Bestatin and bacitracin inhibit porcine kidney cortex dipeptidyl peptidase IV activity and reduce human melanoma MeWo cell viability

Méndez, Laura Rivera; Arrebola, Yarini; Valdés‐Tresanco, Mario E.; Díaz-Guevara, Lisset; Bergado, Gretchen; Sánchez, Belinda; Charlí, Jean-Louis; Alonso, Isel Pascual

doi:10.1016/j.ijbiomac.2020.08.157

Cited by 16 publications

(8 citation statements)

References 59 publications

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“…2A, B). Bestatin is a well-characterized inhibitor of LTA 4 H and was shown to attenuate LTB 4 synthesis in several previous studies [30,31]. Inhibition of LTA 4 H level in mice with DMM-induced OA suppressed OA progression with a lower Mankin score (8.000 ± 1.095) compared to DMM-induced OA mice with vehicle (Fig.…”

Section: Inhibition Of Lta 4 H Level Suppressed Oa Progression In Articular Cartilagementioning

confidence: 75%

Inhibition of Leukotriene A4 Hydrolase Suppressed Cartilage Degradation and Synovial Inflammation in a Mouse Model of Experimental Osteoarthritis

Sun

Crawford

et al. 2022

Preprint

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Chronic inflammation plays an important role in the osteoarthritis (OA) pathology but how this influence OA disease progression is unclear. Leukotrienes (LT) are biologically active lipids that are implicated in various pathological process. Leukotriene B4 (LTB4) is a potent proinflammatory lipid mediator generated from arachidonic acid through the sequential activities of 5-lipoxygenase, 5-lipoxygenase–activating protein, Leukotriene A4 hydrolase (LTA4H) and its downstream product leukotriene B4 (LTB4 or BLT1). The aim of this study is to investigate the involvement of the LTB4 pathway in OA disease progression. Both clinical human samples and mice experimental OA models were used to determine whether LTA4H could serve as a potential therapeutic target for OA. We also determined whether the LTA4H pathway was associated with cartilage degeneration and synovitis inflammation in OA mice models and human articular chondrocytes. We found that both LTA4H and LTB4 receptor BLT1 were highly expressed in human and mice OA cartilage. Inhibition of LTA4H suppressed cartilage degeneration and synovitis in OA mice model. Furthermore, inhibition of LTA4H promoted cartilage regeneration by upregulating chondrogenic genes expression such as aggrecan (ACAN), collagen 2A1 (COL2A1) and SRY-Box transcription factor 9 (SOX9). Our results indicate that the LTA4H pathway is a crucial regulator of OA pathogenesis and suggest that LTA4H could be a therapeutic target in combat OA.

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Section: Inhibition Of Lta 4 H Level Suppressed Oa Progression In Articular Cartilagementioning

confidence: 75%

Inhibition of Leukotriene A4 Hydrolase Suppressed Cartilage Degradation and Synovial Inflammation in a Mouse Model of Experimental Osteoarthritis

Sun

Crawford

et al. 2022

Preprint

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“…Analyzing the countries where patent applications have been submitted, China stands out with the highest number of applications (91), followed by the United States (26), Japan (12), and Australia (14). Examining the country of the patent priority, China maintains the lead (96), followed by the United States (45), Korea (10), Japan (7), and Brazil (7) (Figure 4C and Supporting Information 1.1). These results correspond with the inventors of patents by region.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…To first understand the pharmaceutical significance of AMPs, it needs to be stressed that the use of peptide-based drugs has numerous advantages, such as high potency, selectivity, and low toxicity. − Peptides, compared to small-molecule drugs such as bestatin, bacitracin, vinblastine, and others, can be more specific for their target, so they have fewer side effects, and because of their short half-life are less likely to accumulate in tissues. − However, the development of peptide-based drugs also presents numerous limitations, such as metabolic instability due to cleavage by proteolytic enzymes and high sensitivity to physicochemical changes such as temperature and pH, poor absorption, and limited membrane permeability as a result of the presence of charge and hydrophilic or polar amino acids. Chemical modifications are the most common solutions to overcome these limitations at the expense of increasing production costs. , In addition, approving new drugs, in which peptides are not an exception, is a long process, usually requiring a minimum of 10 to 15 years and compliance with demanding regulatory standards. − In this sense, and despite the marked increase in clinical trials using peptides during the last two decades, , the number of studies at this stage is deficient, especially when considering the exponential ratio in which new AMPs are described yearly. ,, To make the matter more complicated, about 40% of the AMP-based drugs in clinical trials are of human origin, often leading to the development of endogenous resistance mechanisms. , Thus, AMPs from other natural sources, such as microorganisms, insects, marine organisms, and amphibians, represent promising avenues of pharmaceutical investigation (Table , Figure ).…”

