Study on the effects of different dimerization positions on biological activity of partial d-Amino acid substitution analogues of Anoplin

In this study, a series of new C–C terminals and C–N terminals dimer peptides were designed and synthesized by intermolecular dimerization of the partial d-amino acid substitution analogues of Anoplin, and the effects of different dimerization positions on biological activity were researched. The antimicrobial activity and stability of the new C–C terminals and C–N terminals dimer peptides were significantly improved compared with their parent peptide Anoplin. They displayed no obvious hemolytic activity and lower cytotoxicity, with a higher therapeutic index. Furthermore, the new dimer peptides not only enabled to rapidly disrupt bacterial membrane and damage its integrity which was different from conventional antibiotics but also penetrated bacterial membrane into binding to intracellular genomic DNA. More importantly, the new dimer peptides showed excellent antimicrobial activity against multidrug-resistant strains isolated from clinics in contrast to conventional antibiotics with low tendency to develop the bacterial resistance, besides they exhibited better anti-biofilm activity than antibiotic Rifampicin. Interestingly, the C–N terminals dimer peptides were superior to C–C terminals ones in antimicrobial and anti-biofilm activity, therapeutic index, outer membrane permeability, and DNA binding ability, whereas there were no noteworthy effects in different dimerization positions on stability. Thus, these data suggested that dimerizatio...
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research

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Authors: Severyn CJ, Brewster R, Andermann TM Abstract Growing evidence suggests that human microbiota likely influence diverse processes including hematopoiesis, chemotherapy metabolism, and efficacy, as well as overall survival in patients with hematologic malignancies and other cancers. Both host genetic susceptibility and host-microbiota interactions may impact cancer risk and response to treatment; however, microbiota have the potential to be uniquely modifiable and accessible targets for treatment. Here, we focus on strategies to modify microbiota composition and function in patients with cancer. First, we ev...
Source: Hematology ASH Education Program - Category: Hematology Tags: Hematology Am Soc Hematol Educ Program Source Type: research
Conclusions: AEs were common, but not more frequent or severe among MDR-TB/HIV co-infected participants receiving concurrent antiretroviral therapy. Given the favorable treatment outcomes associated with concurrent treatment, antiretroviral therapy initiation should not be delayed in MDR-TB patients with HIV-coinfection.
Source: JAIDS Journal of Acquired Immune Deficiency Syndromes - Category: Infectious Diseases Tags: Clinical Science Source Type: research
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Source: Plant Science - Category: Biology Source Type: research
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Source: Carbohydrate Polymers - Category: Biomedical Science Source Type: research
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Source: Revista Peruana de Medicina de Experimental y Salud Publica - Category: International Medicine & Public Health Tags: Rev Peru Med Exp Salud Publica Source Type: research
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Source: BioImpacts - Category: Research Tags: Bioimpacts Source Type: research
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Source: J Pharm Pharm Sci - Category: Drugs & Pharmacology Authors: Tags: J Pharm Pharm Sci Source Type: research
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Source: Research in Veterinary Science - Category: Veterinary Research Source Type: research
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Source: Expert Review of Anti-Infective Therapy - Category: Infectious Diseases Tags: Expert Rev Anti Infect Ther Source Type: research
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Source: Drug Delivery - Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research
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