Apamin
Apamin
CAS: 24345-16-2
Molecular Formula: C79H131N31O24S4
Apamin - Names and Identifiers
| Name | Apamin |
| Synonyms | APAMIN Apamin APAMIN (HONEYBEE, APIS MELLIFERA) CYS-ASN-CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-CYS-ALA-ARG-CYS-GLN-GLN-HIS-NH2 CYS-ASN-CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-CYS-ALA-ARG-ARG-CYS-GLN-GLN-HIS-NH2 H-CYS-ASN-CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-CYS-ALA-ARG-ARG-CYS-GLN-GLN-HIS-NH2 H-+CYS-ASN-++CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-+CYS-ALA-ARG-ARG-++CYS-GLN-GLN- HIS-NH2 H-Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Cys1-Cys11, Cys3-Cys15) |
| CAS | 24345-16-2 |
| EINECS | 246-182-7 |
| InChI | InChI=1/C79H131N31O24S4/c1-35(2)26-49-70(127)107-51-31-136-135-30-41(81)63(120)105-50(28-57(84)114)71(128)108-53(73(130)99-42(12-7-8-22-80)64(121)96-38(5)77(134)110-25-11-15-54(110)75(132)102-47(18-21-58(115)116)69(126)109-59(39(6)111)76(133)95-37(4)62(119)104-49)33-138-137-32-52(106-66(123)44(14-10-24-92-79(88)89)98-65(122)43(13-9-23-91-78(86)87)97-61(118)36(3)94-72(51)129)74(131)101-45(16-19-55(82)112)67(124)100-46(17-20-56(83)113)68(125)103-48(60(85)117)27-40-29-90-34-93-40/h29,34-39,41-54,59,111H,7-28,30-33,80-81H2,1-6H3,(H2,82,112)(H2,83,113)(H2,84,114)(H2,85,117)(H,90,93)(H,94,129)(H,95,133)(H,96,121)(H,97,118)(H,98,122)(H,99,130)(H,100,124)(H,101,131)(H,102,132)(H,103,125)(H,104,119)(H,105,120)(H,106,123)(H,107,127)(H,108,128)(H,109,126)(H,115,116)(H4,86,87,91)(H4,88,89,92)/t36?,37-,38-,39+,41-,42-,43-,44?,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,59?/m0/s1 |
Apamin - Physico-chemical Properties
| Molecular Formula | C79H131N31O24S4 |
| Molar Mass | 2027.34 |
| Density | 1.63 |
| Boling Point | 847.17°C (rough estimate) |
| Solubility | 0.05 M acetic acid: 5mg/mL, clear, colorless to faintly yellow |
| Appearance | White solid with dark tan cast |
| Merck | 13,732 |
| Storage Condition | -20°C |
| Refractive Index | 1.5530 (estimate) |
| MDL | MFCD00167944 |
| In vitro study | Apamin (0.5-2 µg/mL; 24 hours; HSC-T6 cells) treatment markedly reduces the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Apamin treatment abrogats the activation of p-Smad2/3 and Smad4 induced by TGF-β1. Western Blot Analysis Cell Line: HSC-T6 cells Concentration: 0.5 µg/mL, 1 µg/mL and 2 µg/mL Incubation Time: 24 hours Result: Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1. |
| In vivo study | Apamin (0.1 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; C57BL/6 male mice) treatment results in decreased liver injury and proinflammatory cytokine levels. Apamin suppresses the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-fed mice. Animal Model: 8-week-old C57BL/6 male mice (20-25 g) with DDC feeding Dosage: 0.1 mg/kg Administration: Intraperitoneal injection; twice a week; for 4 weeks Result: Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice. |
Apamin - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| UN IDs | 2811 |
| WGK Germany | 3 |
| RTECS | CD6899900 |
| FLUKA BRAND F CODES | 3-10 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 i.v. in mice: 4 mg/kg (Habermann, Reiz); LD50 intracerebroventricularly in mice: 12 ng/animal (Labbé-Jullié) |
Apamin - Introduction
Amino acid sequence Cys-Asn-Cys-Lys-Ala-Pro-G?lu-Thr-Ala-Leu-Cys-Ala-Ar?g-Arg-Cys-Gln-Gln-His-NH2? [Disulfide Bridges: 1-11, 3-15]
Last Update：2022-10-16 17:15:13
Apamin - Reference Information
| Introduction | melittin is an 18 amino acid peptide neurotoxin found in melittin, it is a specific and selective blocker of Ca2-activated K (SK) channels with anti-inflammatory and anti-fibrotic effects. |
