Page last updated: 2024-11-12

melitten

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Melitten: Basic polypeptide from the venom of the honey bee (Apis mellifera). It contains 26 amino acids, has cytolytic properties, causes contracture of muscle, releases histamine, and disrupts surface tension, probably due to lysis of cell and mitochondrial membranes. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
Lysisgenus[no description available]PrimulaceaeA plant family of the order ERICALES, class MAGNOLIOPSIDA, with flowers having both stamens and pistil, producing encapsulated fruits.[MeSH]

Cross-References

ID SourceID
PubMed CID16129627
SCHEMBL ID19458851
MeSH IDM0013325

Synonyms (14)

Synonym
LS-15546
37231-28-0
melittin-t
melittin i
einecs 253-417-7
mellitin
melittin (honeybee)
l-glutamamide, glycyl-l-isoleucylglycyl-l-alanyl-l-valyl-l-leucyl-l-lysyl-l-valyl-l-leucyl-l-threonyl-l-threonylglycyl-l-leucyl-l-prolyl-l-alanyl-l-leucyl-l-isoleucyl-l-seryl-l-tryptophyl-l-isoleucyl-l-lysyl-l-arginyl-l-lysyl-l-arginyl-l-glutaminyl-
melitten
melittin ,
20449-79-0
SCHEMBL19458851
DTXSID40893812 ,
Q424512

