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Pharmaceuticals
Special Issues
Natural Terpenoids for Drug Candidates
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Natural Terpenoids for Drug Candidates

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (15 February 2023) | Viewed by 5588

Special Issue Editors

Dr. Kuei-Hung Lai

E-Mail Website
Guest Editor
Program in the Clinical Drug Development of Herbal Medicine, Taipei Medical University, Taipei 11031, Taiwan
Interests: natural products chemistry; mass spectrometry-based metabolomics; pharmacognosy
Special Issues, Collections and Topics in MDPI journals
Dr. Bo-Rong Peng

E-Mail Website1 Website2
Guest Editor
National Museum of Marine Biology and Aquarium, Pingtung 94450, Taiwan
Interests: natural products chemistry; marine natural products; aquaculture
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Terpenoids constitute the largest class of natural products. They are a rich source of potential candidates for new drug development. The name “Terpenoids” came from the fact that the first compound of this family was isolated from turpentine. The basic building block of this class of compounds is “Isoprene” unit, which is formed of five carbons. The combination of two isoprene units leads to the formation of “Monoterpenes”, while the combination of three isoprene units leads to the formation of “Sesquiterpenes” and the combination of four units results in the formation of “Diterpenes” and so on. Natural terpenoids can be isolated from different natural sources such as plants, animals, microbes, insects, plant pathogens and endophytes and marine organisms. Several reports including in vitro, preclinical, and clinical studies confirmed the wide array of important pharmacological properties of this class of compounds. Several compounds were developed into drug leads including the anticancer drug Taxol® and the antimalarial drug Artemisinin. It is generally accepted fact among scientists that “Terpenes are the Next Frontiers in Wellness”. In the light of these successes, we are promoting this Special Issue on new insights into natural terpenoids as drug candidates. We aim to publish research manuscripts and reviews focusing on the:

  • Isolation of terpenoids from terrestrial plants, microbes, marine organisms, and other sources.
  • The development of new drug candidates from natural terpenoids.
  • Pharmacokinetics and pharmacodynamics studies of drug candidates from natural terpenoids.
  • The development of new analytical methods for the qualitative and quantitative determination of drug candidates from natural terpenoids.
  • Evaluation of the pharmacological and toxicological effects of natural terpenoids.
  • Evaluation of ADME of drug candidates from natural terpenoids.
  • Clinical trials reporting the activities of drug candidates developed from natural terpenoids.
  • The development of pharmaceutical preparations and new drug delivery systems of drug candidates from natural terpenoids.
  • Evaluation of the biological targets and biomarkers of drug candidates from natural terpenoids including the determination of their target enzymes, receptors, membranes, genes, ion channels, inhibitors, agonists, antagonists, neurons, and binding affinity.
  • The application of computational methods for the development of drug candidates from natural terpenoids.
  • The application of artificial intelligence for the development of drug candidates from natural terpenoids with optimum activity and minimum side effects.
  • The application of biotechnological methods to produce natural terpenoids from different sources.
  • The application of nanotechnology for the formulation of drug candidates from natural terpenoids.

Dr. Kuei-Hung Lai
Dr. Bo-Rong Peng
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 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

  • isoprene
  • terpenoids
  • novel research strategies
  • new drug development

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Published Papers (2 papers)

