Abstract
Pterocephalus hookeri is a widely applied Tibetan medicinal prescription for treatment of diseases such as flu, rheumatoid arthritis, and enteritis in China. It has been reported that Pterocephalus hookeri has anti-inflammatory and analgesic actions. However, the antitumor activity of Pterocephalus hookeri remains unknown. In the present study, we demonstrate that n-butanol extracts of Pterocephalus hookeri (YSC-ZDC) has a strong antitumor activity against hepatoma carcinoma cell in vitro and in vivo. YSC-ZDC inhibited proliferation of all cancer cell lines and significantly inhibited Hep3B cells proliferation in a dose- and time-dependant manner. Transmission electron microscopy, hoechst 33258 staining, and flow cytometry analysis revealed that YSC-ZDC induced apoptosis in Hep3B cells. YSC-ZDC treatment dramatically inhibited PDK1 and Akt phosphorylation in Hep3B cells. Moreover, YSC-ZDC increased Bax expression and inhibited Bcl-2 expression. In addition, YSC-ZDC inhibited growth hepatoma xenografts in vivo with no effect on body weight and spleen index. Consistent with results in vitro, YSC-ZDC increased Bax expression and inhibited Bcl-2 expression in tumor tissue. Taken together, this study shows YSC-ZDC with an antitumor activity both in vitro and in vivo. Its mechanism underlying is related to blocking of the Akt pathway and regulation of Bcl-2 family proteins expression.
Highlights
Hepatocellular carcinoma (HCC) is the fifth most common malignancy worldwide and the third leading cause of mortality in all cancer-related diseases with the highest incidence occurring in eastern and southeastern Asia, middle and western Africa, southern Europe, and South America [1]
The qualitative chemical profile of n-butanol extract was analyzed by high-performance liquid chromatography (HPLC) as described in the Chinese Pharmacopoeia
The HPLC analysis of YSCZDC showed that over 15 peaks were detected within 15 min, among which 5 compounds were identified by comparing individual peak retention times with the standard substances (Figure 1)
Summary
Hepatocellular carcinoma (HCC) is the fifth most common malignancy worldwide and the third leading cause of mortality in all cancer-related diseases with the highest incidence occurring in eastern and southeastern Asia, middle and western Africa, southern Europe, and South America [1]. The overall response to liver cancer treatment is unsatisfactory, mainly due to late diagnosis and poor treatment efficacy; resistance to chemotherapeutic drugs; and metastasis to other organs which negatively affect the mortality rate [2]. New and effective treatment options for liver cancer are urgently needed, supporting the fact that plant-derived natural products occupy an important position in the treatment of diseases due to their minimal side effects and lack of multidrug resistance [3, 4]. As traditional Chinese herbal medicines, have been used to treat a wide variety of clinical diseases in. Pterocephalus hookeri is a popular Tibetan herb, locally known as “Bang-zi-du-wu” in the Tibetan language and recorded in the Tibetan medicine book as “Si-Bu-YiDian” [7]. The effect of Pterocephalus hookeri on antitumor activity remains unknown
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