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Melittin, the main toxic component of bee venom, was biotinylated and used as a model toxicant to determine whether avidin-based extracorporeal hemoperfusion could remove biotinylated melittin and thus alter the severity of the toxic response in rats."( Reversal of toxicity using avidin-based hemoperfusion: a model system in rats using biotinylated melittin.
Billingsley, ML; Britt, AM; Burkhart, KK, 1995
)
0.29
" We have explored the possibility of determining a concentration range of melittin where it is relatively safe to be used as an adsorption enhancer."( Evaluation of cytotoxicity and absorption enhancing effects of melittin - a novel absorption enhancer.
Davis, P; Krishnan, TR; Liu, H; Liu, P, 1999
)
0.3
" In addition to this hypersensitivity, an anaphylactoid reaction occurs by toxic effects even in a non-allergic person via cytolysis followed by similar clinical manifestations."( Gangliosides inhibit bee venom melittin cytotoxicity but not phospholipase A(2)-induced degranulation in mast cells.
Kitani, S; Nishikawa, H, 2011
)
0.37
" The aim of this study was to produce human monoclonal single-chain Fv (scFv) antibody fragments capable of inhibiting the toxic effects of Africanised bee venom."( Production of human antibody fragments binding to melittin and phospholipase A2 in Africanised bee venom: minimising venom toxicity.
Barbosa, JE; Bertolini, TB; Campos, LB; Funayama, JC; Pucca, MB; Roncolato, EC, 2012
)
0.38
" We found that free melittin was toxic to sperm and vaginal epithelium at concentrations greater than 2 µM (p<0."( Nanoparticle incorporation of melittin reduces sperm and vaginal epithelium cytotoxicity.
Hood, JL; Hu, G; Jallouk, AP; Lanza, GM; Moley, KH; Omurtag, K; Wickline, SA, 2014
)
0.4
" The fusion of melittin and glutathione S-transferase results in diminished toxicity of the peptide and retained anti-inflammatory properties at doses that exceed toxic concentration of native melittin."( Melittin-glutathione S-transferase fusion protein exhibits anti-inflammatory properties and minimal toxicity.
Buhrman, JS; Gemeinhart, RA; Rayahin, JE, 2014
)
0.4
" In the present study, we review the current knowledge on the therapeutic effects of melittin and its detailed mechanisms of action against several inflammatory diseases including skin inflammation, neuroinflammation, atherosclerosis, arthritis and liver inflammation, its adverse effects as well as future prospects regarding the use of melittin."( Anti-Inflammatory Applications of Melittin, a Major Component of Bee Venom: Detailed Mechanism of Action and Adverse Effects.
Bae, H; Lee, G, 2016
)
0.43
" Preclinical and clinical studies showed that the main adverse events were allergic reaction and pain at the administration site."( A novel melittin nano-liposome exerted excellent anti-hepatocellular carcinoma efficacy with better biological safety.
Ai, M; Gao, X; Hu, K; Li, X; Liu, S; Mao, J; Wang, D; Wang, Z; Yang, Y, 2017
)
0.46
" In vivo experiments reveal that MEL/Ce6@HA can realize enhanced tumor accumulation, reduced liver deposition, and rapid body clearance, which are beneficial for highly efficient and safe chemo-photodynamic dual therapy."( Turning Toxicants into Safe Therapeutic Drugs: Cytolytic Peptide-Photosensitizer Assemblies for Optimized In Vivo Delivery of Melittin.
Jia, HR; Wu, FG; Xu, KF; Zhu, YX, 2018
)
0.48
"These results indicate that melittin at its safe dose could not exhibit antimicrobial activity, which hinders its application in clinical practice."( In vitro and in vivo toxicity and antibacterial efficacy of melittin against clinical extensively drug-resistant bacteria.
Askari, P; Ghazvini, K; Hosseini, M; Namaei, MH, 2021
)
0.62
" However, the use of bee venom has shown adverse effects."( Detoxification of Bee Venom Increases Its Anti-inflammatory Activity and Decreases Its Cytotoxicity and Allergenic Activity.
Kim, KK; Kim, YS; Lee, CY; Lee, HS; Lee, KS; Seo, HS, 2021
)
0.62
"5 mg/kg doses could not induce significant changes on immune parameters and as a result, melittin was found to be safe for the mice immune system."( Melittin as a safe compound to BALB/c mice immune system; a tiered approach immunotoxicity screening.
Amali, A; Esmaeili, SA; Fatemi, S; Karimi, G; Khorrami, MB; Memar, B; Riahi-Zanjani, B; Sadeghi, M, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" However, the usual transdermal injection of bee venom poses many pharmacokinetic disadvantages."( Pharmacokinetic improvement provided by microneedle patch in delivering bee venom, a case study in combating scopolamine-induced neurodegeneration in mouse model.
An, EJ; Jeong, DH; Kim, JH; Lee, G; Nguyen, CD; Park, SY; Sung, CY; Yoo, J, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
"In vitro antibacterial and anti-biofilm activities of antimicrobial cationic peptides (AMPs) - melittin and colistin - both alone and in combination with antibiotics were evaluated against clinical isolates of Gram-negative bacteria."( Antibacterial and anti-biofilm activities of melittin and colistin, alone and in combination with antibiotics against Gram-negative bacteria.
Alev Gerceker, A; Dosler, S; Karaaslan, E, 2016
)
0.43
" In this study, we aimed to explore the antibiofilm activity of melittin, either alone or in combination with vancomycin and rifampin, against biofilm-producing MRSE strains."( Prevention, inhibition, and degradation effects of melittin alone and in combination with vancomycin and rifampin against strong biofilm producer strains of methicillin-resistant Staphylococcus epidermidis.
Alikhani, MY; Arciola, CR; Bagheri, KP; Mirzaei, R; Sedighi, I; Yousefimashouf, R, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" Melittin, while showing little potential as an antimicrobial agent, may have potential in delivery of poorly bioavailable drugs."( Investigation of the cytotoxicity of eukaryotic and prokaryotic antimicrobial peptides in intestinal epithelial cells in vitro.
Maher, S; McClean, S, 2006
)
0.33
"The rapid and reversible nature of melittin's permeation enhancing properties and its limited cytotoxicity in polarized intestinal epithelia, suggests a potential drug delivery role for the peptide in oral formulations of poorly absorbed drugs."( Melittin as a permeability enhancer II: in vitro investigations in human mucus secreting intestinal monolayers and rat colonic mucosae.
Brayden, DJ; Feighery, L; Maher, S; McClean, S, 2007
)
0.34
" Overall, although melittin appears to stimulate necrosis, with careful dosage selection the peptide could be considered for the oral delivery of poorly bioavailable drugs."( Melittin exhibits necrotic cytotoxicity in gastrointestinal cells which is attenuated by cholesterol.