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13 pages, 836 KiB  
Article
Isolation of the Lanostane Triterpenes Pholiols L–S from Pholiota populnea and Evaluation of Their Antiproliferative and Cytotoxic Activities
by Morteza Yazdani, Anita Barta, Anasztázia Hetényi, Róbert Berkecz, Gabriella Spengler, Attila Ványolós and Judit Hohmann
Pharmaceuticals 2023, 16(1), 104; https://doi.org/10.3390/ph16010104 - 10 Jan 2023
Viewed by 2262
Abstract
Pholiols L-S (1–8), eight undescribed triterpenes were isolated from the sporocarps of the mushroom Pholiota populnea. Various chromatographic techniques, such as open column chromatography, flash chromatography, gel filtration, preparative thin layer chromatography, and HPLC, were applied to purify [...] Read more.
Pholiols L-S (1–8), eight undescribed triterpenes were isolated from the sporocarps of the mushroom Pholiota populnea. Various chromatographic techniques, such as open column chromatography, flash chromatography, gel filtration, preparative thin layer chromatography, and HPLC, were applied to purify the compounds. The structure elucidation was carried out by spectroscopic analysis, including 1D (1H NMR and 13C JMOD) and 2D NMR (1H-1H COSY, HSQC, HMBC and NOESY) and HRESIMS experiments. The isolated compounds had lanostane (1–7) or trinorlanostane (8) skeletons; all of them were substituted with 3-hydroxy-3-methylglutaroyl group or its 6-methyl ester. Five compounds (1, 2, 4, 6, and 8) were investigated for their antiproliferative and cytotoxic activity in vitro by MTT assay on breast cancer (MCF-7), human colon adenocarcinoma (sensitive Colo 205, and resistant Colo 320), non-small cell lung cancer (A549), and human embryonic lung fibroblast (MRC-5) cell lines. Pholiols M (2) and O (4) showed antiproliferative activity against the MCF-7 cell line with IC50 of 2.48 and 9.95 µM, respectively. These compounds displayed tumor cell selectivity on MCF-7 cells with SI values of >40 (2) and 4.3 (4), but they did not show a cytotoxic effect, proving their action exclusively on tumor cell proliferation. Pholiols L (1) and Q (8) were found to have selective cytotoxicity on drug resistant cells in comparison to their effects on Colo320 and Colo205 cells [relative resistance values 0.84 (1) and 0.62 (8)]. Full article
(This article belongs to the Special Issue Natural Terpenoids for Drug Candidates)
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23 pages, 1113 KiB  
Systematic Review
In Vitro Efficacy of Extracts and Isolated Bioactive Compounds from Ascomycota Fungi in the Treatment of Colorectal Cancer: A Systematic Review
by Cristina Luque, Ana Cepero, Gloria Perazzoli, Cristina Mesas, Francisco Quiñonero, Laura Cabeza, Jose Prados and Consolación Melguizo
Pharmaceuticals 2023, 16(1), 22; https://doi.org/10.3390/ph16010022 - 23 Dec 2022
Cited by 5 | Viewed by 2733
Abstract
Colorectal cancer (CRC) is the second leading cause of cancer-related deaths worldwide. Despite the advances and success of current treatments (e.g., chemotherapy), there are multiple serious side effects which require the development of new treatment strategies. In recent years, fungi have gained considerable [...] Read more.
Colorectal cancer (CRC) is the second leading cause of cancer-related deaths worldwide. Despite the advances and success of current treatments (e.g., chemotherapy), there are multiple serious side effects which require the development of new treatment strategies. In recent years, fungi have gained considerable attention as a source of extracts and bioactive compounds with antitumor capabilities because of their antimicrobial and antioxidant properties and even their anti-inflammatory and antiviral activities. In the present review, a systematic search of the existing literature in four electronic databases was carried out in which the antitumor activity against CRC cells of Ascomycota fungi extracts or compounds was tested. The systematical research in the four databases resulted in a total of 883 articles. After applying exclusion and inclusion criteria, a total of 75 articles were finally studied. The order Eurotiales was the most studied (46% of the articles), and the ethyl acetate extraction was the most used method (49% of the papers). Penicillium extracts and gliotoxin and acetylgliotoxin G bioactive compounds showed the highest cytotoxic activity. This review also focuses on the action mechanisms of the extracts and bioactive compounds of fungi against CRC, which were mediated by apoptosis induction and the arrest of the cell cycle, which induces a notable reduction in the CRC cell proliferation capacity, and by the reduction in cell migration that limits their ability to produce metastasis. Thus, the ability of fungi to induce the death of cancer cells through different mechanisms may be the basis for the development of new therapies that improve the current results, especially in the more advanced stages of the CCR. Full article
(This article belongs to the Special Issue Natural Terpenoids for Drug Candidates)
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