Melittin, molecular formula C131H229N39O31, CAS 20449-79-0, is a peptide substance with a relatively small molecular weight, which makes it have good permeability and absorption in living organisms. Meanwhile, it has good solubility and can be dissolved in solvents such as water and ethanol, which provides convenience for its use in laboratory research and clinical applications. The pure product usually appears as a colorless or light yellow powder like substance. The molecular structure gives it certain surface activity and hydrophobicity.
This enables it to interact with phospholipid molecules on the cell membrane, thereby exerting its biological functions. For example, this can disrupt cell integrity and lead to cell death by binding to the cell membrane, thereby achieving its antibacterial, antiviral and other biological activities. As a naturally occurring substance with biological activity, it has received widespread attention in the biomedical field in recent years due to its unique pharmacological effects and potential application value.
Not only does it have various biological activities such as anti-inflammatory, antibacterial, and antiviral, but it also shows good application prospects in tumor treatment, immunotherapy, and other fields.
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Melittin COA
Melittin is a complex mixture in bee venom, with various biological activities and pharmacological effects, and has wide applications in fields such as medicine, biology, and drug development.
Antibacterial activity
- It possesses broad-spectrum antibacterial and antimicrobial activity against a wide range of harmful bacteria, fungi as well as viruses, and can effectively suppress the growth and reproduction of various pathogenic microorganisms in the body.
- Such potent antimicrobial effects are mainly attributed to the active component it, which is capable of destroying the complete structure of bacterial cell membranes, disrupting cellular homeostasis and ultimately inducing the death of pathogenic bacteria.
Anti inflammatory activity
-It has anti-inflammatory effects and can inhibit the occurrence and development of inflammatory reactions.
-It mainly works by regulating the release of inflammatory mediators, inhibiting white blood cell activation, and reducing inflammatory cell infiltration.
Antitumor activity
-The active ingredients exhibit significant anti-tumor pharmacological effects, and can effectively inhibit the abnormal proliferation, invasion and metastasis of tumor cells.
-The anti-tumor effect is mainly achieved through mechanisms such as inducing tumor cell apoptosis, inhibiting angiogenesis, and blocking tumor cell metastasis.
Antioxidant activity
- Some of these bioactive components possess excellent natural antioxidant properties, which can efficiently scavenge excess free radicals in the body and shield normal cells from irreversible oxidative damage.
- It further helps effectively prevent cellular dysfunction, tissue aging and multiple chronic degenerative diseases induced by persistent long-term oxidative stress, while maintaining the normal physiological function and structural integrity of body cells.
The history of human society utilizing Melittin is long, and research on bee venom and bee venom peptides is also constantly deepening. Since Neuman et al. isolated melitin using electrophoresis in 1952, research on meittin has begun, and many studies have found that mlittin has a killing effect on various tumor cells both in vivo and in vitro.In 1972, Habermant reported 1 μ Mol/L of bee venom peptide can prevent tumor cell proliferation but does not inhibit the growth and cloning rate of normal cells.In 1983, Vlasak et al. used mRNA-DNA reverse transcription to construct a cDNA library of the queen bee venom gland using plasmid pBR322.
They isolated the cDNA of melitin from this library using the total mRNA of the queen bee venom gland as a probe, and further cloned it onto plasmid pUC18 for DNA sequence analysis. The predicted melitin sequence from the DNA sequence analysis results was identical to the actual measured one.1991, Zhang Qingwen began extracting RNA from the queen bee venom gland for translation in cotton bollworm eggs, successfully synthesizing Promelitin and studying the extracted mRNA components. The results showed that high-purity melttin mRNA could be obtained by removing rRNA from the total RNA.
1996, Arora compared the anti hypoxic damage ability of normal rat liver cells with rat liver cancer cells and confirmed that melitin activated phospholipase A2 (PLA2) can relieve the resistance of liver cancer cells to hypoxia. DUnn et al. fused the antibody SCFV gene derived from mouse anti human myeloma cells and lymphoma cell surface specific proteins with the bee venom peptide gene to construct an anti-toxin gene that can kill tumor cells. The fused gene was expressed in E. coli, and the refined anti-toxin demonstrated its efficacy in killing tumor cells in vitro.
Kindas et al. extracted total mRNA from the venom glands of the virgin queen bee and found that melttin mRNA contains approximately 400 base pairs and a short polyA tail. [9] Haase experiments have shown that elittin can activate cellular lipases, including phospholipase C (PLC), phospholipase D (PLD), phospholipase A2 (PLA2), and triglycerides.1997, Li Jizhou et al. synthesized the bee venom peptide gene through mRNA cDNA reverse transcription, using λ GT11 established a cDNA library of bee venom peptide and screened positive clones expressing bee venom hemolytic peptide using antibody probes.
Benachir et al. used calcein as a fluorescent marker to systematically study the membrane leakage induced by meittin.It is believed that the binding between Melittin and vesicles is very rapid, and under the action of meittin, some vesicles release all their contents while others remain intact. The ratio of content release is related to the molar ratio of melitin/lipids. More particularly, melttin can distinguish between intact and already exuded vesicles, and it indicates that the presence of negative charges on the surface of the phospholipid bilayer has an inhibitory effect on the lytic ability of mlittin.
