Leachianone A

Leachianone A as a potential anti-cancer drug by induction of apoptosis in human hepatoma HepG2 cells.[Pubmed: 17379399]

Cancer Lett. 2007 Aug 18;253(2):224-35.

The Chinese herbal medicine Radix Sophorae is widely applied as an anti-carcinogenic/ anti-metastatic agent against liver cancer.
METHODS AND RESULTS:
In this study, Leachianone A, isolated from Radix Sophorae, possessed a profound cytotoxic activity against human hepatoma cell line HepG2 in vitro, with an IC(50) value of 3.4microg/ml post-48-h treatment. Its action mechanism via induction of apoptosis involved both extrinsic and intrinsic pathways. Its anti-tumor effect was further demonstrated in vivo by 17-54% reduction of tumor size in HepG2-bearing nude mice, in which no toxicity to the heart and liver tissues was observed.
CONCLUSIONS:
In conclusion, this is the first report describing the isolation of Leachianone A from Radix Sophorae and the molecular mechanism of its anti-proliferative effect on HepG2 cells.

Lavandulyl flavonoids with sodium-dependent glucose cotransporter 2 inhibitory activity from Sophora flavescens.[Reference: WebLink]

Journal of Huazhong Normal University, 2014,  48(4):520-4.

To discover new bioactive Sodium-dependent glucose cotransporter 2(SGLT2)inhibitors from the traditional Chinese medicine"Ku Shen"(roots of Sophora flavescens),the bioassay-guided purification of an active ethyl acetate fraction was performed.
METHODS AND RESULTS:
Sixteen lavandulyl flavonoids were isolated and their structures were elucidated as kushenol H(1),kushenol K(2),kurarinol(3),kushenol Y(4),kushenol P(5),norkurarinone(6),kushenol I(7),kushenol N(8),(-)-kurarinone(9),kushenol X(10),neokurarinol(11),kushenol C(12),sophoraflavanone G(13),Leachianone A(14),kuraridine(15)and kushenol A(16).All isolated compounds exhibited inhibitory activity against SGLT2.Among them,the two main constituents of the active EtOAc fraction,(-)-kurarinone(9)and sophoraflavanone G(13)showed the most potential inhibitory activity against SGLT2with the IC50values of 2.24μmol/L and 1.45μmol/L,respectively.

Inhibitory Effects of Leachianone A from Sophora flavescens Ait. against Cadmium Induced Cytotoxicity.[Reference: WebLink]

Korean J. Oriental Physiology & Pathology,2008, 22(5):1163-7.

In this study, cytotoxicity of cadmium on NIH 3T fibroblasts was utilized in order to discover antitoxic compound in methanol extract of Sophora flavascens Ait.
METHODS AND RESULTS:
There were treatment groups; control (medium only), MTT50 group and five experimental groups. MTT {3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazoliumbromide} assay was performed to evaluate the cytotoxicity of cell organelles and IC50 was also measured. Accordingly we have examined the detoxification effects of methanol extract of S. flavescens Ait. and Leachianone A (LA) on cadmium-treated NIH 3T3 fibroblasts (IC50= 12.5 μM) to observe morphological changes by the light microscopy. Both S. flavescens Ait. methanol extract and LA showed inhibitory effects on cadmium-induced cytotoxicity. Furthermore, LA showed dose-dependency in detoxication.
CONCLUSIONS:
From these results, it is conceivable to suggest that LA from S. flavescens Ait. methanol extract is a potential antitoxic agent.