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Epstein–Barr Virus and Treatment of Its Infection
Published in Satya Prakash Gupta, Cancer-Causing Viruses and Their Inhibitors, 2014
Tarun Jha, Amit Kumar Halder, Nilanjan Adhikari
Forty-nine multiflorane-type triterpenoids consisting of 11 compounds were isolated from the seeds of Trichosanthes kirilowii (Akihisa et al. 2001), and 38 of their derivatives were evaluated for their inhibitory effects on EBV-EA activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. These tested compounds showed variable inhibitory effects against EBV-EA activation, and 5-dehydrokarounidiol (48, Figure 6.8) exhibited activity with potencies either comparable to or stronger than that of glycyrrhetic acid (a well-known natural antitumor promoter). The structure–activity relationship (SAR) study suggested that C-3 hydroxyl group (Figure 6.8) is essential for activity because acetylation or benzoylation reduced the potency of the compound. Moreover, the 3-oxo derivatives also showed lower activity. Unsaturation in the phenyl ring system was found to be conducive. The presence of the oxo group at both or either of C-7 and C-11 as well as the Δ8 compound reduced the activity. Furthermore, esterification with a bulky benzoyl group of the hydroxymethylene moiety greatly reduced the potency.
The Ethanolic Extract of Trichosanthes Kirilowii Root Exerts anti-Cancer Effects in Human Non-Small Cell Lung Cancer Cells Resistant to EGFR TKI
Published in Nutrition and Cancer, 2022
The root of Trichosanthes kirilowii (TK) has been traditionally used in Oriental medicine for the treatment of dry cough, asthma, sputum, sore throat, and diabetes symptoms including thirst [22,23]. Pharmacological studies have reported that the crude extract of TK root or its constituents exhibit anti-inflammatory, antibacterial, antiviral, and antitumor activities [22–28]. Based on its traditional therapeutic action against lung diseases and the reported pharmacological activities, we hypothesized that the ethanolic extract of the TK root (ETK) has potential anticancer effects in lung cancer. Previous studies demonstrated that ETK suppressed cell proliferation and induced apoptosis in NSCLC cells, supporting our hypothesis [22, 28]. However, the role of ETK in the treatment of NSCLC with EGFR TKI resistance has yet to be reported. In the current study, we investigated whether ETK exhibits anticancer effects in EGFR TKI-resistant NSCLC cells and explored the underlying mechanisms.
TKP, a Serine Protease from Trichosanthes kirilowii, Inhibits Cell Proliferation by Blocking Aerobic Glycolysis in Hepatocellular Carcinoma Cells
Published in Nutrition and Cancer, 2022
Hepatocellular carcinoma (HCC) is the most common primary liver cancer (1). Although there are a lot of treatments for HCC available, the survival rate of HCC patients is still low (3). Thence, it is urgent for the development of novel agents displaying effective antitumor activity. In recent years, plants have become a hot spot for anti-tumor research and many anticancer natural products have been discovered (4, 30). Plant Trichosanthes kirilowii is a good potential target for anticancer drug discovery. It has been reported that some bioactive components extracted from T. kirilowii can effectively inhibit tumor growth (11–14). TKP is an anti-tumor active protein extracted from the fruit of T. kirilowii. Previous studies have demonstrated that TKP can induce the apoptosis and inhibit epithelial-mesenchymal transition in colorectal cancer cells (15, 16). In this study, we found that TKP significantly suppressed Bel-7402 and HepG2 cell survival and colony formation capacity. Furthermore, TKP restrained aerobic glycolysis via targeting PKM2 in Bel-7402 and HepG2 cells. Further studies revealed that β-catenin/c-Myc/HnRNPA1 pathway was involved in TKP-induced inhibitory effects on PKM2.
Gualou Guizhi decoction reverses brain damage with cerebral ischemic stroke, multi-component directed multi-target to screen calcium-overload inhibitors using combination of molecular docking and protein–protein docking
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Juan Hu, Wen-Sheng Pang, Jing Han, Kuan Zhang, Ji-Zhou Zhang, Li-Dian Chen
Medicinal slices of TCM material, the root of Trichosanthes kirilowii Maxim. (Tianhuafen), Cinnamomum cassia Presl (Guizhi), Paeonia lactiflora Pall. (Baishao), Zingiber officinale Rose. (Ganjiang), Glycyrrhiz uralensis Fisch. (Gancao), and ZiziPhus jujuba Mill. (Dazao), were purchased from Fujian Xiang’an Pharmaceutical Co., Ltd. (Quanzhou, China). Herbal remedies accorded with the 2015 edition Chinese pharmacopoeia standard after testing13. Six Chinese medicines sliced mixture in prescription proportion was crushed to powder (60 smash), added six times cold-water to soak in 30 min and let it simmer 30 min, strain the medicine juice through a piece of gauze, every boil the volume of decoction about be 150 ml; repeat again. The first filtrate was merged with the second filtrate, was concentrated in a rotary evaporator until the liquid has reduced to 120 ml.