Cyclic Peptides in Pipeline: What Future for These Great Molecules?

Pharmaceuticals, Год журнала: 2023, Номер 16(7), С. 996 - 996

Опубликована: Июль 12, 2023

Cyclic peptides are molecules that already used as drugs in therapies approved for various pharmacological activities, example, antibiotics, antifungals, anticancer, and immunosuppressants. Interest these has been growing due to the improved pharmacokinetic pharmacodynamic properties of cyclic structure over linear by evolution chemical synthesis, computational, vitro methods. To date, 53 have different regulatory authorities, many others clinical trials a wide diversity conditions. In this review, potential is presented, general aspects their synthesis development discussed. Furthermore, an overview also given, summarized.

Язык: Английский

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Marine Cyclic Peptides: Antimicrobial Activity and Synthetic Strategies

Marine Drugs, Год журнала: 2022, Номер 20(6), С. 397 - 397

Опубликована: Июнь 15, 2022

Oceans are a rich source of structurally unique bioactive compounds from the perspective potential therapeutic agents. Marine peptides particularly interesting group secondary metabolites because their chemistry and wide range biological activities. Among them, cyclic exhibit broad spectrum antimicrobial activities, including against bacteria, protozoa, fungi, viruses. Moreover, there several examples marine revealing activities numerous drug-resistant bacteria making these very promising resource in search for novel agents to revert multidrug-resistance. This review summarizes 174 with antibacterial, antifungal, antiparasitic, or antiviral properties. These natural products were categorized according sources—sponges, mollusks, crustaceans, crabs, fungi—and chemical structure—cyclic depsipeptides. The microorganisms, unusual structural characteristics, hits more advanced (pre)clinical studies, highlighted. Nocathiacins I–III (91–93), unnarmicins A (114) C (115), sclerotides (160) B (161), plitidepsin (174) can be highlighted considering not only high potency vitro, but also vivo results. models molecular modifications and/or total synthesis obtain potent compounds, improved properties higher quantity. Solid-phase Fmoc- Boc-protection is major synthetic strategy properties, key presented guiding microbiologist medicinal chemists discovery new drug candidates sources.

Язык: Английский

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Presence of polyketide synthases and nonribosomal peptide synthetase in culturable bacteria associated with Aplysina fulva and Aplysina caissara (Porifera)

Brazilian Journal of Microbiology, Год журнала: 2025, Номер unknown

Опубликована: Янв. 10, 2025

Язык: Английский

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Absolute Stereochemistry Determination of Bioactive Marine-Derived Cyclopeptides by Liquid Chromatography Methods: An Update Review (2018–2022)

Molecules, Год журнала: 2023, Номер 28(2), С. 615 - 615

Опубликована: Янв. 7, 2023

Cyclopeptides are considered as one of the most important classes compounds derived from marine sources, due to their structural diversity and a myriad biological pharmacological activities. Since marine-derived cyclopeptides consist different amino acids, many which non-proteinogenic, they possess various stereogenic centers. In this respect, structure elucidation new molecular scaffolds obtained natural including cyclopeptides, can become very challenging task. The determination absolute configurations acid residues is accomplished, in cases, by performing acidic hydrolysis, followed analyses liquid chromatography (LC). continuation with authors’ previous publication, analyze current trends, present review covers recently published works (from January 2018 November 2022) regarding organisms, special focus on biological/pharmacological activities stereochemical assignment residues. Ninety-one unreported were identified during period, displayed anticancer or antimicrobial Marfey’s method, involves LC, was found be frequently used for purpose.

Язык: Английский

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The natural products discovered in marine sponge-associated microorganisms: structures, activities, and mining strategy

Frontiers in Marine Science, Год журнала: 2023, Номер 10

Опубликована: Май 19, 2023

It is well known that microorganisms are abundant in sponges, which make up 50%-60% of the host biomass. Moreover, mounting evidence suggests bacteria, fungi, and cyanobacteria, all associated with true creators bioactive compounds identified from sponges. The discovery 774 structurally active 1998 to 2017 presents a good overview natural product resources sponge-associated microorganisms. During last 5 years, many new molecules, including peptides, polyketides, alkaloids, terpenes, have been through various mining strategies, exhibiting wide range biological activities, such as anti-microbial, anti-cancer, enzyme inhibition, antioxidant properties. In this paper, 140 produced by 2022 systematically discussed terms their structures, strain sources, not only further updates library but also provides guideline for exploring “dark matter”

Язык: Английский

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Marine sponges as promising candidates for integrated aquaculture combining biomass increase and bioremediation: an updated review

