Novel antitumor activities of Kushen flavonoids In Vitro and In Vivo

Abstract

Kushen (KS), the dried roots of Sophora flavescens Aiton, has a long history of use in traditional Chinese medicine to treat inflammatory diseases and cancer. Kushen alkaloids (KS-As) and Kushen flavonoids (KS-Fs) are the well characterized components in KS. KS-As have been considered biologically active and developed in China as anticancer drugs. In an effort to screen novel antitumor agents from botanicals, more potent antitumor activities were identified in KS-Fs than in KS-As. KS-Fs were able to inhibit the growth of a panel of tumor cell lines and enhanced the antitumor activities of Taxol in vitro. The antitumor activities of KS-Fs and Kur, a single KS-Fs compound, were demonstrated in murine and xenograft human tumor models. Further, it was shown that KS-Fs and Kur were able to enhance the effect of Taxol to inhibit the growth of H460 and Eca-109 xenograft tumors. In addition, peripheral blood cell counts were not significantly affected in normal mice treated with KS-Fs at 200 mg/kg/day for 2 weeks. These results suggest that KS-Fs may be developed as novel antitumor agents and that the currently marketed KS-As drugs in China may have missed the major antitumor activities in Kushen.

Dimeric Matrine-Type Alkaloids from the Roots of Sophora flavescens and Their Anti-Hepatitis B Virus Activities

“…Thus, the structure of 3 was established and named as flavesine C. Thus, compound 4 was identified and named as flavesine D. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 at C-13′ and C-14′, as well as the presence of methylene (δ C 20.3) and methine (δ C 45. 6) carbons. These differences suggested that the double bond was reduced in 5, which was confirmed by the 1 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 In addition, the other two known compounds were identified as matrine …”

“…1,2 The modern pharmacological studies showed that the extracts of S. flavescens displayed the anti-virus, anti-fungi, anti-inflammation, and anti-tumor effects. [3][4][5][6] Phytochemical investigations suggested that matrine-type alkaloids and flavonoids were the main components of this plant. [7][8][9][10][11][12][13][14][15] More than forty matrine-type alkaloids had been isolated from Sophora plants since 1895.…”

Two new eudesmane-type glucopyranosides from the fruits ofDaucus carotaL.

“…Taxol was used as a standard in the cytotoxic assay (Wani & Horwitz 2014) and its IC 50 value is 0.20 mM. Compound 1 and 2 exhibited moderate cytotoxicity against human ECA-109 (Sun et al 2007) compared with report and gave IC 50 values of 23.22 and 26.76 mM, respectively.…”

Inhibitory effect of norcantharidin on melanoma tumor growth and vasculogenic mimicry by suppressing MMP-2 expression

“…Thus, it is important to develop new angiogenic inhibitors that target tumor VM or to combine anti-VM drugs with conventional chemotherapies. Traditional Chinese medicines are reported to have multifunctional antitumor activities (10). …”