来自Euphorbia desmondiiEuphorbia desmondiiEuphorbia desmondii的欧和提鲁卡三烯具有三酸性活性
Muhammad Bello Saidu1, Gordana Krstić1,2, Anita Barta1
1Department of Pharmacognosy, University of Szeged, Eötvös u. 6, 6720 Szeged, Hungary.
Journal of natural products
|September 14, 2024
概括
研究人员从Euphorbia desmondii中分离出了新型的三类植物,证明了对Trypanosoma cruzi的强烈抗性活性. 几种化合物显示出显著的选择性,为新的查加斯病治疗提供了潜在的支架.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 寄生虫学的寄生虫学
背景情况:
- 由Trypanosoma cruzi引起的查加斯病仍然是一个重要的全球健康问题,治疗选择有限.
- 自然产品为抗寄生虫感染的新型治疗剂提供了丰富的来源.
研究的目的:
- 从Euphorbia desmondii中分离和描述新的三类植物.
- 为了评估这些化合物对Trypanosoma cruzi的tripanocidal活性.
- 确定潜在的化合物,用于开发抗毒药物.
主要方法:
- 使用广泛的光谱分析 (NMR,MS) 对Euphorbia desmondii的植物化学研究.
- 隔离和结构阐明15种新的三类化合物 (desmondiins A,C-P) 和8种已知的化合物.
- 在实验室中对Trypanosoma cruzi表皮菌和表皮菌的选择性tripanocidal活性进行了评估,使用RAW264.7巨细胞作为宿主细胞.
主要成果:
- 隔离和鉴定了15种新的提鲁卡和欧三基,德斯蒙第因A,C-P.
- 德斯蒙第因A,C,D,F,H和M对T. cruzi表皮虫有显著的活性 (IC50: 3-5μM),选择性指数为5-9.
- 德斯蒙丁 A 已证明强烈抑制了阿马斯蒂哥特的复制 (IC50 = 2.5 ± 0.3 μM),与本兹尼达可比.
结论:
- 从Euphorbia desmondii中分离出来的euphane和tirucallane三类化合物具有显著的抗性潜力.
- 德斯蒙丁A是一种有前途的候选物,可以作为抗查加斯病治疗剂进一步开发.
- 这些三类化合物代表了设计针对夏加斯病的新药的有价值的脚架.
相关概念视频
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
141
Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
141
01:21Drugs Affecting Neurotransmitter Release or Uptake
1.0K
Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
1.0K
01:17Sedatives and Hypnotics Drugs: Miscellaneous Agents
159
Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
159
01:15Opioid Analgesics: Synthetic and Semisynthetic Opioids
251
Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
251