Richard Seidu A, Kampo Sylvanus, Sackey Marian, Hechavarria Maite Esquijarosa, Buunaaim Alexis D B
Department of Medicine, Princefield University, P.O. Box MA128, Ho, Ghana.
Department of Anesthesia and Critical Care, School of Medicine, University of Health and Allied Sciences, Ho, Ghana.
Evid Based Complement Alternat Med. 2020 Oct 29;2020:4234273. doi: 10.1155/2020/4234273. eCollection 2020.
Scorpion -analgesic-antitumor peptide (BmK AGAP) has been used to treat diseases like tetanus, tuberculosis, apoplexy, epilepsy, spasm, migraine headaches, rheumatic pain, and cancer in China. AGAP is a distinctive long-chain scorpion toxin with a molecular mass of 7142 Da and composed of 66 amino acids cross-linked by four disulfide bridges. Voltage-gated sodium channels (VGSCs) are present in excitable membranes and partakes in essential roles in action potentials generation as compared to the significant function of voltage-gated calcium channels (VGCCs). A total of nine genes (Na1.1-Na1.9) have been recognized to encode practical sodium channel isoforms. Na1.3, Na1.7, Na1.8, and Na1.9 have been recognized as potential targets for analgesics. Na1.8 and Na1.9 are associated with nociception initiated by inflammation signals in the neuronal pain pathway, while Na1.8 is fundamental for neuropathic pain at low temperatures. AGAP has a sturdy inhibitory influence on both viscera and soma pain. AGAP potentiates the effects of MAPK inhibitors on neuropathic as well as inflammation-associated pain. AGAP downregulates the secretion of phosphorylated p38, phosphorylated JNK, and phosphorylated ERK 1/2 . AGAP has an analgesic activity which may be an effective therapeutic agent for pain management because of its downregulation of PTX3 via NF-B and Wnt/beta-catenin signaling pathway. In cancers like colon cancer, breast cancer, lymphoma, and glioma, rAGAP was capable of blocking the proliferation. Thus, AGAP is a promising therapy for these tumors. Nevertheless, research is needed with other tumors.
蝎镇痛抗肿瘤肽（BmK AGAP）在中国已被用于治疗破伤风、结核病、中风、癫痫、痉挛、偏头痛、风湿性疼痛和癌症等疾病。AGAP是一种独特的长链蝎毒素，分子量为7142 Da，由66个氨基酸组成，通过四个二硫键交联。电压门控钠通道（VGSCs）存在于可兴奋膜中，与电压门控钙通道（VGCCs）的重要功能相比，在动作电位产生中起重要作用。总共已识别出九个基因（Na1.1-Na1.9）编码功能性钠通道亚型。Na1.3、Na1.7、Na1.8和Na1.9已被认为是镇痛药的潜在靶点。Na1.8和Na1.9与神经元疼痛通路中炎症信号引发的伤害感受有关，而Na1.8是低温下神经性疼痛的基础。AGAP对内脏和躯体疼痛都有强烈的抑制作用。AGAP增强了MAPK抑制剂对神经性疼痛以及炎症相关疼痛的作用。AGAP下调磷酸化p38、磷酸化JNK和磷酸化ERK 1/2的分泌。AGAP具有镇痛活性，由于其通过NF-κB和Wnt/β-连环蛋白信号通路下调PTX3，可能是一种有效的疼痛管理治疗剂。在结肠癌、乳腺癌、淋巴瘤和神经胶质瘤等癌症中，重组AGAP能够阻断增殖。因此，AGAP是这些肿瘤的一种有前途的治疗方法。然而，还需要对其他肿瘤进行研究。
