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Enzyme Inhibitions of New Synthetic or Natural Organic Compounds: Synthesis...
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Enzyme Inhibitions of New Synthetic or Natural Organic Compounds: Synthesis and Biologic Activity—A Themed Issue in Honor of Prof. Dr. İlhami GÜLÇİN’s Contribution

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

Deadline for manuscript submissions: closed (30 October 2023) | Viewed by 2584

Special Issue Editors

Prof. Dr. Ilhami Gulcin

E-Mail Website
Guest Editor
Department of Chemistry, Faculty of Science, Ataturk University, Erzurum 25240, Turkey
Interests: antioxidant; bioactive compounds; bioorganic chemistry; enzyme inhibition
Dr. Ercan Bursal

E-Mail Website
Guest Editor
Department of Nursing, Faculty of Health, Mus Alparslan University, Muş 49100, Turkey
Interests: bioactive compounds; enzyme inhibition; food; medicinal chemistry; nutrition; organic compounds

Special Issue Information

Dear Colleagues,

Synthetic and natural compounds have been considered major sources of drugs. The recent studies were focused to isolate compounds from natural sources or to synthesize new organic compounds to be the new drug candidates which could be safer with having lower side effects.

Enzymes have received great attention in recent studies due to their critical roles in metabolism. Inhibition and activity determination studies on these enzymes are becoming more and more popular. Inhibitors of different enzymes are used as drugs in the treatment of several diseases. For instance, acetylcholinesterase and butyrylcholinesterase for Alzheimer’s disease, glycosidase and amylase for Diabetes mellitus, Glutathione S-transferase for the detoxification process, tyrosinase for skin problems, pancreatic lipase for the treatment of obesity and carbonic anhydrase for regulating pH and metabolism, etc.

The present Special Issue will gather the latest research studies in the investigation of new drug candidates from natural or synthetic sources, comprising synthesis, biological activity, and enzyme inhibition properties. By collecting the contributions of eminent scientists in the field, this Special Issue would be the main reference material in this field. We invite the authors to report a wide range of studies, including synthesis, in vitro, in vivo, and in silico enzyme inhibition studies of synthetic and natural compounds. Also, we welcome the submission of both original research articles and review articles on organic synthesis, medicinal chemistry, food chemistry, chemical biology, biochemistry, and biotechnology areas.

Prof. Dr. Ilhami Gulcin
Dr. Ercan Bursal
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. 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

  • acetylcholinesterase
  • biochemistry
  • carbonic anhydrase
  • computational modeling
  • chemical compounds
  • drug discovery
  • enzyme kinetics
  • enzyme inhibition
  • glutathione S-transferase
  • glycosidase
  • molecular docking
  • organic compounds
  • structural biology
  • structure-activity relationship
  • synthesis

Published Papers (2 papers)

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Research

11 pages, 2824 KiB  
Article
Ureidobenzenesulfonamides as Selective Carbonic Anhydrase I, IX, and XII Inhibitors
by Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran and René Csuk
Molecules 2023, 28(23), 7782; https://doi.org/10.3390/molecules28237782 - 26 Nov 2023
Cited by 3 | Viewed by 758
Abstract
Sulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby, [...] Read more.
Sulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby, biphenyl- and benzylphenyl-substituted sulfonamides showed high selectivity against hCA IX and hCA XII; these enzymes are common targets in the treatment of hypoxic cancers, and noteworthy inhibitory activity was observed for several compounds toward hCA I that might be of interest for future applications to treat cerebral edema. Compound 3 (4-[3-(2-benzylphenyl)ureido]benzenesulfonamide) held an exceptionally low Ki value of 1.0 nM for hCA XII. Full article
(This article belongs to the Special Issue Enzyme Inhibitions of New Synthetic or Natural Organic Compounds: Synthesis and Biologic Activity—A Themed Issue in Honor of Prof. Dr. İlhami GÜLÇİN’s Contribution)
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17 pages, 2114 KiB  
Article
In Vitro and In Silico Evaluation of Anticholinesterase and Antidiabetic Effects of Furanolabdanes and Other Constituents from Graptophyllum pictum (Linn.) Griffith
by Nathalie Tanko Metiefeng, Alfred Ngenge Tamfu, Maurice Fotsing Tagatsing, Turibio Kuiate Tabopda, Selcuk Kucukaydin, Martin Noah Mbane, Alex de Theodore Atchade, Emmanuel Talla, Celine Henoumont, Sophie Laurent, El Hassane Anouar and Rodica Mihaela Dinica
Molecules 2023, 28(12), 4802; https://doi.org/10.3390/molecules28124802 - 16 Jun 2023
Cited by 3 | Viewed by 1387
Abstract
Graptophyllum pictum is a tropical plant noticeable for its variegated leaves and exploited for various medicinal purposes. In this study, seven compounds, including three furanolabdane diterpenoids, i.e., Hypopurin E, Hypopurin A and Hypopurin B, as well as with Lupeol, β-sitosterol 3-O-β- [...] Read more.
Graptophyllum pictum is a tropical plant noticeable for its variegated leaves and exploited for various medicinal purposes. In this study, seven compounds, including three furanolabdane diterpenoids, i.e., Hypopurin E, Hypopurin A and Hypopurin B, as well as with Lupeol, β-sitosterol 3-O-β-d-glucopyranoside, stigmasterol 3-O-β-d-glucopyranoside and a mixture of β-sitosterol and stigmasterol, were isolated from G. pictum, and their structures were deduced from ESI-TOF-MS, HR-ESI-TOF-MS, 1D and 2D NMR experiments. The compounds were evaluated for their anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BchE), as well as their antidiabetic potential through inhibition of α-glucosidase and α-amylase. For AChE inhibition, no sample had IC50 within tested concentrations, though the most potent was Hypopurin A, which had a percentage inhibition of 40.18 ± 0.75%, compared to 85.91 ± 0.58% for galantamine, at 100 µg/mL. BChE was more susceptible to the leaves extract (IC50 = 58.21 ± 0.65 µg/mL), stem extract (IC50 = 67.05 ± 0.82 µg/mL), Hypopurin A (IC50 = 58.00 ± 0.90 µg/mL), Hypopurin B (IC50 = 67.05 ± 0.92 µg/mL) and Hypopurin E (IC50 = 86.90 ± 0.76 µg/mL). In the antidiabetic assay, the furanolabdane diterpenoids, lupeol and the extracts had moderate to good activities. Against α-glucosidase, lupeol, Hypopurin E, Hypopurin A and Hypopurin B had appreciable activities but the leaves (IC50 = 48.90 ± 0.17 µg/mL) and stem (IC50 = 45.61 ± 0.56 µg/mL) extracts were more active than the pure compounds. In the α-amylase assay, stem extract (IC50 = 64.47 ± 0.78 µg/mL), Hypopurin A (IC50 = 60.68 ± 0.55 µg/mL) and Hypopurin B (IC50 = 69.51 ± 1.30 µg/mL) had moderate activities compared to the standard acarbose (IC50 = 32.25 ± 0.36 µg/mL). Molecular docking was performed to determine the binding modes and free binding energies of Hypopurin E, Hypopurin A and Hypopurin B in relation to the enzymes and decipher the structure–activity relationship. The results indicated that G. pictum and its compounds could, in general, be used in the development of therapies for Alzheimer’s disease and diabetes. Full article
(This article belongs to the Special Issue Enzyme Inhibitions of New Synthetic or Natural Organic Compounds: Synthesis and Biologic Activity—A Themed Issue in Honor of Prof. Dr. İlhami GÜLÇİN’s Contribution)
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