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Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II

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

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 13907

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Dr. Simone Carradori

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Guest Editor

Department of Pharmacy, University “G. d'Annunzio” of Chieti-Pescara, Chieti, Italy
Interests: chemical modification of natural compounds; medicinal chemistry; food chemistry; antioxidants; antimicrobials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

After the important success obtained with the first edition, I accepted an invitation to serve as the Guest Editor for the Special Issue, "Natural Products and their Semi-Synthetic Derivatives Against Bacteria, Fungi and Parasites II”, of the journal Molecules (ISSN 1420-3049 https://www.mdpi.com/journal/molecules). In this regard, I would be pleased if you would agree to contribute an original research paper, short communication, or focus review to this Issue. Provided below is some information that you may find useful in your consideration of this invitation.

This Special Issue will collect and disseminate the most significant and recent contributions in the interdisciplinary area of medicinal chemistry, microbiology, food chemistry, pharmacology, and pharmacognosy, with a particular emphasis on (biotechnological) production, isolation and characterization, biological effects, uses, and the analysis of semi-synthetic and natural products. The main applications of these natural active compounds must be strictly focused on microbial (bacterial, fungal, and viral) infections, parasite disease eradication and prevention, food contamination and preservation, inhibition of biofilm production and resistance development, herbal formulations with a specific chemical profile, new mechanisms of action, new targets to be explored, structure–activity elucidation, and chemically modified natural compounds with improved biological activity or pharmacokinetics. The biological activity of complex natural extracts without a proper chemical characterization or the evaluation of the most representative active compounds will not be considered.

Dr. Simone Carradori
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

Medicinal chemistry
Antimicrobial agents
Anti-parasitic agents
Anti-protozoan agents
Structure–activity relationships
Food contamination and preservation
Innovative (micro)extraction procedures
Synthetic derivatives inspired by natural scaffolds
Food and food supplements analyses
Pharmaco-toxicological activities
Physiological activities of food and food components
Uses of medicinal plants and fungi
Biofilm and resistance
Natural products chemistry and synthesis

Published Papers (7 papers)

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Research

14 pages, 4197 KiB

Open AccessArticle

Benzothiazole—An Antifungal Compound Derived from Medicinal Mushroom Ganoderma lucidum against Mango Anthracnose Pathogen Colletotrichum gloeosporioides (Penz and (Sacc.))

by Gayathri Muniyappan, Thiribhuvanamala Gurudevan, Praveen Thangaraj, Akshaya Subbaih Balamurali, Arumuka Pravin Iyadurai, Rajamanickam Suppaiah, Krishnamoorthy Akkanna Subbiah and Haripriya Shanmugam

Molecules 2023, 28(6), 2476; https://doi.org/10.3390/molecules28062476 - 08 Mar 2023

Cited by 2 | Viewed by 1509

Abstract

The present investigation is focused on exploring the possibilities of identifying biomolecules from the fruiting body of the medicinal mushroom Ganoderma lucidum against the mango anthracnose pathogen Colletotrichum gloeosporioides. The fruiting body (cap and stipe portion) of G. lucidum extracted with ethyl acetate solvent at a maximum inhibitory concentration of 1 percent exhibited the maximum mycelial growth inhibition of C. gloeosporioides with 70.10 percent and 40.77 percent, respectively. Furthermore, subjecting the ethyl acetate extracts from the cap portion of G. lucidum through thin layer chromatography (TLC) revealed the presence of two bands with Rf values of 0.38 and 0.35. The compounds eluted from band 1 recorded with the maximum mycelial growth inhibition of C. gloeosporioides by 53.77 percent followed by band 2 (46.33 percent) using an agar well diffusion test. Similarly, the analysis of ethyl acetate extracts from the cap portion of G. lucidum through Gas Chromatography-Mass spectroscopy (GC-MS) revealed the presence of the organoheterocyclic compound benzothiazole, as expressed in the highest peak area at 22.03 RT with the highest probability percentage (97%). Confirmation of the antifungal nature of benzothiazole was obtained by testing the standard sample of benzothiazole which showed a cent percent of inhibition on mycelial growth of C. gloeosporioides at 50 ppm minimum fungicidal concentration. Furthermore, benzothiazole caused abnormality in the mycelial structures, viz., distortion, shrinkage, clumping of mycelium, conidial malformation, and complete arrestment of conidial germination of C. gloeosporioides as observed through Scanning Electron Microscopy. The research on biomolecular extract of G. lucidum could be a novel and interesting concept for the possibility in suppression of plant pathogenic microbes in the natural field. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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18 pages, 1965 KiB

Open AccessArticle

N-Containing α-Mangostin Analogs via Smiles Rearrangement as the Promising Cytotoxic, Antitrypanosomal, and SARS-CoV-2 Main Protease Inhibitory Agents

by Nan Yadanar Lin Pyae, Arnatchai Maiuthed, Wongsakorn Phongsopitanun, Bongkot Ouengwanarat, Warongrit Sukma, Nitipol Srimongkolpithak, Jutharat Pengon, Roonglawan Rattanajak, Sumalee Kamchonwongpaisan, Zin Zin Ei, Preedakorn Chunhacha, Patcharin Wilasluck, Peerapon Deetanya, Kittikhun Wangkanont, Kowit Hengphasatporn, Yasuteru Shigeta, Thanyada Rungrotmongkol and Supakarn Chamni

