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Traditional Medicine Research Doi: 10.12032/TMR20210616237 Traditional Medicine Research doi: 10.12032/TMR20210616237 Annual advances of integrative pharmacology in 2020 Ke-Wu Zeng1*, Ming-Yao Gu2* 1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; 2Department of Cell Biology and Medical Genetics, School of Basic Medical Sciences, Shenzhen University Health Science Center, Shenzhen 518061, China. *Corresponding to: Ke-Wu Zeng, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, No.38 Xueyuan Road, Haidian District, Beijing 100191, China; E-mail: [email protected]. Ming-Yao Gu, Department of Cell Biology and Medical Genetics, School of Basic Medical Sciences, Shenzhen University Health Science Center, No.1066 Xueyuan Avenue, Nanshan District, Shenzhen 518061, China; E-mail: [email protected]. Highlights This review covers the studies in the year 2020 for pharmacological reports on traditional medicine as well as herb-derived active natural products. Moreover, the pharmacological reports on active natural products against cancers, inflammation, and metabolic diseases were major topics. Tradition This annual integrative pharmacology review includes the reports published in 2020 on bioactive herbal extracts and novel compounds in traditional medicine. Pharmacological reports on traditional herbs as well as their active compounds for anticancer, inflammation, and metabolic diseases occupy dominant positions. Submit a manuscript: https://www.tmrjournals.com/tmr 1 doi: 10.12032/TMR20210616237 REVIEW Abstract Major studies on the pharmacology of traditional herbs as well as active compounds have been introduced in this review over the previous 12 months. This annual integrative pharmacology review includes the reports published in 2020 on bioactive herbal extracts and novel compounds in traditional medicine. Pharmacological reports on traditional herbs as well as their active compounds for anticancer, inflammation, and metabolic diseases occupy dominant positions. Traditional medicines are still widely reported as a crucial treatment to exhibit anticancer efficacy in numerous human cancer cells. Moreover, the focus on the discovery of bioactive compounds from traditional medicines against mental disorders and neurodegenerative diseases seems to increase. The reports on bone loss and organ fibrosis treatments have notably gradually increased. Furthermore, studies of traditional herbs on cardiovascular and cerebrovascular diseases show a declining trend. These pharmacological reports in 2020 collectively show several crucial therapeutic targets and promising candidate compounds from traditional medicines for human diseases. Keywords: Traditional medicine, Natural product, Pharmacology, Cancer, Inflammation, Infectious diseases Author contributions: Ke-Wu Zeng and Ming-Yao Gu wrote the manuscript together, and also contributed to the manuscript editing. Additionally, Ke-Wu Zeng provided the original materials and Ming-Yao Gu prepared the figure and table. Competing interests: The authors declare no conflicts of interest. Acknowledgments: None. Abbreviations: ROS, reactive oxygen species; MAPK, mitogen-activated protein kinases; TNBC, triple-negative breast cancer; HCC, hepatocellular carcinoma; PPAR-γ, peroxisome proliferator-activated receptor gamma. Citation: Zeng KW, Gu MY. Annual advances of integrative pharmacology in 2020. Tradit Med Res. 2021;6(4):31. doi: 10.12032/TMR20210616237. Executive editor: Rui-Wang Zhao. Submitted: 02 June 2020, Accepted: 18 June 2021, Online: 21 June 2021. © 2021 By Authors. Published by TMR Publishing Group Limited. This is an open access article under the CC-BY license (http://creativecommons.org/licenses/BY/4.0/). 2 Submit a manuscript: https://www.tmrjournals.com/tmr Traditional Medicine Research doi: 10.12032/TMR20210616237 Cancers Background Cancer is still one of the greatest threats to human The representative studies on the pharmacology of health. Thus, researchers worldwide are exerting a lot traditional herbs over the previous 12 months have of effort into looking for natural compounds from been summarized in the almanac for 2020 to build a traditional medicinal plants to treat various cancers. A comprehensive understanding of the progress of great number of studies on cancer study exist in the traditional medicines for human disease treatments. year 2020, similar to previous years. Some reports The total number of pharmacological studies on about the natural compounds targeting colorectal traditional medicines has not changed much compared cancer mainly through inhibiting cell with previous years. The studies of the active proliferation-related cell signaling pathways were ingredients from traditional medicines in anticancer