Abstract

Cancer is a severe health problem that continues to be a leading cause of death worldwide. Increasing knowledge of the molecular mechanisms underlying cancer progression has led to the development of a vast number of anticancer drugs. However, the use of chemically synthesized drugs has not significantly improved the overall survival rate over the past few decades. As a result, new strategies and novel chemoprevention agents are needed to complement current cancer therapies to improve efficiency. Naturally occurring compounds from plants known as phytochemicals, serve as vital resources for novel drugs and are also sources for cancer therapy. Some typical examples include taxol analogs, vinca alkaloids such as vincristine, vinblastine, and podophyllotoxin analogs. These phytochemicals often act via regulating molecular pathways which are implicated in growth and progression of cancer. The specific mechanisms include increasing antioxidant status, carcinogen inactivation, inhibiting proliferation, induction of cell cycle arrest and apoptosis; and regulation of the immune system. The primary objective of this review is to describe what we know to date of the active compounds in the natural products, along with their pharmacologic action and molecular or specific targets. Recent trends and gaps in phytochemical based anticancer drug discovery are also explored. The authors wish to expand the phytochemical research area not only for their scientific soundness but also for their potential druggability. Hence, the emphasis is given to information about anticancer phytochemicals which are evaluated at preclinical and clinical level.

Highlights

  • Cancer is a major public health problem that has a significant global impact on both developed and developing countries

  • One major asset of medicinal plant-based drug discovery is the existence of ethnopharmacological information providing ideal opportunities to limit the huge diversity of possible leads to more promising ones

  • A novel approach of integrated drug discovery where ethnopharmacological knowledge is supported by broad interdisciplinary forces involving medicinal chemistry, pharmacology, biochemistry, molecular, and cellular biology along with natural product chemistry is necessary to harvest the full potential of phytochemicals

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Summary

INTRODUCTION

Cancer is a major public health problem that has a significant global impact on both developed and developing countries. An attempt has been made to gather information about the anti-cancer phytochemicals that are evaluated at preclinical and clinical levels as well as those available in the market, until now. Over the period from around 1981 to the end of 2014, more than half of all approved small‐molecule drugs originated from natural products, where they served as drug precursors, templates for synthetic modification, and pharmacological probes (Newman and Cragg, 2016). This in itself demonstrates the enormous medicinal potential of plants that has been known for thousands of years in traditional medicine.

Parkinson Malaria Alzheimer Hepatorenal tyrosinemia Cancer Asthma and COPD
Inhibit cell proliferation and apoptosis
PHYTOCHEMICALS EVALUATED IN CLINICAL TRIALS
Prevention of recurrence
PHYTOCHEMICALS USED IN CURRENT CANCER THERAPY
Vinblastine Vincristine Vindesine Vinflunine Vinorelbine Taxanes
Inhibit microtubule function resulting in cell cycle arrest and aberrant mitosis
Inhibits DNA synthesis by forming a complex
CONCLUSIONS AND FUTURE PERSPECTIVES
Findings
AUTHOR CONTRIBUTIONS
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