Ghareeb Mosad A, Sobeh Mansour, Aboushousha Tarek, Esmat Marwa, Mohammed Hala Sh, El-Wakil Eman S
Medicinal Chemistry Department, Theodor Bilharz Research Institute, Kornaish El-Nile, Warrak El-Hadar, Imbaba, Giza 12411, Egypt.
AgroBioSciences, Mohammed VI Polytechnic University, Lot 660, Hay Moulay Rachid, Ben-Guerir 43150, Morocco.
Pharmaceutics. 2023 Jan 26;15(2):415. doi: 10.3390/pharmaceutics15020415.
J.Gay is widely used in folk medicine to treat hernia. The present study aimed to annotate the phytoconstituents of aerial-part extract and investigate its in vivo anticryptosporidial activity. The chemical characterization was achieved via the LC-ESI-MS/MS technique resulting in the annotation of 37 phytocompounds comprising flavonoids and phenolic acids. Regarding the anticryptosporidial activity, fifty dexamethasone-immunosuppressed mice were separated into five groups: GI, un-infected (normal control); GII, infected but not treated (model); GIII, infected and received NTZ, the reference drug; GIV, infected and received extract (100 mg/kg); and GV, infected and received extract (200 mg/kg). When GIII, GIV, and GV were compared to GII, parasitological analyses displayed highly significant differences in the mean numbers of oocysts in the stool between the different groups. GV demonstrated the highest efficacy of 79%. Histopathological analyses displayed improvement in the small intestine and liver pathology in the treated groups (GIII, IV, and V) related to the model (GII), with GV showing the highest efficacy. Moreover, the docking-based study tentatively highlighted the potential of benzoic acid derivatives as lactate dehydrogenase inhibitors. The docked compounds showed the same binding interactions as oxamic acid, where they established H-bond interactions with ARG-109, ASN-140, ASP-168, ARG-171, and HIS-195. To sum up, is a promising natural therapeutic agent for cryptosporidiosis.
J.Gay在民间医学中被广泛用于治疗疝气。本研究旨在注释地上部分提取物的植物成分,并研究其体内抗隐孢子虫活性。通过LC-ESI-MS/MS技术进行化学表征,结果注释出37种植物化合物,包括黄酮类和酚酸类。关于抗隐孢子虫活性,将50只地塞米松免疫抑制小鼠分为五组:GI,未感染(正常对照);GII,感染但未治疗(模型);GIII,感染并接受参考药物硝唑尼特(NTZ);GIV,感染并接受提取物(100mg/kg);GV,感染并接受提取物(200mg/kg)。当将GIII、GIV和GV与GII进行比较时,寄生虫学分析显示不同组之间粪便中卵囊平均数量存在高度显著差异。GV显示出最高疗效,为79%。组织病理学分析显示,与模型组(GII)相比,治疗组(GIII、IV和V)的小肠和肝脏病理学有所改善,GV显示出最高疗效。此外,基于对接的研究初步突出了苯甲酸衍生物作为乳酸脱氢酶抑制剂的潜力。对接的化合物显示出与草氨酸相同的结合相互作用,它们与ARG-109、ASN-140、ASP-168、ARG-171和HIS-195建立了氢键相互作用。综上所述,J.Gay是一种有前景的隐孢子虫病天然治疗剂。