TCM and Ethnomedicine Innovation & Development International Laboratory, Innovative Drug Research Institute, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China.
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Molecules. 2018 Aug 27;23(9):2147. doi: 10.3390/molecules23092147.
Heilaohu, the roots of has a long history of use in Tujia ethnomedicine for the treatment of rheumatoid arthritis and gastroenteric disorders, and a lot of work has been done in order to know the material basis of its pharmacological activities. The chemical investigation led to the isolation and characterization of three new (⁻) and twenty known (⁻) lignans. Three new heilaohulignans A-C (⁻) and seventeen known (⁻) lignans possessed dibenzocyclooctadiene skeletons. Similarly, one was a diarylbutane () and two were spirobenzofuranoid dibenzocyclooctadiene (⁻) lignans. Among the known compounds, ⁻, , ⁻ and ⁻ were isolated from this species for the first time. The structures were established, using IR, UV, MS and NMR data. The absolute configurations of the new compounds were determined by circular dichroism (CD) spectra. The isolated lignans were further evaluated for their cytotoxicity and antioxidant activities. Compound demonstrated strong cytotoxic activity with an IC value of 9.92 µM, compounds and revealed weak cytotoxicity with IC values of 21.72 µM and 18.72 µM, respectively in the HepG-2 human liver cancer cell line. Compound also showed weak cytotoxicity against the BGC-823 human gastric cancer cell line and the HCT-116 human colon cancer cell line with IC values of 16.75 µM and 16.59 µM, respectively. A chemiluminescence assay for antioxidant status of isolated compounds implied compounds and which showed weak activity with IC values of 25.56 µM and 21.20 µM, respectively.
黑老鸦,其根在土家族民族医学中用于治疗类风湿性关节炎和胃肠疾病已有悠久的历史,为了了解其药理活性的物质基础,已经做了大量的工作。化学研究导致分离和鉴定了三个新的(⁻)和二十个已知的(⁻)木脂素。三个新的黑老鸦木脂素 A-C(⁻)和十七个已知的(⁻)木脂素具有二苯并环辛二烯骨架。同样,一个是二芳基丁烷(),两个是螺苯并呋喃二苯并环辛二烯(⁻)木脂素。在已知的化合物中,⁻、、⁻和⁻首次从该种中分离得到。结构通过红外、紫外、质谱和核磁共振数据确定。新化合物的绝对构型通过圆二色谱(CD)光谱确定。分离得到的木脂素进一步评价了其细胞毒性和抗氧化活性。化合物 表现出较强的细胞毒性,IC 值为 9.92 µM,化合物 和 表现出较弱的细胞毒性,IC 值分别为 21.72 µM 和 18.72 µM,在 HepG-2 人肝癌细胞系中。化合物 对 BGC-823 人胃癌细胞系和 HCT-116 人结肠癌细胞系也表现出较弱的细胞毒性,IC 值分别为 16.75 µM 和 16.59 µM。对分离化合物抗氧化状态的化学发光测定表明,化合物 和 表现出较弱的活性,IC 值分别为 25.56 µM 和 21.20 µM。