Design, synthesis and anti-cancer activity evaluation of podophyllotoxin-norcantharidin hybrid drugs

Han, Hongwei; Qiu, Han‐Yue; Hu, Chenyao; Sun, Wenxue; Yang, Rongwu; Qi, Jinliang; Wang, Xiaoming; Lü, Guihua; Yang, Yonghua

doi:10.1016/j.bmcl.2016.05.063

Cited by 23 publications

(8 citation statements)

References 26 publications

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“…In addition, PTOX may affect other signaling pathways to trigger cell apoptosis. Han et al (2016) synthesized PTOX-norcantharidin hybrids Compound 42 ( Figure 10 ), which showed low cytotoxicity against normal human embryonic kidney cells (293T) and induced cell cycle G2/M arrest and apoptosis in MCF-7 cancer cells. In terms of molecular mechanisms, the results showed an upregulation of the expression of the cell cycle-related protein CDK1 and downregulation of the expression of cyclin B1, a protein required for mitotic initiation.…”

Section: Mechanism Of Ptox Derivatives As An Anticancer Drugmentioning

confidence: 99%

Insight Into the Molecular Mechanism of Podophyllotoxin Derivatives as Anticancer Drugs

Fan

Zhu

Xian

et al. 2021

Front. Cell Dev. Biol.

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Podophyllotoxin (PTOX) is a biologically active compound derived from the podophyllum plant, and both it and its derivatives possess excellent antitumor activity. The PTOX derivatives etoposide (VP-16) and teniposide (VM-26) have been approved by the U.S. Food and Drug Administration (FDA) for cancer treatment, but are far from perfect. Hence, numerous PTOX derivatives have been developed to address the major limitations of PTOX, such as systemic toxicity, drug resistance, and low bioavailability. Regarding their anticancer mechanism, extensive studies have revealed that PTOX derivatives can induce cell cycle G2/M arrest and DNA/RNA breaks by targeting tubulin and topoisomerase II, respectively. However, few studies are dedicated to exploring the interactions between PTOX derivatives and downstream cancer-related signaling pathways, which is reasonably important for gaining insight into the role of PTOX. This review provides a comprehensive analysis of the role of PTOX derivatives in the biological behavior of tumors and potential molecular signaling pathways, aiming to help researchers design and develop better PTOX derivatives.

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Section: Mechanism Of Ptox Derivatives As An Anticancer Drugmentioning

confidence: 99%

Insight Into the Molecular Mechanism of Podophyllotoxin Derivatives as Anticancer Drugs

Fan

Zhu

Xian

et al. 2021

Front. Cell Dev. Biol.

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“…Moreover, compound 20 induced apoptosis in A549 cells and prevented the transition of these cells from the S phase to the G2 phase; however, it had no significant effect on L02 cells. Han et al ( 2016 ) screened an effective podophyllotoxin derivative, namely 21 (IC 50 in MCF-7 cell line = 0.9 μM), with low cytotoxicity to non-cancer cells, including human embryonic kidney cells (293T) (IC 50 = 54.4 μM). Additionally, this derivative can cause a significant cell cycle arrest at the G2/M phase and induce MCF-7 cell apoptosis more than PPT.…”

Section: Application Of Amino Acids In the Structural Modification Of Natural Productsmentioning

confidence: 99%

Application of Amino Acids in the Structural Modification of Natural Products: A Review

Deng

et al. 2021

Front. Chem.

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Natural products and their derivatives are important sources for drug discovery; however, they usually have poor solubility and low activity and require structural modification. Amino acids are highly soluble in water and have a wide range of activities. The introduction of amino acids into natural products is expected to improve the performance of these products and minimize their adverse effects. Therefore, this review summarizes the application of amino acids in the structural modification of natural products and provides a theoretical basis for the structural modification of natural products in the future. The articles were divided into six types based on the backbone structures of the natural products, and the related applications of amino acids in the structural modification of natural products were discussed in detail.

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“…Many cancers are associated with longevity, and the possibility of their appearance increases as the life expectancy of individuals lengthens [6]. On the other hand, cancers of high prevalence are related to environmental factors and lifestyles, which involve a series of modifiable risk factors for their development such as smoking, drinking, diet, sun exposure and others [7]. Currently, many anticancer agents are available, including alkylating agents, antimetabolites, antitumor antibiotics, natural products and hormones [8].…”

Section: Introductionmentioning

confidence: 99%

“…Also, this kind of biocompounds has a selective cytotoxic effect, attacking only to the cancer cells [9,10]. But, before its use, it is necessary to evaluate the activity of these therapies through in vitro antiproliferation assays, using cultures containing both tumour and non-tumour cells and different cell models [7]. Also, only few of these compounds have the potential to be therapeutic against cancer.…”

Section: Introductionmentioning

confidence: 99%

Pharmacology Evaluation of Bioactive Compounds that Regulate Cervical Cancer Cells

Salinas-Santander¹,

Alvarez-Ortiz²,

Valdes³

et al. 2019

Pharmacognosy - Medicinal Plants

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Cancer has been a public health problem that has gained a lot of death. However, in spite of the advances in the diagnosis and treatment of cervical cancer, women follow the struggle versus this disease. Also, those patients suffer from limited efficacy and specificity, undesirable effects, drug resistance, and a high cost of treatments. Currently, several studies have demonstrated the efficiency of natural products, called bioactive compounds, against cervical cancer cell lines. Bioactive compounds, including polyphenols and phenolic acids or flavonoids, etc., have antioxidant and pro-oxidant properties. These compounds are efficacy and show high specificity because probably they act as anti-oxidant and pro-oxidant. The prooxidant activity obstructs growth factors related to different signalling pathways that trigger cancer. Although, usually this kind of compounds helps for dispatching the apoptosis in cervical cancer cell. The aim of this chapter is reviewing how bioactive compounds affect the signalling pathways.

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Design, synthesis and anti-cancer activity evaluation of podophyllotoxin-norcantharidin hybrid drugs

Cited by 23 publications

References 26 publications

Insight Into the Molecular Mechanism of Podophyllotoxin Derivatives as Anticancer Drugs

Insight Into the Molecular Mechanism of Podophyllotoxin Derivatives as Anticancer Drugs

Application of Amino Acids in the Structural Modification of Natural Products: A Review

Pharmacology Evaluation of Bioactive Compounds that Regulate Cervical Cancer Cells

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