Molecules 2023, 28(3), 1104; https://doi.org/10.3390/molecules28031104 - 22 Jan 2023

Cited by 2 | Viewed by 2269

Abstract

New N-containing xanthone analogs of α-mangostin were synthesized via one-pot Smiles rearrangement. Using cesium carbonate in the presence of 2-chloroacetamide and catalytic potassium iodide, α-mangostin (1) was subsequently transformed in three steps to provide ether 2, amide 3, and amine 4 in good yields at an optimum ratio of 1:3:3, respectively. The evaluation of the biological activities of α-mangostin and analogs 2–4 was described. Amine 4 showed promising cytotoxicity against the non-small-cell lung cancer H460 cell line fourfold more potent than that of cisplatin. Both compounds 3 and 4 possessed antitrypanosomal properties against Trypanosoma brucei rhodesiense at a potency threefold stronger than that of α-mangostin. Furthermore, ether 2 gave potent SARS-CoV-2 main protease inhibition by suppressing 3-chymotrypsinlike protease (3CL^pro) activity approximately threefold better than that of 1. Fragment molecular orbital method (FMO–RIMP2/PCM) indicated the improved binding interaction of 2 in the 3CL^pro active site regarding an additional ether moiety. Thus, the series of N-containing α-mangostin analogs prospectively enhance druglike properties based on isosteric replacement and would be further studied as potential biotically active chemical entries, particularly for anti-lung-cancer, antitrypanosomal, and anti-SARS-CoV-2 main protease applications. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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11 pages, 3302 KiB

Open AccessArticle

Emulsifying Properties of Rhamnolipids and Their In Vitro Antifungal Activity against Plant Pathogenic Fungi

by Dongmei Li, Weiyi Tao, Dinghua Yu and Shuang Li

Molecules 2022, 27(22), 7746; https://doi.org/10.3390/molecules27227746 - 10 Nov 2022

Cited by 5 | Viewed by 1260

Abstract

Rhamnolipids have significant emulsifying activity and the potential to become a component of pesticide emulsifier. Rhamnolipids are usually composed of two main components: mono-rhamnolipids (Rha-C₁₀-C₁₀) and di-rhamnolipids (Rha₂-C₁₀-C₁₀). The proportion of di-rhamnolipids in the products ranged between 15% and 90%, affected by the production strains and fermentation process. In this paper, three kinds of rhamnolipid products containing di-rhamnolipids proportions, of 25.45, 46.46 and 89.52%, were used to test their emulsifying ability toward three conventional solvents used in pesticide (S-200, xylene, cyclohexanone) and antifungal activities against five strains of plant pathogenic fungi (Phytophthora capsici, Phytophthora parasitica var.nicotianae, Colletotrichum destructivum, Colletotrichum sublineolum, Fusarium oxysporum). The results indicated that although the CMC of the three rhamnolipids were significantly different, their emulsification properties had no remarkable differences, at a concentration of 10 g/L. However, their antifungal activities were significantly different: the more di-rhamnolipids, the stronger the antifungal activity. This work helps to promote the application of rhamnolipids as pesticides adjuvants. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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17 pages, 3621 KiB

Open AccessArticle

Synthesis and Antifungal Activity of New butenolide Containing Methoxyacrylate Scaffold

by Qian Zhang, Yihao Li, Bin Zhao, Leichuan Xu, Haoyun Ma and Mingan Wang

Molecules 2022, 27(19), 6541; https://doi.org/10.3390/molecules27196541 - 03 Oct 2022

Cited by 1 | Viewed by 1237

Abstract

In order to improve the antifungal activity of new butenolides containing oxime ether moiety, a series of new butenolide compounds containing methoxyacrylate scaffold were designed and synthesized, based on the previous reports. Their structures were characterized by ¹H NMR, ¹³C NMR, HR-MS spectra, and X-ray diffraction analysis. The in vitro antifungal activities were evaluated by the mycelium growth rate method. The results showed that the inhibitory activities of these new compounds against Sclerotinia sclerotiorum were significantly improved, in comparison with that of the lead compound 3–8; the EC₅₀ values of V-6 and VI-7 against S. sclerotiorum were 1.51 and 1.81 mg/L, nearly seven times that of 3–8 (EC₅₀ 10.62 mg/L). Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) observation indicated that compound VI-3 had a significant impact on the structure and function of the hyphal cell of S. sclerotiorum mycelium and the positive control trifloxystrobin. Molecular simulation docking results indicated that the introduction of methoxyacrylate scaffold is beneficial to improving the antifungal activity of these compounds against S. sclerotiorum, which can be used as the lead for further structure optimization. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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15 pages, 4937 KiB

