Anticancer Effect of Capsaicin and Its Analogues

Abstract

Potent biomolecules from natural products from plants, animals, and minerals are the fundamental basis of the ailment of mankind. Capsicum or red pepper plants were grouped under the kingdom Plantae and family Solanaceae. It is used widely throughout the world in foods for their pungent flavor and aroma, and to prolong food spoilage. This chapter presents a frame of a concise compilation of the anticancer and cytotoxic potentials of Capsicum, its analogs, and related compounds. Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) is the most predominant and naturally occurring alkaloid from the Capsicum species. It also details the anticancer efficacy of capsaicin and its analogs like capsaicinoids and capsiates which possess antioxidants and targets multiple signaling pathways, ontogenesis, and tumor-suppressor genes in various types of cancer models. Capsaicin is a major ingredient and has been linked to suppression of growth in various cancer cells. The data available strongly indicate the significant anticancer benefits of capsaicin and its potent analog molecules. It shows a significant effect on cancer cell proliferation, apoptosis, cancer cell surveillance, growth arrest, and metastasis. This chapter also predominantly focuses on the combinational use of capsaicin with other natural dietary compounds as a measure of synergistic anticancer activities.

Anticancer Activity of Region B Capsaicin Analogs

“…SAR studies involving 17 resulted in the synthesis of almost 30 synthetic analogs which were screened for growth-inhibitory activity using HeLa human ovarian carcinoma cells. 96 MTT assays revealed that four of these compounds, C-29 (18), CIDD-24 (19), CIDD-111 (20), and CIDD-99 (21), displayed the maximal decrease in cell viability of the HeLa cells over 24 h. The growth suppressive activities of 18, 19, and 21 were similar to each other (IC 50 < 5 μM) in HeLa cells. However, the growthinhibitory activity of 20 (IC 50 ∼ 25 μM) was lower than 18, 19, and 21.…”

“…The vanilloid phytochemical 1 displays potent antineoplastic activity in multiple human cancers ,, and can improve the therapeutic efficacy of chemotherapeutic drugs and radiation therapy when used in combination. − Despite such promising applications, the development of 1 as a clinically useful anticancer drug has been limited by its unpleasant side effects. The administration of 1 causes skin redness, hyperalgesia, nausea, intense tearing in the eyes, conjunctivitis, blepharospasm (sustained, forced, and involuntary closing of the eyelids), vomiting, abdominal pain, stomach cramps, bronchospasm, and burning diarrhea in patients. − Clinical trials exploring the pain-relieving activity of 1 have shown that such side effects have resulted in patients discontinuing use of the drug.…”

“…It was observed that the programmed cell death induced by 5 (in human pancreatic cancer cells and SCCs) was mediated by its ability to block the mitochondrial electron transport chain (Table ). Both 1 and 5 have been shown to be potent inhibitors of complex I of the mitochondrial electron transport chain . The vanillyl moiety of 1 and 5 (indicated by the purple color in Figure ) is structurally similar to the cyclic portion of coenzyme Q, which explains the fact that these compounds act as coenzyme Q antagonists .…”

“…The antineoplastic activity of 1 has been observed in leukemia, breast, lung, prostate, brain, gastrointestinal, and gynecological cancers. 20 − 22 In several types of human cancers, capsaicin inhibits tumor invasion and metastasis to distant organs. 23 , 24 Apart from exerting direct growth-inhibitory activity toward human tumors, 1 sensitizes human cancer cells to the growth-suppressive effects of established chemotherapy drugs and radiotherapy.…”

How Should the Worldwide Knowledge of Traditional Cancer Healing Be Integrated with Herbs and Mushrooms into Modern Molecular Pharmacology?

“…A huge number of studies have demonstrated the capsaicin-mediated anticancer effects [ 122 , 123 ]. In non-small cell lung cancer (NSCLC), capsaicin inhibits vascular endothelial growth factor (VEGF) expression and angiogenesis via the p53-HIF1-VEGF pathway [ 124 ].…”