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Molecules
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Development of New Drugs from Bioactive Compounds
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Development of New Drugs from Bioactive Compounds

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

Deadline for manuscript submissions: closed (28 April 2023) | Viewed by 2862

Special Issue Editor

Prof. Dr. Qingyong Li

E-Mail Website
Guest Editor
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China
Interests: extraction and separation of bioactive compounds from natural sources; development of new drugs

Special Issue Information

Dear Colleagues,

Research on new drugs from bioactive compounds has uncovered important treatment strategies for diseases with a high medical need, such as oncology, Alzheimer’s disease, metabolic diseases, etc. A large number of new drugs have numerous problems, such as a suboptimal effect, high recurrence, multiple side-effects, and the requirement of long-term administration. Accordingly, there is a need for novel drugs with improved effects. This Special Issue on “Development of New Drugs from Bioactive Compounds” aims to gather contributions to examine the issue of novel bioactive molecules with therapeutic effects. Research involving new compounds, new targets, new mechanisms, pharmacokinetics, improved formulation and efficacy, etc. is of interest. Importantly, the exact functional properties of novel bioactive molecules must show exclusive features and significant improvements compared with the known reports, since papers describing the effects of compounds with no advantages will not be accepted.

Prof. Dr. Qingyong Li
Guest Editor

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. Molecules is an international peer-reviewed open access semimonthly 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 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

  • new drugs
  • new compounds
  • new targets
  • new mechanism
  • pharmacokinetics
  • improved formulation and efficacy

Published Papers (2 papers)

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Research

16 pages, 1511 KiB  
Article
Anti-Candida and Anti-Leishmanial Activities of Encapsulated Cinnamomum verum Essential Oil in Chitosan Nanoparticles
by Rym Essid, Ameni Ayed, Kais Djebali, Houda Saad, Mondher Srasra, Yasmine Othmani, Nadia Fares, Selim Jallouli, Islem Abid, Monerah Rashed Alothman, Ferid Limam and Olfa Tabbene
Molecules 2023, 28(15), 5681; https://doi.org/10.3390/molecules28155681 - 27 Jul 2023
Cited by 2 | Viewed by 1297
Abstract
Nanoencapsulation is widely considered as a highly effective strategy to enhance essential oils’ (EO) stability by protecting them from oxidative deterioration and evaporation. The present study aims to optimize and characterize an efficient technique for encapsulating Cinnamomum (C.) verum essential oil into chitosan [...] Read more.
Nanoencapsulation is widely considered as a highly effective strategy to enhance essential oils’ (EO) stability by protecting them from oxidative deterioration and evaporation. The present study aims to optimize and characterize an efficient technique for encapsulating Cinnamomum (C.) verum essential oil into chitosan nanoparticles using response surface methodology (RSM). Moreover, the optimized C. verum EO nanoparticle was investigated for its antibacterial (against Gram-positive and Gram-negative bacteria), antifungal (against Candida albicans), and antiparasitic activity (against Leishmania parasites). Five parameters were investigated using a Plackett–Burman and Box–Behnken statistical design: the chitosan molecular weight, TPP concentration, C. verum EO/chitosan ratio, mixing method, and the duration of the reaction. Encapsulation efficiency and anti-candida activity were considered as responses. The antibacterial, anticandidal, and anti-leishmanial activities were also assessed using a standard micro-broth dilution assay and the cytotoxicity assay was assessed against the macrophage cell line RAW 264.7. The optimized nanoparticles were characterized using Fourier transform infrared spectroscopy, Zeta potential, and scanning electron microscopy. The study results indicated that under optimal conditions, the nanoencapsulation of C. verum EO into chitosan nanoparticles resulted in an encapsulation efficiency of 92.58%, with a regular distribution, a nanoparticle size of 480 ± 14.55 nm, and a favorable Zeta potential of 35.64 ± 1.37 mV. The optimized C. verum EO/chitosan nanoparticles showed strong antifungal activity against C. albicans pathogens (CMI = 125 µg mL−1), notable antibacterial activity against both Gram-positive and Gram-negative bacteria (ranging from 125 to 250 µg mL−1), high leishmanicidal potential against the promastigotes form of L. tropica and L. major (IC50 = 10.47 and 15.09 µg mL−1, respectively), and a four-fold cytotoxicity reduction compared to non-encapsulated essential oil. These results suggest that C. verum EO-loaded chitosan nanoparticles could be a promising delivery system for the treatment of cutaneous Candida albicans infections. Full article
(This article belongs to the Special Issue Development of New Drugs from Bioactive Compounds)
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14 pages, 769 KiB  
Article
Assessing Boron-Pleuromutilin AN11251 for the Development of Antibacterial Agents
by Ming-Jie Han, Miaomiao Pan, Genhui Xiao, Ying Yuan, Shawn Chen and Zhiyang Zou
Molecules 2023, 28(12), 4628; https://doi.org/10.3390/molecules28124628 - 8 Jun 2023
Viewed by 1191
Abstract
Pleuromutilins are a group of antibiotics derived from the naturally occurring compound. The recent approval of lefamulin for both intravenous and oral doses in humans to treat community-acquired bacterial pneumonia has prompted investigations in modifying the structure to broaden the antibacterial spectrum, enhance [...] Read more.
Pleuromutilins are a group of antibiotics derived from the naturally occurring compound. The recent approval of lefamulin for both intravenous and oral doses in humans to treat community-acquired bacterial pneumonia has prompted investigations in modifying the structure to broaden the antibacterial spectrum, enhance the activity, and improve the pharmacokinetic properties. AN11251 is a C(14)-functionalized pleuromutilin with a boron-containing heterocycle substructure. It was demonstrated to be an anti-Wolbachia agent with therapeutic potential for Onchocerciasis and lymphatic filariasis. Here, the in vitro and in vivo PK parameters of AN11251 were measured including PPB, intrinsic clearance, half-life, systemic clearance, and volume of distribution. The results indicate that the benzoxaborole-modified pleuromutilin possesses good ADME and PK properties. AN11251 has potent activities against the Gram-positive bacterial pathogens tested, including various drug-resistant strains, and against the slow-growing mycobacterial species. Finally, we employed PK/PD modeling to predict the human dose for treatment of disease caused by Wolbachia, Gram-positive bacteria, or Mycobacterium tuberculosis, which might facilitate the further development of AN11251. Full article
(This article belongs to the Special Issue Development of New Drugs from Bioactive Compounds)
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