (Acanthaceae) is known as traditional medicine for the treatment of various diseases, such as cancer, fungal infections, herpes virus infections and several types of skin diseases in South-East Asian countries. In this study, eight compounds 1-8 were isolated from the aerial parts of R. nasutus. The structures of compounds were determined by the spectroscopic methods, including 1D and 2D NMR. The isolated compounds were evaluated for neuraminidase inhibitory activity. Several lignans, 2,3-bis[(4-hydroxy-3,5-dimethoxyphenyl)methyl]-1,4-butanediol (5) and 8,8'-bisdihydrosiringenin glucoside (6), significantly inhibited neuraminidase activity, which was comparable to the positive controls, mangiferin and oseltamivir. In addition, a structure-based virtual screening against neuraminidase using bioactive components was demonstrated.
长穗爵床（Rhinacanthus nasutus (L.) Kurz，爵床科）在东南亚国家作为治疗多种疾病的传统药物，如癌症、真菌感染、疱疹病毒感染和几种皮肤病。在本研究中，从长穗爵床地上部分分离出8种化合物1 - 8。通过包括一维和二维核磁共振在内的光谱方法确定了化合物的结构。对分离出的化合物进行了神经氨酸酶抑制活性评估。几种木脂素，2,3 - 双[(4 - 羟基 - 3,5 - 二甲氧基苯基)甲基] - 1,4 - 丁二醇（5）和8,8'- 双二氢水苏素葡萄糖苷（6），显著抑制神经氨酸酶活性，与阳性对照芒果苷和奥司他韦相当。此外，还展示了使用生物活性成分对神经氨酸酶进行基于结构的虚拟筛选。