Open AccessArticle

In Silico Screening of Quorum Sensing Inhibitor Candidates Obtained by Chemical Similarity Search

by Sharath Belenahalli Shekarappa, Hrvoje Rimac and Julian Lee

Molecules 2022, 27(15), 4887; https://doi.org/10.3390/molecules27154887 - 30 Jul 2022

Cited by 1 | Viewed by 1680

Abstract

Quorum sensing (QS) is a bacterial communication using signal molecules, by which they sense population density of their own species, leading to group behavior such as biofilm formation and virulence. Autoinducer-2 (AI2) is a QS signal molecule universally used by both gram-positive and gram-negative bacteria. Inhibition of QS mediated by AI2 is important for various practical applications, including prevention of gum-disease caused by biofilm formation of oral bacteria. In this research, molecular docking and molecular dynamics (MD) simulations were performed for molecules that are chemically similar to known AI2 inhibitors that might have a potential to be quorum sensing inhibitors. The molecules that form stable complexes with the AI2 receptor protein were found, suggesting that they could be developed as a novel AI2 inhibitors after further in vitro validation. The result suggests that combination of ligand-based drug design and computational methods such as MD simulation, and experimental verification, may lead to development of novel AI inhibitor, with a broad range of practical applications. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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11 pages, 1209 KiB

Open AccessArticle

Pentacyclic Triterpenoids from Sabia discolor Dunn and Their α-Glycosidase Inhibitory Activities

by Jin-Hong Ma, Dan Hu, Lu-Lu Deng, Jiang Li, Xiao-Jiang Hao and Shu-Zhen Mu

Molecules 2022, 27(7), 2161; https://doi.org/10.3390/molecules27072161 - 27 Mar 2022

Cited by 3 | Viewed by 1651

Abstract

Four new pentacyclic triterpenoids named Sabiadiscolor A–D (1 and 7–9) together with eleven known ones were isolated by repeated column chromatography. Their structures were identified and characterized by NMR and MS spectral data as 6 oleanane-type pentacyclic triterpenoids (1–6), 7 ursane-type ones (7–13), and 2 lupanane-type ones (14–15). Except for compound 15, all other compounds were isolated from Sabia discolor Dunn for the first time. Their α-glycosidase inhibitory activities were evaluated, which showed that compounds 1, 3, 8, 9, 13, and 15 implied remarkable activities with IC₅₀ values ranging from 0.09 to 0.27 μM, and the preliminary structure–activity relationship was discussed. Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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19 pages, 1937 KiB

Open AccessArticle

Antifungal and Anti-Virulent Activity of Origanum majorana L. Essential Oil on Candida albicans and In Vivo Toxicity in the Galleria mellonella Larval Model

by Banu Kaskatepe, Sinem Aslan Erdem, Sukran Ozturk, Zehra Safi Oz, Eldan Subasi, Mehmet Koyuncu, Josipa Vlainić and Ivan Kosalec

Molecules 2022, 27(3), 663; https://doi.org/10.3390/molecules27030663 - 20 Jan 2022

Cited by 15 | Viewed by 2886

Abstract

The aim of this study was to investigate and compare in detail both the antifungal activity in vitro (with planktonic and biofilm-forming cells) and the essential oil composition (EOs) of naturally growing (OMN) and cultivated (OMC) samples of Origanum majorana L. (marjoram). The essential oil composition was analyzed using GC-MS. The major constituent of both EOs was carvacrol: 75.3% and 84%, respectively. Both essential oils showed high antifungal activity against clinically relevant Candida spp. with IC₅₀ and IC₉₀ less than or equal to 0.5 µg mL⁻¹ and inhibition of biofilm with a concentration of 3.5 µg mL⁻¹ or less. Cultivated marjoram oil showed higher anti-biofilm activity against C. albicans. In addition, OMC showed greater inhibition of germ-tube formation (inhibition by 83% in Spider media), the major virulence factor of C. albicans at a concentration of 0.125 µg mL⁻¹. Both EOs modulated cell surface hydrophobicity (CSH), but OMN proved to be more active with a CSH% up to 58.41%. The efficacy of O. majorana EOs was also investigated using Galleria mellonella larvae as a model. It was observed that while the larvae of the control group infected with C. albicans (6.0 × 10⁸ cells) and not receiving treatment died in the controls carried out after 24 h, all larvae in the infected treatment group survived at the end of the 96th hour. When the treatment group and the infected group were evaluated in terms of vital activities, it was found that the difference was statistically significant (p < 0.001). The infection of larvae with C. albicans and the effects of O. majorana EOs on the hemocytes of the model organism and the blastospores of C. albicans were evaluated by light microscopy on slides stained with Giemsa. Cytological examination in the treatment group revealed that C. albicans blastospores were phagocytosed and morphological changes occurred in hemocytes. Our results indicated that the essential oil of both samples showed strong antifungal activities against planktonic and biofilm-forming C. albicans cells and also had an influence on putative virulence factors (germ-tube formation and its length and on CSH). Full article

(This article belongs to the Special Issue Natural Products and Their Semi-synthetic Derivatives against Bacteria, Fungi, and Parasites II)

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