scholarly journals Natural Products as Chemopreventive Agents by Potential Inhibition of the Kinase Domain in ErbB Receptors

Molecules ◽  
2017 ◽  
Vol 22 (2) ◽  
pp. 308 ◽  
Author(s):  
Maria Olivero-Acosta ◽  
Wilson Maldonado-Rojas ◽  
Jesus Olivero-Verbel
2015 ◽  
Vol 2015 ◽  
pp. 1-26 ◽  
Author(s):  
Chen-Yi Liao ◽  
Ching-Chang Lee ◽  
Chi-chang Tsai ◽  
Chao-Wen Hsueh ◽  
Chih-Chiang Wang ◽  
...  

We would like to highlight the application of natural products to hepatocellular carcinoma (HCC). We will focus on the natural products known as flavonoids, which target this disease at different stages of hepatocarcinogenesis. In spite of the use of chemotherapy and radiotherapy in treating HCC, patients with HCC still face poor prognosis because of the nature of multidrug resistance and toxicity derived from chemotherapy and radiotherapy. Flavonoids can be found in many vegetables, fruits, and herbal medicines that exert their different anticancer effects via different intracellular signaling pathways and serve as antioxidants. In this review, we will discuss seven common flavonoids that exert different biological effects against HCC via different pathways.


Author(s):  
BALABHASKAR R ◽  
RAJENDRA KUMAR A ◽  
SELVARAJAN S ◽  
FARIDHA A ◽  
GAYATHRI GUNALAN

Natural products continue to be a source for the discovery of drugs and drug leads even from ancient period. 80% of drug molecules have been obtained from either natural products or derivatives of the natural product. It has been found that the concept of a single drug for treating single disease may become outdated in the near future and the need of polyherbal formulations, as an alternate remedy is under investigation. Medicinal and aromatic plants contain biologically important phytochemicals, which have known curative properties. They are found as secondary metabolites in plants. Plants also contain certain other compounds that moderate the effects of the active ingredients. Medicinal and aromatic plants have their own contribution toward the treatment of both noncommunicable and communicable diseases. A survey done by the WHO indicates that a majority of the world population tends to use plants for treating diseases. Cancer, the second largest cause of death after cardiovascular disease accounts for about 3500 million people globally. Due to the serious side effects of synthetic chemopreventive agents, research is going onto investigate the nature derived chemopreventive agents. In addition to the plant-derived compounds, marine, and animal resources also play an important role as clinically beneficial anticancer agents with minimal or no toxicity. The best examples for plant-derived compounds include vincristine, vinblastine, irinotecan, etoposide, and paclitaxel; they have a different mode of action against cancer such as interaction with microtubules, inhibition of topoisomerases I or II, alkylation of DNA, and interference with tumor signal transduction. The natural products from marine sources such as bryostatin, squalamine exhibit a significant antimitotic, and anti-angiogenic activities. The benefits of various anticancer drugs derived from natural products are the fact that it can have its effect on cancer cells alone without harming healthy cells, which is unlikely to be the case with other conventional chemotherapeutics. In this review, various natural products and their anticancer properties have been discussed briefly.


Biomolecules ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 508 ◽  
Author(s):  
Yonghyo Kim ◽  
Yutaka Sugihara ◽  
Tae Young Kim ◽  
Sung Min Cho ◽  
Jin Young Kim ◽  
...  

Although natural products are an important source of drugs and drug leads, identification and validation of their target proteins have proven difficult. Here, we report the development of a systematic strategy for target identification and validation employing drug affinity responsive target stability (DARTS) and mass spectrometry imaging (MSI) without modifying or labeling natural compounds. Through a validation step using curcumin, which targets aminopeptidase N (APN), we successfully standardized the systematic strategy. Using label-free voacangine, an antiangiogenic alkaloid molecule as the model natural compound, DARTS analysis revealed vascular endothelial growth factor receptor 2 (VEGFR2) as a target protein. Voacangine inhibits VEGFR2 kinase activity and its downstream signaling by binding to the kinase domain of VEGFR2, as was revealed by docking simulation. Through cell culture assays, voacangine was found to inhibit the growth of glioblastoma cells expressing high levels of VEGFR2. Specific localization of voacangine to tumor compartments in a glioblastoma xenograft mouse was revealed by MSI analysis. The overlap of histological images with the MSI signals for voacangine was intense in the tumor regions and showed colocalization of voacangine and VEGFR2 in the tumor tissues by immunofluorescence analysis of VEGFR2. The strategy employing DARTS and MSI to identify and validate the targets of a natural compound as demonstrated for voacangine in this study is expected to streamline the general approach of drug discovery and validation using other biomolecules including natural products.


