Shoaib Mohammad, Shah Syed Wadood Ali, Ali Niaz, Shah Ismail, Shafiullah -, Ayaz Muhammad, Tahir Muhammad Nawaz, Akhtar Sohail, Ayub Muhammad Tahir
Department of Pharmacy, University of Malakand, Khyber Pakhtunkhwa, Pakistan.
Department of Pharmacology, Institute of Basic Medical Sciences, Khyber Medical University, Khyber Pakhtunkhwa, Pakistan.
Pak J Pharm Sci. 2017 Sep;30(5):1573-1580.
Flavonoids are phenolic compounds that have always attracted pharmaceutical researchers and food manufacturers. Nature has indirectly provided us flavones in our daily diet i.e. tea, fruits, juices and vegetables. Flavones have got special position in research field of natural and synthetic organic chemistry due to their biological capabilities. Flavone derivative has been synthesized in good yield from ketone and corresponding aldehydes. The structures have been established by different spectroscopic techniques like H NMR, C NMR, IR and elemental analysis. The compounds were then screened for its acute toxicity and antinociceptive response in mice models with writhings induced by acetic acid, tail immersion and formalin-induced nociception assay procedures and structure activity relationship was established. The compounds were safe up to a maximum dose of 1200 mg/kg body weight in mice. The effects following pretreatment with naloxone were also studied to reveal the involvement of opioid receptors in the antinociceptive action. The flavone derivatives showed significant reduction in number of abdominal constrictions, increase in paw licking response time in both phases and a significant raise in latency time in nociception models. Moreover, the antinociceptive response was significantly attenuated by pretreatment with naloxone suggesting the involvement of opioid system in the antinociceptive action. The promising effects were shown by halogenated flavone. The flavone derivatives showed analgesic response in all models of nociception suggesting the involvement of opioid system in the antinociceptive action.
黄酮类化合物是一类酚类化合物，一直吸引着药物研究人员和食品制造商。大自然在我们的日常饮食中，如茶、水果、果汁和蔬菜中，间接地为我们提供了黄酮。由于黄酮的生物学特性，它们在天然和合成有机化学研究领域中占据特殊地位。黄酮衍生物已由酮和相应的醛以良好的产率合成。其结构已通过不同的光谱技术如氢核磁共振（H NMR）、碳核磁共振（C NMR）、红外光谱（IR）和元素分析得以确定。然后，在小鼠模型中，通过乙酸诱导扭体、尾部浸浴和福尔马林诱导疼痛测定程序，对这些化合物进行急性毒性和抗伤害感受反应的筛选，并建立结构活性关系。在小鼠中，这些化合物在高达1200毫克/千克体重的最大剂量下是安全的。还研究了用纳洛酮预处理后的效果，以揭示阿片受体在抗伤害感受作用中的参与情况。黄酮衍生物在腹部收缩次数上显著减少，在两个阶段的舔爪反应时间增加，并且在疼痛模型中的潜伏期时间显著延长。此外，用纳洛酮预处理后，抗伤害感受反应显著减弱，这表明阿片系统参与了抗伤害感受作用。卤代黄酮显示出有前景的效果。黄酮衍生物在所有疼痛模型中均显示出镇痛反应，表明阿片系统参与了抗伤害感受作用。
