Anti-tumor activities of active ingredients in Compound Kushen Injection

Abstract

Kushen (Radix Sophorae Flavescentis) has a long history of use for the treatment of tumors, inflammation and other diseases in traditional Chinese medicine. Compound Kushen Injection (CKI) is a mixture of natural compounds extracted from Kushen and Baituling (Rhizoma Smilacis Glabrae). The main principles of CKI are matrine (MT) and oxymatrine (OMT) that exhibit a variety of pharmacological activities, including anti-inflammatory, anti-allergic, anti-viral, anti-fibrotic and cardiovascular protective effects. Recent evidence shows that these compounds also produce anti-cancer actions, such as inhibiting cancer cell proliferation, inducing cell cycle arrest, accelerating apoptosis, restraining angiogenesis, inducing cell differentiation, inhibiting cancer metastasis and invasion, reversing multidrug resistance, and preventing or reducing chemotherapy-and/or radiotherapy-induced toxicity when combined with chemotherapeutic drugs. In this review, we summarize recent progress in studying the anti-cancer activities of MT, OMT and CKI and their potential molecular targets, which provide clues and references for further study.

Understanding the Effectiveness of Natural Compound Mixtures in Cancer through Their Molecular Mode of Action

“…It contains alkaloids, flavonoids, saccharides, and organic acids [82] and is extracted from two medical herbs including Radix Sophorae flavescentis and Rhizoma Smilacis Glabrae [83]. It modulates immunity, decreases inflammation, relieves cancer pain, and, most importantly, has anti-neoplastic activity [83].…”

“…It contains alkaloids, flavonoids, saccharides, and organic acids [82] and is extracted from two medical herbs including Radix Sophorae flavescentis and Rhizoma Smilacis Glabrae [83]. It modulates immunity, decreases inflammation, relieves cancer pain, and, most importantly, has anti-neoplastic activity [83]. For example, CKI downregulates β-catenin through the Wnt signaling pathway, which in turn targets the oncogenes c-MYC and CyclinD1 [84], leading to suppression of MCF-7 cancer stem cell-like side population (SP) cells [85].…”

“…The primary effect of CKI on cancer cells is through the cell cycle, but it also affects many other pathways and it may be useful as both an anticancer and anti-inflammatory agent. It was claimed that CKI is effective in inhibiting metastasis and reversing multi-drug resistance (MDR) as well [83]. Yet, there is currently no research evidence supporting the effectiveness of CKI on reversing MDR in English-language journals.…”

Meta-Analysis of Randomized Controlled Trial in Treating Primary Liver Cancer by Fufang Kushen Injection Combined with TACE

“…In recent years, transarterial chemoembolization (TACE) is one of the preferred treatments for patients with PLC who are not suitable for surgery or postoperative recurrence. FFKS was extracted from the mixture of Sophora flavescens and Heterosmilacis Japonicae with the mass ratio of 7 than 3, Experimental studies showed that FFKS could inhibit tumor cell growth, alleviate pain, elevated white blood cell, anti-infection and protect the body immune function [2,3].Until now, Many clinical trials showed that FFKS-TACE can reduce the adverse reactions and improve quality of life for primary liver cancer (PLC). however, a multi-center, randomized, double-blind PlaceboControlled Trial of FFKS-TACE for Treatment of PLC have not been reported.…”

Fangjiomics: revealing adaptive omics pharmacological mechanisms of the myriad combination therapies to achieve personalized medicine

“…PBCRBS could ameliorate neurological function deficits, reduce volume of hematoma and volume of perihematomal edema, and lower mortality rate and dependency in comparison with Western conventional medication controls or placebo based on a Meta-analysis [8] . Wang et al summarized the recent investigations on the anticancer activities and possible molecular targets of the Compound Kusen Injection, and then hypothesized that altering gene regulation in several pathways including Wnt signaling pathway might be involved in the underlying mechanisms [9] . To summarize the targets distribution of Fangjis, Liu and Wang defined multiple modes of array-designed combination therapies of Fangjiomics, such as "magic shotguns", vertical, horizontal, focusing, siege and dynamic arrays according to hits on targets, pathways or networks [10] .…”