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Lipidated cyclic ?-AApeptides display both antimicrobial and anti-inflammatory activity.

ABSTRACT: Antimicrobial peptides (AMPs) are host-defense agents capable of both bacterial membrane disruption and immunomodulation. However, the development of natural AMPs as potential therapeutics is hampered by their moderate activity and susceptibility to protease degradation. Herein we report lipidated cyclic ?-AApeptides that have potent antibacterial activity against clinically relevant Gram-positive and Gram-negative bacteria, many of which are resistant to conventional antibiotics. We show that lipidated cyclic ?-AApeptides mimic the bactericidal mechanism of AMPs by disrupting bacterial membranes. Interestingly, they also harness the immune response and inhibit lipopolysaccharide (LPS) activated Toll-like receptor 4 (TLR4) signaling, suggesting that lipidated cyclic ?-AApeptides have dual roles as novel antimicrobial and anti-inflammatory agents.

SUBMITTER: Li Y

PROVIDER: S-EPMC3947011 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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Lipidated cyclic γ-AApeptides display both antimicrobial and anti-inflammatory activity.

Li Yaqiong Y Smith Christina C Wu Haifan H Padhee Shruti S Manoj Namitha N Cardiello Joseph J Qiao Qiao Q Cao Chuanhai C Yin Hang H Cai Jianfeng J

ACS chemical biology 20131101 1

Antimicrobial peptides (AMPs) are host-defense agents capable of both bacterial membrane disruption and immunomodulation. However, the development of natural AMPs as potential therapeutics is hampered by their moderate activity and susceptibility to protease degradation. Herein we report lipidated cyclic γ-AApeptides that have potent antibacterial activity against clinically relevant Gram-positive and Gram-negative bacteria, many of which are resistant to conventional antibiotics. We show that l ...[more]

PMID: 24144063

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Project description:Conventional therapeutic agents used for treatment of Acne are associated with various adverse effects necessitating development of safe and effective alternative therapeutic agents. In this context, a polyherbal formulation AHPL/AYCAP/0413 was developed for treatment of Acne.To evaluate Anti-inflammatory and antimicrobial activity of AHPL/AYCAP/0413.1) Anti-inflammatory activity: Anti-inflammatory activity of AHPL/AYCAP/0413 in comparison with Diclofenac was assessed in carrageenan induced rat Paw edema model. 2) Anti-microbial activity for P. acne: Propionibacterium acnes were incubated under anaerobic conditions. Aliquots of molten BHI with glucose agar were used as the agar base. Formulation and clindamycin (10 μg/ml) were introduced in to the Agar wells randomly. 3) Anti-microbial activity for Staphylococcus epidermidis and Staphylococcus aureus: Staphylococcus epidermidis and Staphylococcus aureus were incubated under aerobic conditions at 37°C. TSB with glucose agar was used as the agar base. 0.5ml of formulation and clindamycin (10 μg/ml) were introduced in to the wells randomly. The antibacterial activity was evaluated by measuring zones of inhibition (in mm).Significant reduction in rat paw edema (51% inhibition) was observed with formulation AHPL/AYCAP/0413 which was also comparable to that of Diclofenac (58% inhibition). Zone of inhibition for formulation was 18.33 mm, 19.20 mm and 26.30 mm for P. acnes, S. epidermidis and S. aureus respectively. This activity was also comparable to that of Clindamycin.AHPL/AYCAP/0413 capsule possesses significant Anti-inflammatory and Anti-microbial activities which further justifies its role in the management of Acne vulgaris.Anti-inflammatory and antimicrobial activities of polyherbal formulation AHPL/AYCAP/0413 were evaluatedAHPL/AYCAP/0413 contains Guduchi extract (Tinospora cordifolia), Manjishtha extract (Rubia cordifolia), Sariva extract (Hemidesmus indicus), Nimba extract (Azardirachta indica), Khadira extract (Acacia catechu) and Kakmachi extract (Solanum nigrum)Anti-inflammatory activity of AHPL/AYCAP/0413 in comparison with Diclofenac was assessed in carrageenan induced rat Paw edema model. Significant reduction in rat paw edema (51% inhibition) was observed with formulation AHPL/AYCAP/0413 which was also comparable to that of Diclofenac (58% inhibition)Anti-microbial activity of AHPL/AYCAP/0413 was assessed against Propionibacterium acnes, Staphylococcus epidermidis and Staphylococcus aureus. Zone of inhibition for formulation was 18.33 mm, 19.20 mm and 26.30 mm for P. acnes, S. epidermidis and S. aureus respectively indicating 68.42%, 85.71% and 81.17% activity. This activity was also comparable to that of ClindamycinTherefore it is evident that, AHPL/AYCAP/0413 capsule possesses significant Anti-inflammatory and Anti-microbial activities which further justifies its role in the management of Acne vulgaris. Abbreviations Used: mg: Milligram, kg: Kilogram, w/v: Weight by volume, ml: Milliliters, h: Hour, BHI: Brain Heart Infusion, CFU: Colony forming units, μg: Microgram, A.I.: Activity index, P.I.: Percent inhibition, TSB: Trypticsoy Broth, mm: millimeters, P. acnes: Propionibacterium acnes, S. epidermidis: Staphylococcus epidermidis, S. aureus: Staphylococcus aureus.

Dataset Information

Lipidated cyclic ?-AApeptides display both antimicrobial and anti-inflammatory activity.

Publications

Lipidated cyclic γ-AApeptides display both antimicrobial and anti-inflammatory activity.

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