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Numerous antitumor drugs exhibited excellent anti-proliferation activities, discovered from natural products. Oridonin is isolated from a traditional Chinese medicine Isodon rubescens, and it exhibit various biological functions including anticancer, anti-inflammation, antibacterial, and so on. The anticancer mechanisms of oridonin include apoptosis, autophagy, cell cycle arrest, and so on. However, clinical research and application of oridonin has been hampered, due to the poor pharmaceutical property. So many studies on oridonin have been explored in the purpose of improve the pharmaceutical property, including investigation of the mechanism of action in depth and structural modification. In this review, we summarized oridonin and oridonin derivatives as potential anticancer agents, and detailed discussion on biological properties, mechanism of actions and potential for overcoming therapeutic resistance. [ABSTRACT FROM AUTHOR]

Background: The Hippo pathway is widely considered to inhibit cell growth and play an important role in regulating the size of organs. However, recent studies have shown that abnormal regulation of the Hippo pathway can also affect tumor invasion and metastasis. Therefore, finding out how the Hippo pathway promotes tumor development by regulating the expression of target genes provides new ideas for future research on targeted drugs that inhibit tumor progression. Methods: PubMed, Embase, Web of Science, and the Cochrane Library were systematically searched. Results: The search strategy identified 1892 hits and 196 publications were finally included in this review. As the core molecule of the Hippo pathway, YAP/TAZ are usually highly expressed in tumors that undergo invasion and migration and are accompanied by abnormally strong nuclear metastasis. Through its interaction with nuclear transcription factors TEADs, it directly or indirectly regulates and the expressions of target genes related to tumor metastasis and invasion. These target genes can induce the formation of invasive pseudopodia in tumor cells, reduce intercellular adhesion, degrade extracellular matrix (ECM), and cause epithelial-mesenchymal transition (EMT), or indirectly promote through other signaling pathways, such as mitogen-activated protein kinases (MAPK), TGF/Smad, etc, which facilitate the invasion and metastasis of tumors. Conclusion: This article mainly introduces the research progress of YAP/TAZ which are the core molecules of the Hippo pathway regulating related target genes to promote tumor invasion and metastasis. Focus on the target genes that affect tumor invasion and metastasis, providing the possibility for the selection of clinical drug treatment targets, to provide some help for a more in-depth study of tumor invasion and migration mechanism and the development of clinical drugs. [ABSTRACT FROM AUTHOR]

We have evaluated the antiproliferative activity of (E)-3-(3,5-difluorophenyl)-1-(2,4,6-trimethoxyphenyl)- prop-2-en-1-one (chalcone 5) against MGC-803 cells. This chalcone analog displayed a potent antiproliferative activity with an IC50 value of 0.23 μM against MGC-803 cells. It could induce apoptosis and regulate the apoptosis-related markers (Bax, Bcl-2, Bcl-xl, and Bid) in a concentration dependent manner. Treatment with NAC almost completely attenuated chalcone-induced cell inhibition and cell apoptosis in MGC-803 cells, indicating that the apoptotic mechanisms were related to ROS generation. Therefore, this chalcone derivative is a new apoptosis inducer for prevention and treatment of gastric cancer. [ABSTRACT FROM AUTHOR]

(E)-3-(3-(Allyloxy)-2-methoxyphenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one displayed potent antiproliferative activity against the PC-3 cell line. For colony assay, it can inhibit the colony formation at a concentration of 10 μM. Morphological changes of PC-3 cells were determined using DAPI (4′,6-diamidino-2-phenylindole) staining and chromatin condensation. Treatment with this compound at 10 μM induced apoptosis from 2.0% to 30.4% compared with control according to flow cytometry analysis. It also induced the downregulation of apoptosis-related markers Bcl-2 and XIAP (X-linked inhibitor of apoptosis protein). However, treatment with NAC (N-acetyl-L-cysteine) almost completely attenuated chalcone-induced cell inhibition and cell apoptosis in PC-3 cells. [ABSTRACT FROM AUTHOR]

Abstract : Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate ( 8a) showed the most potent inhibitory activity with an $$\hbox {IC}_{50}$$ value of $$11.59\,\upmu \hbox {M}$$ against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers. Graphical Abstract: [ABSTRACT FROM AUTHOR]

A series of novel coumarin derivatives were synthesized from commercially available chemical agents. All prepared compounds were evaluated for their in vitro antiproliferative activity against five selected human cancer cell lines (EC109, MGC-803, PC-3, MCF-7, and EC9706) and their in vitro antimicrobial activity against E. coli and M. albicans. 4-(3-Bromopropoxy)-2 H-chromen-2-one exhibited the highest growth inhibition against MGC-803 cell line (IC 47.7 μM) and 7-(2-bromoethoxy)-2 H-chromen-2-one exhibited the highest growth inhibition against MCF-7 cell line (IC 48.3 μM). The latter compound was also the most active against E. coli (MIC 0.27 μg/ml). [ABSTRACT FROM AUTHOR]