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Natural Products as Antitumor Agents

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 11221

Special Issue Editor

College of Medicine, University of Sharjah, Sharjah P. O. Box 27272, United Arab Emirates
Interests: nanoparticles; drug delivery; nanocarriers; cancer therapy; computational modeling; nanomaterials; cancer biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products are beneficial to human health and, at large, to different aspects of our society. In fact, most therapeutic agents are derived from plants and microorganisms. In addition, many of the recently discovered anti-cancer nanoformulations are based on natural products. This Special Issue will focus on the anticancer activity obtained from natural sources.

Cancer is the second leading cause of death, following cardiovascular disease,  worldwide. The main cancer treatment is chemotherapy, which inhibits proliferation and modulates the key pathways of somatic cells. In recent years, continuous progress has been achieved in the development of therapeutic agents against cancer. Several compounds, including anthracyclines, enediynes, isoprenoids and macrolides, are proven to exert anticancer activity by inhibiting key regulators involved in different signal transduction pathways. Therefore, whether directly as biomolecules or indirectly through nanoformulations, natural products have great potential in the fight against cancer, both as preventive and therapeutic medicine and important contributors to nanomedicine (in diagnostics and therapeutics).

Research and review articles pertaining to the advances in natural product-based drug discovery are welcome for submission to this Special Issue. The development of new inhibitor compounds with potency against various cancer types, as well as the experimental validations, are welcome. Novel approaches (such as metabolomics, 3D culturing and biomolecule-based metal–organic frameworks) adopted in studying anticancer activity will receive high priority.

Prof. Dr. Amr Amin
Guest Editor

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • anticancer drugs
  • antitumor drugs
  • cancer therapy
  • drug discovery and development
  • inhibitor
  • chemical synthesis
  • natural products
  • biological activity
  • biomolecule-based nanoformulations
  • anticancer patents

Published Papers (5 papers)

