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We previously reported a series of novel endomorphin analogs with unnatural amino acid modifications. These analogs display good binding affinity and functional activity toward the μ opioid receptor (MOP). In the present study, we further investigated the spinal antinociceptive activity of these compounds. The analogs were potent in several nociceptive models. Opioid antagonists and antibodies against...
Currently, antimicrobial peptides have attracted considerable attention because of their broad-sprectum activity and low prognostic to induce antibiotic resistance. In our study, for the first time, a series of side-chain hybrid dimer peptides J-AA (Anoplin-Anoplin), J-RR (RW-RW), and J-AR (Anoplin-RW) based on the wasp peptide Anoplin and the arginine- and tryptophan-rich hexapeptide RW were designed...
Neurite outgrowth is an important process in neural regeneration and plasticity, especially after neural injury, and recent evidence indicates that several Gαi/o protein-coupled receptors play an important role in neurite outgrowth. The neuropeptide (NP)FF system contains two Gαi/o protein-coupled receptors, NPFF1 and NPFF2 receptors, which are mainly distributed in the central nervous system. The...
Receptors and their regulatory peptides are aberrantly expressed in tumors, suggesting a potential tumor therapy target. Human hemokinin-1 (hHK-1) is a tachykinin peptide ligand of the neurokinin-1 (NK1) receptor which is overexpressed in melanoma and other tumor tissues. Here, we investigated the role of hHK-1 and the NK1 receptor in melanoma cell migration. NK1 receptor expression was associated...
Attachment of traditional anticancer drugs to cell penetrating peptides is an effective strategy to improve their application in cancer treatment. In this study, we designed and synthesized the conjugates TAT-CPT and TAT-2CPT by attaching camptothecin (CPT) to the N-terminus of the cell penetrating peptide TAT. Interestingly, we found that TAT-CPT and especially TAT-2CPT could kill cancer cells via...
Apelin and its receptor APJ (apelin receptor) are prominently expressed in brain regions involved in learning and memory. However, the role of apelin in cognition was largely unclear. Here, the role of apelin-13 in memory processes was investigated in mice novel object recognition task. Post-training injection of apelin-13 (0.3 and 1nmol) dose-dependently impaired short-term memory (STM), however,...
With the increasing emergence of resistant fungi, the discovery and development of novel antifungal therapeutics were urgently needed. Compared with conventional antibiotics, the limited propensity of AMPs to induce resistance in pathogens has attracted great interest. In the present study, the antifungal activity and its mechanism-of-action of polybia-MPI, a cationic peptide from the venom of Social...
Previous studies suggest that cannabinoids system plays an important role in cardiovascular regulation. (m)VD-hemopressin(α) (VD-Hpα), an 11-residue peptide originating from the α 1 chain of hemoglobin, was recently reported as a selective agonist of cannabinoid CB 1 receptor. The present study was undertaken to investigate the intrathecal (i.t.) action of (m)VD-Hpα on blood pressure...
Neuropeptide FF (NPFF) has many functions in regulating various biological processes. However, little attention has been focused on the anti-inflammatory effect of this peptide. In the present study, the in vitro anti-inflammatory activity of NPFF in both primary peritoneal macrophages and RAW 264.7 macrophages was investigated. Our data showed that NPFF suppressed the nitric oxide (NO) production...
Stearyl-cell penetrating peptides (CPPs) have been proved to be efficient nonviral gene vectors. Due to the similarities between antimicrobial peptides and CPPs, we constructed a novel type of gene vectors by introducing stearyl moiety to the N-terminus of antimicrobial peptide [D]-K6L9. In this study, stearyl-[D]-K6L9 delivered plasmids into cells by clathrin- and caveolin-mediated endocytosis. Gratifyingly,...
To evaluate the therapeutic efficacy of high-dose octreotide in patients with predicted severe acute pancreatitis (SAP) or SAP, two hundred and thirty-six patients with predicted SAP and 136 patients with SAP were randomized into control, high-dose octreotide (High-O) and low-dose octreotide (Low-O) groups. In addition to the conventional managements administrated in control group, High-O group received...
As the frequent emergence of the resistant bacteria, the development of new agents with a new action mode attracts a great deal of interest. It is now widely accepted that antimicrobial peptides (AMPs) are promising alternatives to conventional antibiotics. In this study, antimicrobial peptide polybia-MPI and its analogs were synthesized and their antibacterial activity was studied. Our results revealed...
Neuropeptide FF (NPFF) has been reported to play important roles in regulating diverse biological processes. However, little attention has been focused on the downstream signal transduction pathway of NPFF. Here, we used the differentiated neuroblastoma cell line, dSH-SY5Y, which endogenously expresses hNPFF2 receptor, to investigate the signal transduction downstream of NPFF. In particular we investigated...
Transportan 10 (TP10) is an amphipathic cell-penetrating peptide with high translocation ability. In order to obtain more details of structure–activity relationship of TP10, we evaluated the effects of structure and charge on its translocation ability. Our results demonstrated that disrupting the helical structure or Arg substitution could remarkably decrease the cellular uptake of TP10. However,...
The monocyte locomotion inhibitory factor (MLIF) is an anti-inflammatory oligopeptide produced by Entamoeba histolytica. Among its different effects, it inhibits locomotion of human monocytes, hence its original name. The carboxyl-terminal end group Cys-Asn-Ser is the pharmacophore of anti-inflammatory peptide Met-Gln-Cys-Asn-Ser. In this study, the N-terminal of Cys-Asn-Ser was modified. With the...
The endogenous opioid system has been found to be involved in the fever caused by lipopolysaccharide (LPS). Neuropeptide FF (NPFF, FLFQPQRF-NH 2 ) is an endogenous peptide known to modulate opioid activity, mainly in the central nervous system. Therefore, those data suggested a link between LPS-induced fever and NPFF systems. Using a model of acute neuroinflammation, we sought to determine...
Endomorphins (EMs) cannot be delivered into the central nervous system (CNS) in sufficient quantity to elicit antinociception when given systemically because they are severely restricted by the blood–brain barrier (BBB). In the present study, we investigated herein a series of EM-1 analogs with C-terminal linked by oligoarginine in order to improve the brain delivery and antinociception after systemic...
Neuropeptide S (NPS), the endogenous ligand of NPS receptor (NPSR), can regulate a variety of biological functions, including arousal, anxiety, locomotion, memory and drug abuse. Previous studies have shown that central NPS inhibited food intake in rats and chicks. In the present study, we investigated the role of central NPS on food intake in fasted mice, and detected the underlying mechanism(s)...
Neuropeptide S (NPS), a recently discovered bioactive peptide, was reported to regulate arousal, anxiety, locomotion, feeding behaviors, memory, and drug addiction. NPS receptor (NPSR) mRNA was found in several brain regions related to descending control system of pain, including the periaqueductal gray (PAG). Our previous study had shown that NPS could produce antinociception in mice. The present...
Polybia-MPI (MPI), a short cationic α-helical antimicrobial peptide, exhibited excellent anticancer activity and selectivity in vitro in our previous studies. To improve its in vivo application, we synthesized an analog (MPI-1) of MPI by replacing the C terminal amide –[CO–NH 2 ] with thioamide –ψ[CS–NH 2 ]. Although there is just one atom difference, the MPI-1 exhibited some surprising...
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