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Honglin Jin, Chao Wan, Zhenwei Zou, Guifang Zhao, Lingling Zhang, Yuanyuan Geng, Tong Chen, Ai Huang, Fagang Jiang, Jue-Ping Feng, Jonathan F Lovell, Jing Chen, Gang Wu, Kunyu Yang
Immunosuppressive tumor microenvironments (TMEs) create tremendous obstacles for an effective cancer therapy. Herein, we developed a melittin-RADA32 hybrid peptide hydrogel loaded with doxorubicin (DOX) for a potent chemoimmunotherapy against melanoma through the active regulation of TMEs. The formed melittin-RADA32-DOX (MRD) hydrogel has an interweaving nanofiber structure and exhibits excellent biocompatibility, controlled drug release properties both in vitro and in vivo, and an enhanced killing effect to melanoma cells...
March 20, 2018: ACS Nano
Süleyman Cinar, Claus Czeslik
We compare the binding of an inhibitor with that of a natural peptide to Ca2+ saturated calmodulin (holo-CaM). As inhibitor we have chosen trifluoperazine (TFP) that is inducing a huge conformational change of holo-CaM from the open dumbbell-shaped to the closed globular conformation upon binding. On the other hand, melittin is used as model peptide, which is a well-known natural binding partner of holo-CaM. The experiments are carried out as a function of pressure to reveal the contribution of volume or packing effects to the stability of the calmodulin-ligand complexes...
March 16, 2018: Biochimica et Biophysica Acta
Svetlana S Efimova, Evgeny G Chulkov, Olga S Ostroumova
The effects of local anesthetics (LAs), namely, lidocaine (LDC), prilocaine (PLC), mepivacaine (MPV), bupivacaine (BPV), procaine (PC), and tetracaine (TTC), on the steady-state transmembrane conductance induced by the cis-side addition of the antifungal polyene macrolide antibiotic, nystatin (NYS), in planar lipid bilayers were studied. The addition of TTC to model membranes comprising DOPC and cholesterol (33 mol%) led to a nearly twenty-fold increase in the steady-state NYS-induced membrane conductance...
March 8, 2018: Colloids and Surfaces. B, Biointerfaces
Suvimol Somwongin, Panuwan Chantawannakul, Wantida Chaiyana
Pharmacological effects of bee venom has been reported, however, it has been restricted to the bee venom collected from European honey bee (Apis mellifera). The aim of the present study was to compare the antioxidant activities and irritation properties of venoms collected from four different Apis species in Thailand, which includes Apis cerena (Asian cavity nesting honeybee), Apis florea (dwarf honeybee), Apis dorsata (giant honeybee), and A. mellifera. Melittin content of each bee venom extracts was investigated by using high-performance liquid chromatography...
February 27, 2018: Toxicon: Official Journal of the International Society on Toxinology
Daniel P Feldmann, Yilong Cheng, Rima Kandil, Yuran Xie, Mariam Mohammadi, Hartmann Harz, Akhil Sharma, David J Peeler, Anna Moszczynska, Heinrich Leonhardt, Suzie H Pun, Olivia M Merkel
The block copolymer VIPER (virus-inspired polymer for endosomal release) has been reported to be a promising novel delivery system of DNA plasmids both in vitro and in vivo. VIPER is comprised of a polycation segment for condensation of nucleic acids as well as a pH-sensitive segment that exposes the membrane lytic peptide melittin in acidic environments to facilitate endosomal escape. The objective of this study was to investigate VIPER/siRNA polyplex characteristics, and compare their in vitro and in vivo performance with commercially available transfection reagents and a control version of VIPER lacking melittin...
February 20, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Yijie Chen, Mengchun Chen, Yue Zhang, Joo Hee Lee, Tamara Escajadillo, Hua Gong, Ronnie H Fang, Weiwei Gao, Victor Nizet, Liangfang Zhang
Neutralization of bacterial toxins has become a compelling approach to treating bacterial infections as it may pose less selective pressure for the development of bacterial resistance. Currently, the majority of toxin neutralization platforms act by targeting the molecular structure of the toxin, which requires toxin identification and customized design for different diseases. Therefore, their development has been challenged by the enormous number and complexity of bacterial toxins. Herein, biomimetic toxin nanosponges are formulated by coating membranes of human red blood cells (hRBCs) onto polymeric nanoparticles, which act as a toxin decoy to absorb and neutralize a broad-spectrum of hemolytic toxins regardless of their molecular structure...