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Research

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18 pages, 3143 KiB  
Article
Development and Evaluation of Crocetin-Functionalized Pegylated Magnetite Nanoparticles for Hepatocellular Carcinoma
by Sulafa Ibrahim, Badriya Baig, Soleiman Hisaindee, Hussein Darwish, Ashraf Abdel-Ghany, Hesham El-Maghraby, Amr Amin and Yaser Greish
Molecules 2023, 28(7), 2882; https://doi.org/10.3390/molecules28072882 - 23 Mar 2023
Cited by 7 | Viewed by 1523
Abstract
Liver cancer remains among the leading causes of cancer-related deaths worldwide. This is due to many reasons, including limitations of available drugs, late diagnosis due to the overlapping symptoms with many other liver diseases, and lack of effective screening modalities. Compared to conventional [...] Read more.
Liver cancer remains among the leading causes of cancer-related deaths worldwide. This is due to many reasons, including limitations of available drugs, late diagnosis due to the overlapping symptoms with many other liver diseases, and lack of effective screening modalities. Compared to conventional chemotherapy, targeted drug delivery systems are advantageous in many ways, as they minimize drug resistance and improve therapeutic value for cancer patients. Nanomaterials, in general, and nanoparticles, in particular, possess nm size, which provides a high surface area for a great extent of functionalization to be used for the targeted delivery of cancer drugs. Amongst the different formulations of nanoparticles, magnetic nanoparticles (MNPs) have unique chemical and physical characteristics and magnetic behavior, making them preferable candidates as a core for drug delivery systems. To maintain the nanosized structure of MNPs, a polymeric coating is usually applied to maintain the nanoparticles dispersed in the solution. Moreover, the polymeric coating provides a plate form for carrying drug molecules on its surface. In the present study, poly(ethylene glycol) (PEG)-coated MNPs were successfully synthesized, where the optimum concentration of PEG on the surface of the MNPs was investigated. The PEG-coated MNPs were further coated with crocetin at different concentrations. The crocetin-coated pegylated MNPs were evaluated in vitro using a hepatic cell line (HepG2) for up to 72 h. Results showed good release kinetics under acidic and neutral conditions. The optimally prepared drug delivery system showed a high potential for reducing the HepG2 cell proliferation in vitro using an MTT assay. The calculated IC50 for Cro-PEG-MNPs were 0.1019, 0.0903, and 0.0462 mg/mL of 5×, 10× and 20×, respectively. Full article
(This article belongs to the Special Issue Natural Products as Antitumor Agents)
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20 pages, 3238 KiB  
Article
Effects of Sorafenib and Quercetin Alone or in Combination in Treating Hepatocellular Carcinoma: In Vitro and In Vivo Approaches
by Suzan Abdu, Nouf Juaid, Amr Amin, Mohamed Moulay and Nabil Miled
Molecules 2022, 27(22), 8082; https://doi.org/10.3390/molecules27228082 - 21 Nov 2022
Cited by 38 | Viewed by 2725
Abstract
Sorafenib is the first drug approved to treat advanced hepatocellular carcinoma (HCC) and continues as the gold-standard therapy against HCC. However, acquired drug resistance represents a main concern about sorafenib therapy. The flavanol quercetin found in plants has shown great anti-cancer and anti-inflammatory [...] Read more.
Sorafenib is the first drug approved to treat advanced hepatocellular carcinoma (HCC) and continues as the gold-standard therapy against HCC. However, acquired drug resistance represents a main concern about sorafenib therapy. The flavanol quercetin found in plants has shown great anti-cancer and anti-inflammatory properties. In this work, quercetin was used as a therapeutic agent alone or in combination with a sorafenib chemotherapy drug to improve the routine HCC treatment with sorafenib. The in vitro and in vivo results presented here confirm that quercetin alone or in combination with sorafenib significantly inhibited HCC growth, induced cell cycle arrest and induced apoptosis and necrosis. Further molecular data shown in this report demonstrate that quercetin alone or combined with sorafenib downregulated key inflammatory, proliferative and angiogenesis-related genes (TNF-α, VEGF, P53 and NF-κB). Combined quercetin/sorafenib treatment markedly improved the morphology of the induced liver damage and showed significant antioxidant and anti-tumor effects. The advantage of combined treatment efficacy reported here can be attributed to quercetin’s prominent effects in modulating cell cycle arrest, apoptosis, oxidative stress and inflammation. Full article
(This article belongs to the Special Issue Natural Products as Antitumor Agents)
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20 pages, 8018 KiB  
Article
Uncovering the Mechanisms of Active Components from Toad Venom against Hepatocellular Carcinoma Using Untargeted Metabolomics
by Pan Liang, Yining Ma, Luyin Yang, Linshen Mao, Qin Sun, Changzhen Sun, Zengjin Liu, Maryam Mazhar, Sijin Yang and Wei Ren
Molecules 2022, 27(22), 7758; https://doi.org/10.3390/molecules27227758 - 10 Nov 2022
Cited by 3 | Viewed by 2240
Abstract
Toad venom, a dried product of secretion from Bufo bufo gargarizans Cantor or Bufo melanostictus Schneider, has had the therapeutic effects of hepatocellular carcinoma confirmed. Bufalin and cinobufagin were considered as the two most representative antitumor active components in toad venom. However, the [...] Read more.
Toad venom, a dried product of secretion from Bufo bufo gargarizans Cantor or Bufo melanostictus Schneider, has had the therapeutic effects of hepatocellular carcinoma confirmed. Bufalin and cinobufagin were considered as the two most representative antitumor active components in toad venom. However, the underlying mechanisms of this antitumor effect have not been fully implemented, especially the changes in endogenous small molecules after treatment. Therefore, this study was designed to explore the intrinsic mechanism on hepatocellular carcinoma after the cotreatment of bufalin and cinobufagin based on untargeted tumor metabolomics. Ultraperformance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) was performed to identify the absorbed components of toad venom in rat plasma. In vitro experiments were determined to evaluate the therapeutic effects of bufalin and cinobufagin and screen the optimal ratio between them. An in vivo HepG2 tumor-bearing nude mice model was established, and a series of pharmacodynamic indicators were determined, including the body weight of mice, tumor volume, tumor weight, and histopathological examination of tumor. Further, the entire metabolic alterations in tumor after treating with bufalin and cinobufagin were also profiled by UHPLC-MS/MS. Twenty-seven active components from toad venom were absorbed in rat plasma. We found that the cotreatment of bufalin and cinobufagin exerted significant antitumor effects both in vitro and in vivo, which were reflected in inhibiting proliferation and inducing apoptosis of HepG2 cells and thereby causing cell necrosis. After cotherapy of bufalin and cinobufagin for twenty days, compared with the normal group, fifty-six endogenous metabolites were obviously changed on HepG2 tumor-bearing nude mice. Meanwhile, the abundance of α-linolenic acid and phenethylamine after the bufalin and cinobufagin intervention was significantly upregulated, which involved phenylalanine metabolism and α-linolenic acid metabolism. Furthermore, we noticed that amino acid metabolites were also altered in HepG2 tumor after drug intervention, such as norvaline and Leu-Ala. Taken together, the cotreatment of bufalin and cinobufagin has significant antitumor effects on HepG2 tumor-bearing nude mice. Our work demonstrated that the in-depth mechanism of antitumor activity was mainly through the regulation of phenylalanine metabolism and α-Linolenic acid metabolism. Full article
(This article belongs to the Special Issue Natural Products as Antitumor Agents)
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12 pages, 467 KiB  
Article
Antifungal Effects and Active Components of Ligusticum chuanxiong
by Huabao Chen, Yingchun Zhao, Guangwei Qin, Yan Bi, Guizhou Yue, Min Zhang, Xiaoli Chang, Xiaoyan Qiu, Liya Luo and Chunping Yang
Molecules 2022, 27(14), 4589; https://doi.org/10.3390/molecules27144589 - 19 Jul 2022
Cited by 5 | Viewed by 1918
Abstract
The separation of chemical components from wild plants to develop new pesticides is a hot topic in current research. To evaluate the antimicrobial effects of metabolites of Ligusticum chuanxiong (CX), we systematically studied the antimicrobial activity of extracts of CX, and the [...] Read more.
The separation of chemical components from wild plants to develop new pesticides is a hot topic in current research. To evaluate the antimicrobial effects of metabolites of Ligusticum chuanxiong (CX), we systematically studied the antimicrobial activity of extracts of CX, and the active compounds were isolated, purified and structurally identified. The results of toxicity measurement showed that the extracts of CX had good biological activities against Botrytis cinerea, Sclerotinia sclerotiorum, Alternaria alternata and Pythium aphanidermatum, and the value of EC50 were 130.95, 242.36, 332.73 and 307.29 mg/L, respectively. The results of in vivo determination showed that under the concentration of 1000 mg/L, the control effect of CX extract on Blumeria graminis was more than 40%, and the control effect on Botrytis cinerea was 100%. The antifungal active components of CX were identified as Senkyunolide A and Ligustilide by mass spectrometry and nuclear magnetic resonance. The MIC (minimum inhibitory concentration) value of Senkyunolide A and Ligustilide against Fusarium graminearum were 7.81 and 62.25 mg/L, respectively. As a new botanical fungicide with a brightly exploitative prospect, CX extract has potential research value in the prevention and control of plant diseases. Full article
(This article belongs to the Special Issue Natural Products as Antitumor Agents)
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Review