found. Delicaflavone, isolated from Selaginella research still occupy a dominant position. In particular, doederleinii, inhibits the viability of colorectal cancer some famous natural products (e.g., berberine, cells by blocking both Ras/MEK/Erk and tanshinol A, lycorine, and emodin) are major topics of PI3K/AKT/mTOR pathways [1]. Acetylshikonin, a concern. Moreover, research reports of traditional diterpenoid compound from the root of Lithospermum medicines used as therapy for metabolic diseases erythrorhizon, has been identified as a maintained strong upwards momentum in 2020. T-lymphokine-activated killer cell-originated protein Pharmacological studies of active compounds kinase inhibitor to attenuate the proliferation of including isoliquiritigenin, hypericin, and colorectal cancer cells [2]. Moreover, berberine serves protocatechuic acid on diabetes have obtained more as a potential therapeutic agent against colon cancer by attention. Interestingly, the bioactive compounds from targeting the cleavage activating protein/sterol traditional herbs against inflammation-associated regulatory element binding protein-1 pathway [3]. The diseases including artesunate, ginsenoside, and natural product β-elemene, from Curcumae rhizoma, is celastrol arouse people’s interest again. Meanwhile, a novel ferroptosis inducer. In addition, β-elemene pharmacological studies have shown a diversification co-treatment with cetuximab suppresses KRAS mutant trend. For example, increasing number of studies tumor cell proliferation as well as metastases by reported the protective effects of traditional herbs on inducing iron-dependent reactive oxygen species (ROS) bone loss and organ fibrosis. Unexpectedly, the studies accumulation, lipid peroxidation, and downregulation on cardiovascular and cerebrovascular diseases have of negative regulatory proteins [4]. Palmatine is an decreased, which is different from previous years. isoquinoline alkaloid from Rhizoma coptidis, which Thus, this review provides a broad annual summary of shows significant anticolon cancer effects by the pharmacological study progress on traditional promoting ROS production [5]. Furthermore, medicine during the year 2020 (Figure 1). triterpenoid saponin extracted from Melia toosendan Sieb et Zucc suppresses Wnt/β-catenin signaling to reduce the proliferation of colorectal cancer cells [6]. Lung cancer is well-known as the most common type of malignant tumor in the respiratory system. Many natural products are to be studied to treat lung cancer mainly via targeting tumor angiogenesis with the increasing number of lung cancer patients and the related treatment research. Tanshinol A, a natural compound from Salvia miltiorrhiza, exerts its anticancer effect in the lung by inducing intracellular adenosine triphosphate depletion and ROS generation [7]. Deguelin, a natural product isolated from Derris elliptica, decreases the Mcl-1 protein level in an ubiquitination-dependent fashion against non-small cell lung cancer cells [8]. Pristimerin, isolated from Figure 1 Comparison of published reports about 9 Celastrus aculeatus Merr, inhibits vessel sprouts diseases between 2019 and 2020. C, cancer; CCD, formation by targeting Shh/Gli1 signaling pathway to cardiovascular and cerebrovascular diseases; IRD, suppress tumor angiogenesis in NCI-H1299 xenografts inflammation-related diseases; ND, neurodegerative [9]. Arctigenin from Arctium lappa suppresses lung diseases; MD, diabetes and metabolic diseases; ID, adenocarcinoma growth via the mitogen-activated infectious diseases; DMD, depression and mental protein kinases (MAPK) pathway [10]. Erianin, a disorders; OD, other diseases; BL, bone loss; OF, novel dibenzyl compound in Dendrobium chrysotoxum organ fibrosis. Lindl, induces Ca2+/CaM-dependent ferroptosis in lung cancer cells [11]. Lycorine, a natural small molecule Submit a manuscript: https://www.tmrjournals.com/tmr 3 doi: 10.12032/TMR20210616237 REVIEW from Lycoris radiate, suppresses tumorigenicity, Schisandra chinensis has an antiproliferation effect on angiogenesis, and invasion of lung cancer cells by gastric cancer cell lines by inducing cell cycle arrest at inducing the accumulation of tumor suppressor the G2/M phase and cell apoptosis [30]. Imperatorin, a Salvador homolog 1 [12]. Hederagenin, a triterpenoid natural active compound from Angelica dahurica, is derived from the Hedera helix, may be used as an reported to treat muscle wasting in cancer cachexia by adjuvant to promote the antineoplastic effects of inhibiting the signal transducer and activator of conventional chemotherapeutics [13]. Moreover, transcription 3 pathway [31]. Fisetin from Rhus thevebioside, from Thevetia peruviana, is a potent succedanea L. inhibits cell proliferation
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