Author(s):  
Yonghyo Kim ◽  
Yutaka Sugihara ◽  
Tae Young Kim ◽  
Sung Min Cho ◽  
Jin Young Kim ◽  
...  

Although natural products are an important source of drugs and drug leads, identification and validation of their target proteins have proven difficult. Here, we report the development of a systematic strategy for target identification and validation employing drug affinity responsive target stability (DARTS) and mass spectrometry imaging (MSI) without modifying or labeling natural compounds. Through a validation step using curcumin, which targets aminopeptidase N (APN), we successfully standardized the systematic strategy. Using label-free voacangine, an antiangiogenic alkaloid molecule as the model natural compound, DARTS analysis revealed vascular endothelial growth factor receptor 2 (VEGFR2) as a target protein. Voacangine inhibits VEGFR2 kinase activity and its downstream signaling by binding to the kinase domain of VEGFR2, as was revealed by docking simulation. Through cell culture assays, voacangine was found to inhibit the growth of glioblastoma cells expressing high levels of VEGFR2. Specific localization of voacangine to tumor compartments in a glioblastoma xenograft mouse was revealed by MSI analysis. The overlap of histological images with the MSI signals for voacangine was intense in the tumor regions and showed colocalization of voacangine and VEGFR2 in the tumor tissues by immunofluorescence analysis of VEGFR2. The strategy employing DARTS and MSI to identify and validate the targets of a natural compound as demonstrated for voacangine in this study is expected to streamline the general approach of drug discovery and validation using other biomolecules including natural products.


Author(s):  
P. García-Pérez ◽  
M.E. Barreal ◽  
L. Rojo-De Dios ◽  
J.F. Cameselle-Teijeiro ◽  
P.P. Gallego

2020 ◽  
Vol 21 ◽  
Author(s):  
Mohammad El-Harakeh ◽  
Sara Al-Ghadban ◽  
Rémi Safi

: Skin cancer remains a major cause of mortality worldwide. It can be divided into melanoma and non-melanoma cancer which comprises mainly squamous cell carcinoma and basal cell carcinoma. Although conventional therapies have ameliorated the management of skin cancer, the search for chemopreventive compounds is still the most effective and safer strategy to treat cancer. Nowadays, chemoprevention is recognized as a novel approach to prevent or inhibit carcinogenesis steps by the use of natural products. Crude extracts of plants and isolated phytocompounds are considered chemopreventive agents since they harbor anti-inflammatory, antioxidant and anti-oncogenic properties against many types of diseases and cancers. In this review, we will discuss the therapeutic effect and preventive potential of selected medicinal plants used as crude extracts or as phytocompounds against melanoma and non-melanoma cutaneous cancers.


2021 ◽  
Vol 12 ◽  
Author(s):  
Bingke Bai ◽  
Qianbo Chen ◽  
Rui Jing ◽  
Xuhui He ◽  
Hongrui Wang ◽  
...  

Prostate cancer is the second most common malignant cancer in males. It involves a complex process driven by diverse molecular pathways that closely related to the survival, apoptosis, metabolic and metastatic characteristics of aggressive cancer. Prostate cancer can be categorized into androgen dependent prostate cancer and castration-resistant prostate cancer and cure remains elusive due to the developed resistance of the disease. Natural compounds represent an extraordinary resource of structural scaffolds with high diversity that can offer promising chemical agents for making prostate cancer less devastating and curable. Herein, those natural compounds of different origins and structures with potential cytotoxicity and/or in vivo anti-tumor activities against prostate cancer are critically reviewed and summarized according to the cellular signaling pathways they interfere. Moreover, the anti-prostate cancer efficacy of many nutrients, medicinal plant extracts and Chinese medical formulations were presented, and the future prospects for the application of these compounds and extracts were discussed. Although the failure of conventional chemotherapy as well as involved serious side effects makes natural products ideal candidates for the treatment of prostate cancer, more investigations of preclinical and even clinical studies are necessary to make use of these medical substances reasonably. Therefore, the elucidation of structure-activity relationship and precise mechanism of action, identification of novel potential molecular targets, and optimization of drug combination are essential in natural medicine research and development.


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