| pharmacological effects | (1) effects on the nervous system: it can block the conduction of inhibitory impulse that innervates the smooth muscle of the gastrointestinal tract, the gastrointestinal smooth muscle excitability is enhanced, and the contraction state; Can act on the intermediate neurons of the spinal cord, the descending reticular spinal cord and vestibular spinal cord, or the central gray matter around the cerebral aqueduct, organic synergy that affects action. (2) strong heart, anti-arrhythmic effect: has a strong p-epinephrine-like effect, expand the coronary, increase myocardial blood supply, so that myocardial contractility is significantly enhanced, heart rate, heart pump blood function is enhanced, can be used to treat heart failure; With isoproterenol-like effect, and than isoproterenol maintenance time (about 10 times), anti-arrhythmia. (3) increase capillary permeability and improve microcirculation. (4) anti-inflammatory, regulating immunity: directly increase plasma cortisol or stimulate the pituitary-adrenal system to promote the secretion of cortical hormones; Inhibit serotonin activity. (5) nutritional repair of muscular dystrophy cells: in the tonic muscle, there is a melittin peptide receptor, and the bee venom peptide plays a role in the treatment of the vegetative muscle cells by binding to its receptor. Can be used for the treatment of ankylosing spondylitis, multiple sclerosis. |
| Application | melittin accounts for 3% of dry weight of bee venom and is an important polypeptide in bee venom. Melittin is the smallest neurotoxic peptide in animal neurotoxins. It can cross the blood-brain barrier through various routes of administration and act on the central nervous system. Myotonic dystrophy, melittin peptide receptor, therefore, melittin peptide on the treatment of muscular dystrophy. |
| biological activity | Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in melittin, it is a specific and selective blocker of Ca2-activated K (SK) channels with anti-inflammatory and anti-fibrotic effects. |
| Target | K channel |
| in vitro study | Apamin (0.5-2 µg/mL; 24 hours; HSC-T6 cells) treatment marked reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. the activation of p-Smad2/3 and Smad4 induced by TGF-β1. Western Blot Analysis Cell Line: HSC-T6 cells Concentration: 0.5 µg/mL, 1 µg/mL and 2 µg/mL Incubation Time: 24 hours Result: Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1. |
| Cell Line: | HSC-T6 cells |
| Concentration: | 0.5 µg/mL, 1 µg/mL and 2 µg/mL |
| Incubation Time: | 24 hours |
| Result: | Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1. Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice. |
| in vivo study | Apamin (0.1 mg/kg; Intraperone injection; twice a week; for 4 weeks; c57BL/6 male mice) treatment results. Apamin preferences the disposition of collagen, propagation of BECs and expression of fibrogenic genes in the 3, 5-diethooxycarbonyl-1, 4-dihydroxycollidine (DDC)-micfed E. Animal Model: 8-week-old C57BL/6 male mice (20-25 g) with DDC feeding Dosage: 0.1 mg/kg Administration: Intraperitoneal injection; twice a week; for 4 weeks Result: Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice. |
| Animal Model: | 8-week-old C57BL/6 male mice (20-25 g) with DDC feeding |
| Dosage: | 0.1 mg/kg |
| Administration: | Intraperitoneal injection; twice a week; for 4 weeks |
| category | toxic substances |
| toxicity grade | highly toxic |
| Acute toxicity | intraperitoneal-mouse LD50: 3.8 mg/kg; Intravenous-mouse LD50: 4 mg/kg |
| flammability hazard characteristics | flammability; Toxic nitrogen oxide and sulfur oxide fumes from combustion |
| storage and transportation characteristics | The warehouse is ventilated and dried at low temperature; Stored separately from food raw materials |
| fire extinguishing agent | dry powder, foam, sand, carbon dioxide, water mist |
Last Update：2024-04-09 21:31:59
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