The effect of halogenation on the antimicrobial activity, antibiofilm activity, cytotoxicity and proteolytic stability of the antimicrobial peptide Jelleine-I.


:Antimicrobial peptides (AMPs) are believed to be a promising class of antimicrobial agents against bacteria and fungi. To promote the clinical use of AMPs, their antimicrobial activity and susceptibility to protease degradation should be further improved. The antimicrobial peptide Jelleine-I was originally isolated from the royal jelly of honeybees (Apis mellifera) with a short sequence of PFKLSLHL-NH2 (953.24 Da). Here, a series of halogenated derivatives of the antimicrobial peptide Jelleine-I were designed and synthesized. The results showed that the in vitro antimicrobial activity, antibiofilm activity and in vivo antimicrobial efficacy were enhanced 1-8-fold after halogenation. Additionally, the proteolytic stability of Jelleine-I was improved 10-100-fold by halogenation. Meanwhile, the halogenated derivatives retained negligible hemolytic activity and cytotoxicity. Among these derivatives, the antimicrobial activity and antibiofilm activity of chlorine-Jelleine-I (Cl-J-I), bromine-Jelleine-I (Br-J-I), and iodine-Jelleine-I (I-J-I) were better than those of fluorine-Jelleine-I (F-J-I). The stabilities of Br-J-I and I-J-I against the degradation of enzymes and the serum were better than those of F-J-I and Cl-J-I. In conclusion, this study may offer a useful strategy to enhance antimicrobial efficacy and proteolytic stability by halogenation. The halogenated derivatives Cl-J-I, Br-J-I and I-J-I may be considered as potential antimicrobial agents against microbial infection.






Jia F,Zhang Y,Wang J,Peng J,Zhao P,Zhang L,Yao H,Ni J,Wang K




Has Abstract


2019-02-01 00:00:00














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    abstract::[125I]beta-endorphin bound to high affinity (Kd = 0.25 nM) receptors in the caudal dorsomedial medulla of rats with a Bmax of 97 fmol/mg protein. The relative potency for displacement of [125I]beta-endorphin binding was: beta-endorphin(1-31) > beta-endorphin(1-27) > DAMGO > naloxone > N-acetyl-beta-endorphin(1-31) > U...


    pub_type: 杂志文章


    authors: D'Souza MM,Carr JA

    更新日期:1998-01-01 00:00:00

  • Identification of a novel N-cadherin antagonist.

    abstract::The cell adhesion molecule, N-cadherin plays a pivotal role in many biological and disease processes. Drugs that modulate N-cadherin function should therefore be useful therapeutic agents. We have used phage display technology to identify amino acid sequences capable of binding to N-cadherin. All of these sequences ha...


    pub_type: 杂志文章


    authors: Devemy E,Blaschuk OW

    更新日期:2008-11-01 00:00:00

  • Prolongation of intermeal interval by gastrin-releasing peptide depends upon time of delivery.

    abstract::We have previously shown that brief, vena caval infusion of gastrin-releasing peptide1-27 (GRP), delivered shortly (5 min) after the end of the first spontaneous nocturnal meal, significantly prolongs the postprandial intermeal interval (IMI) without affecting the size of the subsequent meal in freely-feeding rats. In...


    pub_type: 杂志文章


    authors: Rushing PA,Gibbs J

    更新日期:1998-01-01 00:00:00

  • Multiple antigenic peptides designed to structurally related Drosophila peptides.

    abstract::We have isolated TDVDHVFLRFamide (DMS), FDDYGHMRFamide (DSK), and DPKQDFMRFamide from Drosophila melanogaster. These peptides, structurally related by a common C-terminus -XRFamide, where X = L or M, are encoded by three different genes. To determine cellular expression, we have generated antisera to multiple antigeni...


    pub_type: 杂志文章


    authors: Nichols R,McCormick J,Lim I

    更新日期:1997-01-01 00:00:00

  • Agrocybin, an antifungal peptide from the edible mushroom Agrocybe cylindracea.

    abstract::An antifungal peptide with a molecular mass of 9 kDa was isolated from fresh fruiting bodies of the mushroom Agrocybe cylindracea. The isolation procedure comprised ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography by fast protein liquid chromatogr...


    pub_type: 杂志文章


    authors: Ngai PH,Zhao Z,Ng TB

    更新日期:2005-02-01 00:00:00

  • Control of GnRH expression in the olfactory lobe of Octopus vulgaris.

    abstract::In the cephalopod mollusk Octopus vulgaris, the gonadotropic hormone released by the optic gland controls sexual maturity. Several lobes of the central nervous system control the activity of this gland. In one of these lobes, the olfactory lobe, a gonadotropin releasing hormone (GnRH) neuronal system has been describe...


    pub_type: 杂志文章


    authors: Di Cristo C,De Lisa E,Di Cosmo A

    更新日期:2009-03-01 00:00:00

  • Correlation between apolipoprotein B and endothelin-1-induced vasoconstriction in humans.

    abstract::Low-density lipoprotein (LDL) concentrations have been linked to altered responses to endogenous vasodilators and vasoconstrictors. We evaluated retrospectively the relationship between LDL and vasoconstrictor (endothelin-1, phenylephrine) responsiveness of the forearm vasculature in 15 elderly healthy volunteers with...


    pub_type: 杂志文章


    authors: Romerio SC,Linder L,Flammer J,Haefeli WE

    更新日期:2000-06-01 00:00:00

  • Bovine pancreatic polypeptide-like immunoreactivity in brain and peripheral nervous system: coexistence with catecholaminergic nerves.