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15 pages, 1401 KiB  
Review
Recent Updates on the Functional Impact of Kahweol and Cafestol on Cancer
by Salma Eldesouki, Rama Qadri, Rashid Abu Helwa, Hiba Barqawi, Yasser Bustanji, Eman Abu-Gharbieh and Waseem El-Huneidi
Molecules 2022, 27(21), 7332; https://doi.org/10.3390/molecules27217332 - 28 Oct 2022
Cited by 9 | Viewed by 2093
Abstract
Kahweol and cafestol are two diterpenes extracted from Coffea arabica beans that have distinct biological activities. Recent research describes their potential activities, which include anti-inflammatory, anti-diabetic, and anti-cancer properties, among others. The two diterpenes have been shown to have anticancer effects in various [...] Read more.
Kahweol and cafestol are two diterpenes extracted from Coffea arabica beans that have distinct biological activities. Recent research describes their potential activities, which include anti-inflammatory, anti-diabetic, and anti-cancer properties, among others. The two diterpenes have been shown to have anticancer effects in various in vitro and in vivo cancer models. This review aims to shed light on the recent developments regarding the potential effects of kahweol and cafestol on various cancers. A systematic literature search through Google Scholar and PubMed was performed between February and May 2022 to collect updates about the potential effects of cafestol and kahweol on different cancers in in vitro and in vivo models. The search terms “Kahweol and Cancer” and “Cafestol and Cancer” were used in this literature review as keywords; the findings demonstrated that kahweol and cafestol exhibit diverse effects on different cancers in in vitro and in vivo models, showing pro-apoptotic, cytotoxic, anti-proliferative, and anti-migratory properties. In conclusion, the diterpenes kahweol and cafestol display significant anticancer effects, while remarkably unaffecting normal cells. Our results show that both kahweol and cafestol exert their actions on various cancers via inducing apoptosis and inhibiting cell growth. Additionally, kahweol acts by inhibiting cell migration. Full article
(This article belongs to the Special Issue Natural Products as Antitumor Agents)
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