February 13, 2018: Advanced Healthcare Materials
Gongyu Li, Siming Yuan, Shihui Zheng, Yangzhong Liu, Guangming Huang
In-situ living cell protein analysis would enable the structural identification and functional interrogation of intracellular proteins in native cellular environments. Previously, we have presented an in-situ MS strategy to identify protein and protein/metal ion complex with relatively small molecular weight (Anal. Chem. 2016, 88, 10860-10866). However, it is still challenging to directly identify larger proteins and protein/ligand complexes in cell, due to numerous non-specific binding of ligands, solvents and other cellular constituents...
February 6, 2018: Analytical Chemistry
Woon-Hae Kim, Hyun-Jin An, Jung-Yeon Kim, Mi-Gyeong Gwon, Hyemin Gu, Minji Jeon, Min-Kyung Kim, Sang-Mi Han, Kwan-Kyu Park
Periodontitis is a chronic inflammatory disease that contributes to the destruction of the gingiva. Porphyromonas gingivalis (P. gingivalis) can cause periodontitis via its pathogenic lipopolysaccharides (LPS). Melittin, a major component of bee venom, is known to have anti-inflammatory and antibacterial effects. However, the role of melittin in the inflammatory response has not been elucidated in periodontitis-like human keratinocytes. Therefore, we investigated the anti-inflammatory effects of melittin on a P...
February 5, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Zhilin Yang, Heejun Choi, James C Weisshaar
The permeabilization of model lipid bilayers by cationic peptides has been studied extensively over decades, with the bee-sting toxin melittin perhaps serving as the canonical example. However, the relevance of these studies to the permeabilization of real bacterial membranes by antimicrobial peptides remains uncertain. Here, we employ single-cell fluorescence microscopy in a detailed study of the interactions of melittin with the outer membrane (OM) and the cytoplasmic membrane (CM) of live Escherichia coli...
January 23, 2018: Biophysical Journal
William C Wimley
No abstract text is available yet for this article.
January 23, 2018: Biophysical Journal
Lanlan Wan, Daqi Zhang, Jinnan Zhang, Liqun Ren
Melittin is a 26 amino acid residue antimicrobial peptide with known antitumor activity. In the present study, a novel peptide TT-1, derived from melittin and contained only 11 amino acids, was designed, and its antitumor effect was investigated. The present study is aimed to elucidate the effects and relative mechanisms of TT-1 on a human thyroid cancer cell line (TT) in vitro and in vivo. Cell viability assays, Annexin V/propidium iodide assays, western blotting and quantitative reverse transcription polymerase chain reaction were performed...
January 2018: Oncology Letters
Ali Mohammadi Bardbari, Mohammad Reza Arabestani, Manoochehr Karami, Fariba Keramat, Hossein Aghazadeh, Mohammad Yousef Alikhani, Kamran Pooshang Bagheri
The rapid increase of drug resistance and failure of available antibiotics to treat biofilm-associated infections is of great health concern. Accordingly, our study aimed to evaluate the synergistic antibacterial, biofilm inhibitory, and biofilm removal activities of melittin in combination with colistin, imipenem, and ciprofloxacin against multidrug-resistant (MDR) strong biofilm producer Acinetobacter baumannii isolates. The kinetics of biofilm formation were evaluated for the isolates for 144 h. Minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs), minimum biofilm inhibitory concentrations (MBICs), and biofilm removal activities for melittin and combinations with antibiotics were determined...
January 20, 2018: European Journal of Clinical Microbiology & Infectious Diseases
Hongzhi Qiao, Dong Fang, Lei Zhang, Xiaochen Gu, Yin Lu, Minjie Sun, Chunmeng Sun, Qineng Ping, Junsong Li, Zhipeng Chen, Jun Chen, Lihong Hu, Liuqing Di
Melittin (Mel), one of the host defense peptides (HDPs) derived from venom of honeybees, demonstrates substantial anticancer properties, which is considered attributed to augmenting reactive oxygen species (ROS) generation. However, little has been reported on its pro-oxidation capacity in cancer oxidation therapy. In this study, a ROS amplifying nanodevice was fabricated through direct complexation of two natural pro-oxidants, Mel and condensed epigallocatechin gallate (pEGCG). The obtained nanocomplex (NC) was further covered with phenylboronic acid derivatized hyaluronic acid (pHA) through ROS-responsive boronate ester coordination bond to produce pHA-NC...
January 16, 2018: ACS Applied Materials & Interfaces
Natalia B Baranova, Tatyana Y Malygina, Elena S Medvedeva, Eugenia A Boulygina, Maria N Siniagina, Mohamed Amine Dramchini, Reshad Akbor Prottoy, Alexey A Mouzykantov, Marina N Davydova, Olga A Chernova, Vladislav M Chernov
Acholeplasma laidlawii is a well-suited model for studying the molecular basis for adapting mollicutes to environmental conditions. Here, we present the whole-genome sequences of two strains of A. laidlawii with increased resistance to tetracycline and melittin.