Section: Introductionmentioning

confidence: 99%

A Comprehensive Review of Patented Antimicrobial Peptides from Amphibian Anurans

García,

Fuentes,

Alonso

et al. 2024

J. Nat. Prod.

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Since the 1980s, studies of antimicrobial peptides (AMPs) derived from anuran skin secretions have unveiled remarkable structural diversity and a wide range of activities. This study explores the potential of these peptides for drug development by examining granted patents, amino acid modifications related to patented peptides, and recent amphibians' taxonomic updates influencing AMP names. A total of 188 granted patents related to different anuran peptides were found, with Asia and North America being the predominant regions, contributing 65.4% and 15.4%, respectively. Conversely, although the Neotropical region is the world's most diversified region for amphibians, it holds only 3.7% of the identified patents. The antimicrobial activities of the peptides are claimed in 118 of these 188 patents. Additionally, for 160 of these peptides, 66 patents were registered for the natural sequence, 69 for both natural and derivative sequences, and 20 exclusively for sequence derivatives. Notably, common modifications include alterations in the side chains of amino acids and modifications to the peptides' N-and C-termini. This review underscores the biomedical potential of anuran-derived AMPs, emphasizing the need to bridge the gap between AMP description and practical drug development while highlighting the urgency of biodiversity conservation to facilitate biomedical discoveries.

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“…Supernatants of these strains were also treated with α-amylase, and showed 50% residual activity [ 63 ]. In addition, the possible production of bacitracin could inhibit proteinase K [ 64 ] as it is known to be capable of protease inhibition [ 65 ].…”

Section: Discussionmentioning

confidence: 99%

Inhibitory Effect of Bacillus licheniformis Strains Isolated from Canine Oral Cavity

Hudáková

Kačírová

Sondorová

et al. 2022

Life

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Bacillus licheniformis is used in a broad spectrum of areas, including some probiotic preparations for human and veterinary health. Moreover, B. licheniformis strains are known producers of various bioactive substances with antimicrobial and antibiofilm effects. In searching for new potentially beneficial bacteria for oral health, the inhibitory effect of B. licheniformis strains isolated from canine dental biofilm against pathogenic oral bacteria was evaluated. The antimicrobial effect of neutralized cell-free supernatants (nCFS) was assessed in vitro on polystyrene microtiter plates. Furthermore, molecular and morphological analyses were executed to evaluate the production of bioactive substances. To determine the nature of antimicrobial substance present in nCFS of B. licheniformis A-1-5B-AP, nCFS was exposed to the activity of various enzymes. The nCFS of B. licheniformis A-1-5B-AP significantly (p < 0.0001) reduced the growth of Porphyromonas gulae 3/H, Prevotella intermedia 1/P and Streptococcus mutans ATCC 35668. On the other hand, B. licheniformis A-2-11B-AP only significantly (p < 0.0001) inhibited the growth of P. intermedia 1/P and S. mutans ATCC 35668. However, enzyme-treated nCFS of B. licheniformis A-1-5B-AP did not lose its antimicrobial effect and significantly (p < 0.0001) inhibited the growth of Micrococcus luteus DSM 1790. Further studies are needed for the identification of antimicrobial substances.

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Bestatin and bacitracin inhibit porcine kidney cortex dipeptidyl peptidase IV activity and reduce human melanoma MeWo cell viability

Cited by 16 publications

References 59 publications

Inhibition of Leukotriene A4 Hydrolase Suppressed Cartilage Degradation and Synovial Inflammation in a Mouse Model of Experimental Osteoarthritis

Inhibition of Leukotriene A4 Hydrolase Suppressed Cartilage Degradation and Synovial Inflammation in a Mouse Model of Experimental Osteoarthritis

A Comprehensive Review of Patented Antimicrobial Peptides from Amphibian Anurans

Inhibitory Effect of Bacillus licheniformis Strains Isolated from Canine Oral Cavity

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