Maher, S; McClean, S, 2008
)
0.35
"We compared the effectiveness of two absorption promoters, sodium caprate (C(10)) and melittin, in increasing the bioavailability (F) of poorly absorbed paracellular flux markers across the intestinal mucosae of rats in situ, together with examination of their effects on morphology."( Evaluation of intestinal absorption and mucosal toxicity using two promoters. II. Rat instillation and perfusion studies.
Brayden, DJ; Bzik, V; Maher, S; McClean, S; Wang, X, 2009
)
0.35
" Two modified melittin peptides displayed rapid bactericidal properties against antibiotic-resistant strains, low innate resistance development by pathogenic bacteria, remained nonimmunogenic for T lymphocytes, and increased bioavailability in tear fluids."( Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
Agrawal, R; Barathi, VA; Beuerman, RW; Chan, LW; Jie, TY; Koh, SK; Lakshminarayanan, R; Leng, ET; Mayandi, V; Sebastian, TM; Somaraju Chalasani, ML; Ting, DSJ; Urf Turabe Fazil, MH; Varadarajan, J; Verma, NK; Xi, Q; Zhou, L, 2020
)
0.56
" However, their applications are limited due to poor oral bioavailability and the lack of tumor-targeting property."( iRGD-grafted N-trimethyl chitosan-coated protein nanotubes enhanced the anticancer efficacy of curcumin and melittin.
Hou, G; Li, Y; Liang, S; Liu, B; Shi, W; Wang, Q; Zhang, H, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" The dose-response curve, the latent period and temperature dependence of HR induced by MCD-peptide were similar to those of HR induced by compound 48/80."( [Histamine-liberating action of MCD-peptide from bee venom].
Gushchin, IS; Martynov, VI; Miroshnikov, AI, 1977
)
0.26
" The effect of melittin was maximum at about 25 ng/ml, and the dose-response curve was biphasic."( Stimulation of prostaglandin production in bone by phorbol diesters and melittin.
Delclos, B; Ivey, JL; Levine, L; Tashjian, AH, 1978
)
0.26
" TNF alpha potentiated the release of [3H]arachidonate and PRL promoted by phospholipase-A2 and melittin, and markedly shifted the dose-response curve to the left."( Tumor necrosis factor-alpha increases release of arachidonate and prolactin from rat anterior pituitary cells.
Hirota, K; Ikegami, H; Kadowaki, K; Koike, K; Miyake, A; Ohmichi, M; Tanizawa, O; Yamaguchi, M, 1991
)
0.28
" The C6 dose-response curve for release of C20:4 plus its metabolites was monotonic, which indicates dependence on channel formation, whereas the dose-response curve for lysis displayed multi-hit behavior."( Release of arachidonic acid and formation of oxygenated derivatives after complement attack on macrophages: role of channel formation.
Hammer, CH; Imagawa, DK; Koga, PG; Mayer, MM; Osifchin, NE; Ramm, LE; Shin, HS, 1986
)
0.27
" The dose-response data correlated well with target cell viable count."( Real-time measurement of cell permeabilization with low-molecular-weight membranolytic agents.
Akerman, KE; Karp, MT; Oker-Blom, C; Saviranta, P; Virta, M, 1995
)
0.29
" By comparing the time course of stimulation and dose-response relationships between PGF2 alpha and PLC activity, it appears that oxytocin may stimulate PGF2 alpha secretion by activating PLC."( Cellular mechanisms by which oxytocin stimulates uterine PGF2 alpha synthesis in bovine endometrium: roles of phospholipases C and A2.
Burns, PD; Graf, GA; Hayes, SH; Silvia, WJ, 1997
)
0.3
" Overall, although melittin appears to stimulate necrosis, with careful dosage selection the peptide could be considered for the oral delivery of poorly bioavailable drugs."( Melittin exhibits necrotic cytotoxicity in gastrointestinal cells which is attenuated by cholesterol.
Maher, S; McClean, S, 2008
)
0.35
" Using a panel of human breast cancer cells with different HER2 expression levels, these immunoliposomes decreased cancer cells viability in a dose-response manner and in correlation to their level of HER2 expression."( Selective death of human breast cancer cells by lytic immunoliposomes: Correlation with their HER2 expression level.
Barrajón-Catalán, E; Carrato, A; Falco, A; Menéndez-Gutiérrez, MP; Micol, V; Saceda, M, 2010
)
0.36
" This study will be extended to a dose-response evaluation to further establish safety and response, prior to a randomized trial."( Effects of sweet bee venom pharmacopuncture treatment for chemotherapy-induced peripheral neuropathy: a case series.
Cho, CK; Jeon, JH; Jung, TY; Kwon, KR; Lee, YW; Park, JW; Sagar, S; Wong, R; Yoo, HS; Yoon, J, 2012
)
0.38
"56 mV) with reduced cytotoxicity and a widened safe dosage range."( Hybrid melittin cytolytic Peptide-driven ultrasmall lipid nanoparticles block melanoma growth in vivo.
Huang, C; Jin, H; Luo, H; Luo, Q; Qi, S; Qian, Y; Zhang, Z, 2013
)
0.39
" However, efficacy of melittin, especially if applied in a higher dosage as in the present study or for a longer period, could be evaluated in further studies."( Clinical efficacy of melittin in the treatment of cats infected with the feline immunodeficiency virus.
Erfle, V; Hartmann, AD; Hartmann, K; Wilhelm, N, 2016
)
0.43
" This GMT/DS binary system shows great promise due to its simple components, facile preparation method, and enhanced potential druggability, including a decreased dosing frequency, decreased acute toxicity, and improved pathological indicators."( Prolonged melittin release from polyelectrolyte-based nanocomplexes decreases acute toxicity and improves blood glycemic control in a mouse model of type II diabetes.
Cai, X; Cao, P; Chen, J; Gui, Z; He, Z; Hu, C; Ling, Y; Ye, J; Ye, S; Zhu, J, 2020
)
0.56
" We then use a tissue-engineered model of the human BBB to optimize dosing and elucidate the mechanism of opening."( Reversible blood-brain barrier opening utilizing the membrane active peptide melittin in vitro and in vivo.
Chu, C; DeStefano, JG; Hristova, K; Komin, A; Lan, X; Linville, RM; Liu, G; Searson, PC; Walczak, P, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,042)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990450 (22.04)18.7374
1990's554 (27.13)18.2507
2000's416 (20.37)29.6817
2010's440 (21.55)24.3611
2020's182 (8.91)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.32 (24.57)
Research Supply Index7.66 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index91.05 (26.88)
Search Engine Supply Index3.00 (0.95)

This Compound (37.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (0.19%)5.53%
Reviews78 (3.68%)6.00%
Case Studies4 (0.19%)4.05%
Observational0 (0.00%)0.25%
Other2,035 (95.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]