January 11, 2018: Genome Announcements
Seyed Hossein Rajabnejad, Ahad Mokhtarzadeh, Khalil Abnous, Seyed Mohammad Taghdisi, Mohammad Ramezani, Bibi Marjan Razavi
Melittin, a small water-soluble cationic amphipathic α-helical linear peptide, consisted of 26 amino acids, is the honeybee venom major constituent. Several reports have proved the lytic and apoptotic effects of melittin in several cancerous cell lines. In this study, we aimed to fabricate an AS1411 aptamer-melittin to specifically deliver melittin to nucleolin positive cells (A549). Melittin was covalently attached to antinucleolin aptamer (AS1411) and its toxicity in A549 (Nucleolin positive) and L929 (Nucleolin negative) was studied using MTT and Annexin V flow cytometry methods...
January 12, 2018: Drug Development and Industrial Pharmacy
Xi Yu, Xingchun Gou, Peng Wu, Liang Han, Daofeng Tian, Fengyi Du, Zeming Chen, Fuyao Liu, Gang Deng, Ann T Chen, Chao Ma, Jun Liu, Sara M Hashmi, Xing Guo, Xiaolong Wang, Haitian Zhao, Xinran Liu, Xudong Zhu, Kevin Sheth, Qianxue Chen, Louzhen Fan, Jiangbing Zhou
Clinical translation of therapeutic peptides, particularly those that require penetration of the cell membrane or are cytolytic, is a major challenge. A novel approach based on a complementary mechanism, which has been widely used for guided synthesis of DNA or RNA nanoparticles, for de novo design of activatable protein nanoparticles (APNPs) for targeted delivery of therapeutic peptides is described. APNPs are formed through self-assembly of three independent polypeptides based on pairwise coiled-coil dimerization...
January 8, 2018: Advanced Materials
Tânia Silva, Bárbara Claro, Bruno Brás Silva, Nuno Vale, Paula Gomes, Maria Salomé Gomes, Sergio S Funari, Jose Teixeira, Daniela Uhrikova, Margarida Bastos
The understanding of the mechanism of action of antimicrobial peptides is fundamental for the development of new and more active antibiotics. In present work, we use a wide range of techniques (SANS, SAXD, DSC, ITC, CD, confocal and electron microscopy) in order to fully characterize the interaction of a cecropin A-melittin hybrid antimicrobial peptide, CA(1-7)M(2-9), of known antimicrobial activity, with a bacterial model membrane of POPE/POPG, in an effort to unravel its mechanism of action. We found that CA(1-7)M(2-9) disrupts the vesicles inducing membrane condensation, forming an 'onion-like' structure of multilamellar stacks, held together by the intercalated peptides...
January 5, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Woon-Hae Kim, Hyun-Jin An, Jung-Yeon Kim, Mi-Gyeong Gwon, Hyemin Gu, Minji Jeon, Woo Jung Sung, Sang Mi Han, Sok Cheon Pak, Min-Kyung Kim, Kwan-Kyu Park
Atopic dermatitis (AD) is an inflammatory skin disease characterized by intense pruritus and relapsable eczematous lesions. The hallmarks of AD are defects in the epidermal barrier and immunoglobulin E (IgE)-mediated sensitization to several environmental allergens, as well as an immune disorder mediated by an imbalance toward T-helper-2 response. Melittin, a major component of bee venom, has been studied in various inflammatory diseases. However, the beneficial effects of melittin on mouse with AD-like symptoms have not been explored...
December 15, 2017: Scientific Reports
Mariana Tilinca, Adrian Florea
In this study, we aimed to investigate the testicular toxicity of two molecules derived from bee venom (BV): phospholipase A2 (PlA2) and melittin (Mlt). Ultrastructural effects of purified BV PlA2 and Mlt were assessed consecutive to repeated dose (30 days) and acute toxicity studies. For the subchronic treatment, PlA2 and Mlt were injected in daily doses equivalent to those released by a bee sting (105 μg PlA2/kg/day and 350 μg Mlt/kg/day), while in the acute treatment their doses corresponded to those released by 100 bee stings (9...
January 2018: Toxicon: Official Journal of the International Society on Toxinology
Kayla M Socarras, Priyanka A S Theophilus, Jason P Torres, Khusali Gupta, Eva Sapi
Lyme disease is a tick-borne, multi-systemic disease, caused by the bacterium Borrelia burgdorferi. Though antibiotics are used as a primary treatment, relapse often occurs after the discontinuation of antimicrobial agents. The reason for relapse remains unknown, however previous studies suggest the possible presence of antibiotic resistant Borrelia round bodies, persisters and attached biofilm forms. Thus, there is an urgent need to find antimicrobial agents suitable to eliminate all known forms of B. burgdorferi ...
November 29, 2017: Antibiotics
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