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2.
Toxins (Basel) ; 12(3)2020 03 19.
Artigo em Inglês | MEDLINE | ID: mdl-32204567

RESUMO

Bee venom is a natural toxin produced by honeybees and plays an important role in defending bee colonies. Bee venom has several kinds of peptides, including melittin, apamin, adolapamine, and mast cell degranulation peptides. Apamin accounts for about 2%-3% dry weight of bee venom and is a peptide neurotoxin that contains 18 amino acid residues that are tightly crosslinked by two disulfide bonds. It is well known for its pharmacological functions, which irreversibly block Ca2+-activated K+ (SK) channels. Apamin regulates gene expression in various signal transduction pathways involved in cell development. The aim of this study was to review the current understanding of apamin in the treatment of apoptosis, fibrosis, and central nervous system diseases, which are the pathological processes of various diseases. Apamin's potential therapeutic and pharmacological applications are also discussed.


Assuntos
Apamina/uso terapêutico , Aterosclerose/tratamento farmacológico , Venenos de Abelha/química , Sistema Nervoso Central/efeitos dos fármacos , Cirrose Hepática/tratamento farmacológico , Canais de Potássio Cálcio-Ativados/antagonistas & inibidores , Apamina/isolamento & purificação , Apoptose/efeitos dos fármacos , Aterosclerose/metabolismo , Sistema Nervoso Central/patologia , Citocinas/antagonistas & inibidores , Fibrose , Humanos , Cirrose Hepática/patologia
3.
Toxins (Basel) ; 7(4): 1126-50, 2015 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-25835385

RESUMO

While knowledge of the composition and mode of action of bee and wasp venoms dates back 50 years, the therapeutic value of these toxins remains relatively unexploded. The properties of these venoms are now being studied with the aim to design and develop new therapeutic drugs. Far from evaluating the extensive number of monographs, journals and books related to bee and wasp venoms and the therapeutic effect of these toxins in numerous diseases, the following review focuses on the three most characterized peptides, namely melittin, apamin, and mastoparan. Here, we update information related to these compounds from the perspective of applied science and discuss their potential therapeutic and biotechnological applications in biomedicine.


Assuntos
Apamina , Meliteno , Peptídeos , Venenos de Vespas , Animais , Apamina/farmacologia , Apamina/uso terapêutico , Humanos , Peptídeos e Proteínas de Sinalização Intercelular , Meliteno/farmacologia , Meliteno/uso terapêutico , Peptídeos/farmacologia , Peptídeos/uso terapêutico , Venenos de Vespas/farmacologia , Venenos de Vespas/uso terapêutico
4.
Arch Pharm Res ; 37(8): 1016-31, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24293065

RESUMO

Diabetes is one of the leading causes of impaired wound healing. The objective of this study was to develop a bee venom-loaded wound dressing with an enhanced healing and anti-inflammatory effects to be examined in diabetic rats. Different preparations of polyvinyl alcohol (PVA), chitosan (Chit) hydrogel matrix-based wound dressing containing bee venom (BV) were developed using freeze-thawing method. The mechanical properties such as gel fraction, swelling ratio, tensile strength, percentage of elongation and surface pH were determined. The pharmacological activities including wound healing and anti-inflammatory effects in addition to primary skin irritation and microbial penetration tests were evaluated. Moreover, hydroxyproline, glutathione and IL-6 levels were measured in the wound tissues of diabetic rats. The bee venom-loaded wound dressing composed of 10 % PVA, 0.6 % Chit and 4 % BV was more swellable, flexible and elastic than other formulations. Pharmacologically, the bee venom-loaded wound dressing that has the same previous composition showed accelerated healing of wounds made in diabetic rats compared to the control. Moreover, this bee venom-loaded wound dressing exhibited anti-inflammatory effect that is comparable to that of diclofenac gel, the standard anti-inflammatory drug. Simultaneously, wound tissues covered with this preparation displayed higher hydroxyproline and glutathione levels and lower IL-6 levels compared to control. Thus, the bee venom-loaded hydrogel composed of 10 % PVA, 0.6 % Chit and 4 % BV is a promising wound dressing with excellent forming and enhanced wound healing as well as anti-inflammatory activities.


Assuntos
Anti-Inflamatórios/uso terapêutico , Apamina/uso terapêutico , Quitosana/química , Reagentes de Ligações Cruzadas/química , Diabetes Mellitus Experimental/complicações , Portadores de Fármacos/química , Álcool de Polivinil/química , Cicatrização/efeitos dos fármacos , Aloxano/farmacologia , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/efeitos adversos , Anti-Inflamatórios/farmacologia , Apamina/administração & dosagem , Apamina/efeitos adversos , Apamina/farmacologia , Infecções Bacterianas/microbiologia , Infecções Bacterianas/prevenção & controle , Fenômenos Químicos , Química Farmacêutica , Composição de Medicamentos , Hidrogéis , Masculino , Ratos Wistar , Pele/efeitos dos fármacos , Pele/lesões , Pele/microbiologia , Cicatrização/imunologia , Ferimentos Penetrantes/complicações , Ferimentos Penetrantes/tratamento farmacológico , Ferimentos Penetrantes/imunologia , Ferimentos Penetrantes/microbiologia
5.
Pharmacol Ther ; 115(2): 246-70, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17555825

RESUMO

Bee venom (BV) therapy (BVT), the therapeutic application of BV, has been used in traditional medicine to treat diseases, such as arthritis, rheumatism, pain, cancerous tumors, and skin diseases. BV contains a variety of peptides, including melittin, apamin, adolapin, the mast-cell-degranulating (MCD) peptide, enzymes (i.e., phospholipase [PL] A(2)), biologically active amines (i.e., histamine and epinephrine), and nonpeptide components which have a variety of pharmaceutical properties. BV has been reported to have anti-arthritis effects in several arthritis models. Melittin, a major peptide component of BV, has anti-inflammatory and anti-arthritis properties, and its inhibitory activity on nuclear factor kappaB (NF-kappaB) may be essential for the effects of BV. The anti-nociceptive effects of BV have also been demonstrated in thermal, visceral, and inflammatory pain models. Apcupoint stimulation (apipuncture) therapy into subcutaneous region may be important in the BV-induced anti-nociceptive effects. Multiple mechanisms, such as activation of the central and spinal opiod receptor, and alpha(2)-adrenergic activity, as well as activation of the descending serotonergic pathway have been suggested. The inhibition of c-Fos expression in the spinal cord by BV apipuncture in several nociceptive models is also reported to be a possible mechanism. BV also has anti-cancer activity. The cell cytotoxic effects through the activation of PLA(2) by melittin have been suggested to be the critical mechanism for the anti-cancer activity of BV. The conjugation of cell lytic peptide (melittin) with hormone receptors and gene therapy carrying melittin can be useful as a novel targeted therapy for some types of cancer, such as prostate and breast cancer.


Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/uso terapêutico , Antirreumáticos/uso terapêutico , Venenos de Abelha/uso terapêutico , Terapia por Acupuntura , Analgésicos/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Antirreumáticos/química , Antirreumáticos/farmacologia , Apamina/uso terapêutico , Artrite Reumatoide/tratamento farmacológico , Venenos de Abelha/química , Venenos de Abelha/farmacologia , Humanos , Hialuronoglucosaminidase/uso terapêutico , Peptídeos e Proteínas de Sinalização Intercelular , Meliteno/uso terapêutico , Peptídeos/uso terapêutico , Dermatopatias/tratamento farmacológico
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