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    pub_type: 杂志文章


    authors: Jacobowitz DM,Olschowka JA

    更新日期:1982-05-01 00:00:00

  • Multiplicity of receptors for vasoactive intestinal polypeptide (VIP): differential effects of apamin on binding in brain, uterus and liver.

    abstract::Apamin is a neurotoxic octadecapeptide from bee venom, which has been shown to inhibit the non-adrenergic, non-cholinergic inhibitory innervation of the smooth muscle of the gut. Since vasoactive intestinal polypeptide (VIP) has been proposed as a possible inhibitory neurotransmitter, the effect of apamin on the recep...


    pub_type: 杂志文章


    authors: Fahrenkrug J,Gammeltoft S,Staun-Olsen P,Ottesen B,Sjöquist A

    更新日期:1983-03-01 00:00:00

  • Characterization of binding sites of a memory-enhancing peptide AVP(4-8) in rat cortical synaptosomal membranes.

    abstract::The pentapeptide pGlu-Asn-Cyt-Pro-Arg [AVP(4-8), termed ZNC(C)PR in this article] has been found as a metabolite of arginine-vasopressin (AVP) in rat brain and has been shown to have potent memory-enhancing activity and to yield a series of biochemical events in brain tissues. [35S]ZNC(C)PR was chemically synthesized ...


    pub_type: 杂志文章


    authors: Du YC,Wu JH,Jiang XM,Gu YJ

    更新日期:1994-01-01 00:00:00

  • The Mycobacterium tuberculosis membrane protein Rv0180c: Evaluation of peptide sequences implicated in mycobacterial invasion of two human cell lines.

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    pub_type: 杂志文章


    authors: Cáceres SM,Ocampo M,Arévalo-Pinzón G,Jimenez RA,Patarroyo ME,Patarroyo MA

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  • Down-regulation of haloperidol-induced striatal dopamine receptor supersensitivity by active analogues of L-prolyl-L-leucyl-glycinamide (PLG).

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    pub_type: 杂志文章


    authors: Rajakumar G,Naas F,Johnson RL,Chiu S,Yu KL,Mishra RK

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  • Expression of C-type natriuretic peptide and of its receptor NPR-B in normal and failing heart.

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    pub_type: 杂志文章


    authors: Del Ry S,Cabiati M,Lionetti V,Emdin M,Recchia FA,Giannessi D

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  • The effects of MIF-I, beta-endorphin and alpha-MSH on d-amphetamine induced paradoxical behavioral thermoregulation: possible involvement of the dopaminergic system.

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    pub_type: 杂志文章


    authors: Yehuda S,Sheleff P

    更新日期:1985-03-01 00:00:00

  • Studies on beta-endorphin and membrane-bound calcium interaction using chlorotetracycline (CTC) as a fluorescence probe.

    abstract::Studies on the in vitro interaction of beta-endorphin with different biomembrane preparations, measured in terms of Ca2+ induced chlorotetracycline (CTC) fluorescence alterations indicate that beta-endorphin causes release of calcium ion from both synaptosomal and erythrocyte membrane stores but not from rat brain mit...


    pub_type: 杂志文章


    authors: Chakrabarti AK,Chatterjee TK,Ghosh JJ

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  • Substance P and the neurokinin-1 receptor in relation to eosinophilia in ulcerative colitis.

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    pub_type: 杂志文章


    authors: Jönsson M,Norrgård O,Forsgren S

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    pub_type: 杂志文章


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    pub_type: 杂志文章


    authors: Gue M,Bueno L

    更新日期:1991-05-01 00:00:00

  • Des-acetyl MSH and gamma-MSH act as partial agonists to alpha-MSH on the Anolis melanophore.

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    pub_type: 杂志文章


    authors: McCormack AM,Carter RJ,Thody AJ,Shuster S

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  • FMRFamide-related peptides in the gut of Locusta migratoria L.: a comprehensive map and developmental profile.

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    pub_type: 杂志文章


    authors: Hill SR,Orchard I

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  • Blockade of early and late retinal biochemical alterations associated with diabetes development by the selective bradykinin B1 receptor antagonist R-954.

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    pub_type: 杂志文章


    authors: Catanzaro O,Labal E,Andornino A,Capponi JA,Di Martino I,Sirois P

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    pub_type: 杂志文章


    authors: Lee RJ,Lomax P

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    pub_type: 杂志文章


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    authors: Yamamoto N,Tamura A

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    pub_type: 杂志文章


    authors: Shibano A,Kawai Y,Senba E

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    pub_type: 杂志文章


    authors: Guo CT,McClean S,Shaw C,Rao PF,Ye MY,Bjourson AJ

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    pub_type: 杂志文章


    authors: Predel R,Russell WK,Russell DH,Lopez J,Esquivel J,Nachman RJ

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    pub_type: 杂志文章


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    pub_type: 杂志文章


    authors: Fehmann HC,Göke B

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