Frontiers in Marine Science, Год журнала: 2024, Номер 10

Опубликована: Янв. 31, 2024

Sponge farming has been experimentally performed for more than 100 years, with early attempts mainly devoted the supply of bath sponges and ornamental purposes. During last decades, sponge proposed to produce biomass specifically those species from which many structurally diverse bioactive compounds were isolated, frequently present in a low concentration that limits their commercial production. This point is very important because it offers an environmental-friendly approach use as source natural pharmacological, cosmeceutical, nutraceutical industries. In addition, can have ecological role filter-feeding animals great significance marine benthic communities. Thanks aquiferous system, they filter large amounts sea water, retaining up 80% suspended particles, resulting good system bioremediate environment different contaminants. Remarkably, few at integrating aquaculture systems by combining increase bioremediation, showing impressive results opening new possibilities sector. review concerns both situ lab-based methods production sponge-related bioremediation focusing on microorganisms contaminants (heavy metals, pesticides, microplastics, others). Moreover, first overview about integrated challenging perspective biotechnologies, included.

Язык: Английский

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A comprehensive review of marine sponge metabolites, with emphasis on Neopetrosia sp.

International Journal of Biological Macromolecules, Год журнала: 2024, Номер unknown, С. 135823 - 135823

Опубликована: Сен. 1, 2024

Язык: Английский

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Purification and biochemical characterization of SM14est, a PET-hydrolyzing enzyme from the marine sponge-derived Streptomyces sp. SM14

Frontiers in Microbiology, Год журнала: 2023, Номер 14

Опубликована: Май 12, 2023

The successful enzymatic degradation of polyester substrates has fueled worldwide investigation into the treatment plastic waste using bio-based processes. Within this realm, marine-associated microorganisms have emerged as a promising source polyester-degrading enzymes. In work, we describe hydrolysis synthetic polymer PET by SM14est, polyesterase which was previously identified from Streptomyces sp. SM14, an isolate marine sponge Haliclona simulans. hydrolase activity purified SM14est assessed suspension-based assay and subsequent analysis reaction products UV-spectrophotometry RP-HPLC. displayed preference for high salt conditions, with significantly increasing at sodium chloride concentrations 100 mM up to 1,000 mM. initial rate determined be 0.004 s-1 45°C, increased 5-fold 0.02 upon addition 500 chloride. Sequence alignment structural comparison known hydrolases, including halophile PET6, highly efficient, thermophilic PHL7, revealed conserved features interest. Based on emerges useful enzyme that is more similar key players in area hydrolysis, like PHL7 IsPETase, than it its counterparts. Salt-tolerant polyesterases such are potentially valuable biological particles readily contaminate ecosystems industrial wastewaters.

Язык: Английский

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Polyketides with Cardioprotective Bioactivities from Sponge-Associated Fungus Aspergillus giganteus MA46-5

Molecules, Год журнала: 2025, Номер 30(7), С. 1632 - 1632

Опубликована: Апрель 6, 2025

One pair of novel enantiomers, gigantdioxin A (+)-1 and B (−)-1, with a skeleton benzo[d][1,3]dioxin; new acetophenone gigantone (3); known 3-chlorogentisyl alcohol (2), which is the bioprecursor 1; (4); chromone derivative (5) were obtained from sponge-associated fungus Aspergillus giganteus MA46-5. Their structures established by extensive in-depth spectral analysis, such as UV, 1D 2D NMR, HRESIMS. The absolute configurations (±)-1 deduced ORD, chiral separation, experimental computational ECD. Meanwhile, we proposed possible biosynthetic pathway (±)-1. Fortunately, was proved biomimetic synthesis through 2, bioprecursor, reacted n-butyraldehyde. Myocardial protection assays showed that 3 4 possessed stronger protective effects than positive control against myocardial cell H9c2 ischemia–reperfusion injury in low concentrations, effect (−)-1 almost equal to control. Further, explored mechanism network pharmacology. Adenosine A2a receptor (ADORA2A) serum albumin (ALB) represent potential targets for associated 4, respectively. Based on pharmacology, docked predicted proteins bioactive compounds using Autodock Vina.

Язык: Английский

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Therapeutic Potential of Marine-Derived Cyclic Peptides as Antiparasitic Agents

Marine Drugs, Год журнала: 2023, Номер 21(12), С. 609 - 609

Опубликована: Ноя. 25, 2023

Parasitic diseases still compromise human health. Some of the currently available therapeutic drugs have limitations considering their adverse effects, questionable efficacy, and long treatment, which encouraged drug resistance. There is an urgent need to find new, safe, effective, affordable antiparasitic drugs. Marine-derived cyclic peptides been increasingly screened as candidates for developing new Therefore, in this review, a systematic analysis scientific literature was performed 25 marine-derived with activity (1–25) were found. Antimalarial most reported (51%), followed by antileishmanial (27%) antitrypanosomal (20%) activities. compounds showed promising at nM scale, being active against various parasites. The mechanisms action targets some investigated, revealing different strategies

Язык: Английский

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