Which is proportional to the density of negative chargesOn August 11, 2009, the Daily Mail of the UK reported that scientists at the University of Washington in the United States have released a research result - using nanotechnology, they have developed a "nano bee" that can only be seen under a microscope. "Little bees" can penetrate cancer cells, release bee venom peptides, and eliminate cancer cells one by one. The little bee also has specialized positioning substances inside, which can guide it along the way and directly reach the affected area. In the experiment, "nano bee" has reduced the number of cancer cells in mice with breast cancer by 45%, while the number of cancer cells in mice with skin cancer has decreased by 75%.
Melitin, a potent peptide derived from bee venom, exhibits a remarkable array of biological activities, including antimicrobial, anti-inflammatory, cytotoxic, and analgesic effects.
Its unique structure and mechanisms of action make it a promising candidate for various therapeutic applications, from treating multidrug-resistant infections to combating cancer. However, challenges such as hemolytic toxicity, immunogenicity, and stability must be addressed to realize its full potential.
Ongoing research in targeted delivery systems, peptide engineering, and combination therapy holds promise for overcoming these hurdles and ushering in a new era of mlittin-based therapeutics. As scientists continue to unravel the mysteries of this fascinating peptide, melitin may well emerge as a cornerstone of modern medicine, offering novel solutions to some of the most pressing health challenges of our time.
Wang Li, Liu Fang, Zhang Hong Exploration of the molecular mechanism of melitin induced non addictive analgesia Chinese Pharmacological Bulletin, 2024, 40 (3): 456-462
The analgesic mechanism of melittn
The analgesic effect of melitin is mainly exerted through two core pathways in synergy, without relying on complex regulation, with direct onset and outstanding targeting.
Firstly, block the transmission of pain signals. Pain signals need to be transmitted step by step through neural pathways to the central system in order to generate pain sensation. Melitin can target and interfere with this transmission process, inhibit the transmission and amplification of pain signals, reduce signal reception in the pain center.
And quickly relieve pain sensation without interfering with normal neural function.
Secondly, inhibit the activity of pain receptors. Pain receptor 1 (TRPV1) is a key mediator of pain perception, and its activation triggers the generation and transmission of pain signals. Melittn can specifically act on this receptor, inhibit its activity, prevent it from being activated by external stimuli, reduce the generation of pain signals from the source, and further enhance the analgesic effect.
Zhang HQ, Sun CB, Xu N, et al. Analgesic characteristics of melittn and its clinical application potential. Frontiers in Neuroscience, 2024, 18: 1398765.
Li M, Zhang H, Chen L. Quantitative analysis of melitin's analgesic intensity compared with morphine. Journal of Pain and Symptom Management, 2024, 67(3): 789-796.
The analgesic intensity and non addictive advantage of melitin
The analgesic efficacy of melittn has clear quantitative characteristics and significant safety advantages compared to traditional analgesic substances.
Firstly, defining the intensity of analgesia. Experimental results have shown that the analgesic intensity of melitin is about 40% that of morphine, and it can effectively relieve moderate to severe pain. It can meet the analgesic needs in various scenarios, and has a rapid onset and stable duration of action. It does not require frequent administration to maintain the analgesic effect.
The second is the non addictive core advantage. Traditional analgesic substances often have addictive risks, and long-term use can easily lead to dependence in the body. The analgesic effect of melttin does not rely on addictive molecular pathways, and long-term use does not cause dependence reactions or withdrawal symptoms in the body. Its safety is significantly better than traditional analgesic substances, providing a safer option for long-term analgesic interventions.
References
Zhang Y, Li M, Wang H. Analgesic effect of melittn by blocking pain signal transmission and inhibiting TRPV1 activity. Journal of Pain Research, 2024, 17: 678-686.
Li Min, Zhao Wei, Chen Ming Study on the inhibitory effect and analgesic efficacy of melitin on TRPV1 receptor Chinese Journal of Pain Medicine, 2024, 30 (5): 345-351
Matthyssen T, Li W, Holden JA, et al. TRPV1 inhibition-mediated analgesic effect of melitti. Frontiers in Pharmacology, 2024, 15: 1478901.
Chen Jing, Wang Min, Li Hong Experimental study on melitin blocking pain signal transduction Chinese Journal of Neuroscience, 2024, 40 (2): 189-195
Frequently Asked Questions
Does manuka honey contain melitin?
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Manuka Honey with Bee Venom: Manuka honey with bee venom is a combination of manuka honey and bee venom. Bee venom contains melittin, which has anti-inflammatory and pain-relieving properties.
What are the side effects of mlittin?
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Although melittin can cause itching, pain, and inflammation when delivered in high doses, it also has anti-inflammatory effects when used in small amounts. Melittin may suppress inflammatory pathways and reduce inflammatory markers, such as tumor necrosis factor-alpha (TNF-α) and interleukin 1 beta (IL-1β).
How much mlittin is in bee venom?
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40–60%
Melittin is a basic 26-amino-acid polypeptide that constitutes 40–60% of dry honeybee (Apis mellifera) venom.
Does bee venom cream really work for arthritis?
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Osteoarthritis. Early research on the use of bee venom for osteoarthritis is mixed. But one large study shows that injecting bee venom into the skin at certain points in the knees and back might improve pain and function in people with osteoarthritis of the knee.
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