Advances of antitumor drug discovery in traditional Chinese medicine and natural active products by using multi‐active components combination

Abstract

The antitumor efficacy of Chinese herbal medicines has been widely recognized. Leading compounds such as sterols, glycosides, flavonoids, alkaloids, terpenoids, phenylpropanoids, and polyketides constitute their complex active components. The antitumor monomers derived from Chinese medicine possess an attractive anticancer activity. However, their use was limited by low bioavailability, significant toxicity, and side effects, hindering their clinical applications. Recently, new chemical entities have been designed and synthesized by combining natural drugs with other small drug molecules or active moieties to improve the antitumor activity and selectivity, and reduce side effects. Such a novel conjugated drug that can interact with several vital biological targets in cells may have a more significant or synergistic anticancer activity than a single‐molecule drug. In addition, antitumor conjugates could be obtained by combining pharmacophores containing two or more known drugs or leading compounds. Based on these studies, the new drug research and development could be greatly shortened. This study reviews the research progress of conjugates with antitumor activity based on Chinese herbal medicine. It is expected to serve as a valuable reference to antitumor drug research and clinical application of traditional Chinese medicine.

Identifying the Main Components and Mechanisms of Action of Artemisia annua L. in the Treatment of Endometrial Cancer Using Network Pharmacology

“…annua, it does not delve into the potential interactions between these components. Such interactions could significantly affect the therapeutic outcomes, especially when patients consume complex mixtures rather than isolated compounds . Moreover, we used only two cell lines, HEC-1-A and Ishikawa, to validate the results of the pharmacological network.…”

Traditionelle Chinesische Medizin in der Onkologie: wissenschaftliche Evidenz und Leitlinien

“…Klinische Studien belegen bislang keine ausreichende Evidenz für den Einsatz von chinesischen Arzneipflanzen als Tumortherapie. Das Potenzial der therapeutischen Möglichkeiten ist in diesem Bereich aber sicher noch nicht ausgeschöpft, sodass dringender Bedarf für weitere Forschung besteht [50].…”

A Comprehensive Review of Patented Antimicrobial Peptides from Amphibian Anurans

“…To first understand the pharmaceutical significance of AMPs, it needs to be stressed that the use of peptide-based drugs has numerous advantages, such as high potency, selectivity, and low toxicity. − Peptides, compared to small-molecule drugs such as bestatin, bacitracin, vinblastine, and others, can be more specific for their target, so they have fewer side effects, and because of their short half-life are less likely to accumulate in tissues. − However, the development of peptide-based drugs also presents numerous limitations, such as metabolic instability due to cleavage by proteolytic enzymes and high sensitivity to physicochemical changes such as temperature and pH, poor absorption, and limited membrane permeability as a result of the presence of charge and hydrophilic or polar amino acids. Chemical modifications are the most common solutions to overcome these limitations at the expense of increasing production costs. , In addition, approving new drugs, in which peptides are not an exception, is a long process, usually requiring a minimum of 10 to 15 years and compliance with demanding regulatory standards. − In this sense, and despite the marked increase in clinical trials using peptides during the last two decades, , the number of studies at this stage is deficient, especially when considering the exponential ratio in which new AMPs are described yearly. ,, To make the matter more complicated, about 40% of the AMP-based drugs in clinical trials are of human origin, often leading to the development of endogenous resistance mechanisms. , Thus, AMPs from other natural sources, such as microorganisms, insects, marine organisms, and amphibians, represent promising avenues of pharmaceutical investigation (Table , Figure ).…”