Alotaibi Badriyah, Mokhtar Fatma Alzahraa, El-Masry Thanaa A, Elekhnawy Engy, Mostafa Sally A, Abdelkader Dalia H, Elharty Mohamed E, Saleh Asmaa, Negm Walaa A
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdulrahman University, Riyadh, 84428, Saudi Arabia.
Department of Pharmacognosy, Faculty of Pharmacy, ALsalam University, Al Gharbiyah, Egypt.
J Inflamm Res. 2021 Dec 29;14:7411-7430. doi: 10.2147/JIR.S345780. eCollection 2021.
The gastrointestinal tract (GIT) is vulnerable to various diseases. In this study, we explored the therapeutic effects of flower extract (BRFE) on GIT diseases.
Liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) was used for phytochemical identification of the compounds in BRFE. The antibacterial activity of BRFE was investigated, and its impact on the bacterial outer and inner membrane permeability and membrane depolarization (using flow cytometry) was studied. In addition, the immunomodulatory activity of BRFE was investigated in vitro on lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells (PBMCs) using quantitative reverse transcription polymerase chain reaction (qRT-PCR). Furthermore, the anti-inflammatory activity of BRFE was investigated by histopathological examination and qRT-PCR on indomethacin-induced gastric ulcers in rats.
LC-ESI-MS/MS phytochemically identified 57 compounds in BRFE for the first time. BRFE displayed antibacterial activity against bacteria that cause GIT infections, with increasing outer and inner membrane permeability. However, membrane depolarization was unaffected. BRFE also exhibited immunomodulatory activity in LPS-stimulated PBMCs by attenuating the upregulation of cyclooxygenase 2 (COX-2), inducible nitric oxide synthase (iNOS), interleukin (IL)-6, tumor necrosis factor-alpha (TNF-α), and nuclear factor kappa B (NF-κB) gene expression compared with untreated LPS-stimulated PBMCs. In addition, BRFE exhibited anti-inflammatory activity required for maintaining gastric mucosa homeostasis by decreasing neutrophil infiltration with subsequent myeloperoxidase production, in addition to an increase in glutathione peroxidase (GPx) activity. Histopathological findings presented the gastroprotective effects of BRFE, as a relatively normal stomach mucosa was found in treated rats. In addition, BRFE modulated the expression of genes encoding IL-10, NF-κB, GPx, and myeloperoxidase (MPO).
BRFE can be a promising source of therapeutic agents for treatment of GIT diseases.
胃肠道(GIT)易患多种疾病。在本研究中,我们探讨了花提取物(BRFE)对胃肠道疾病的治疗作用。
采用液相色谱-电喷雾电离-串联质谱(LC-ESI-MS/MS)对BRFE中的化合物进行植物化学鉴定。研究了BRFE的抗菌活性,并通过流式细胞术研究了其对细菌外膜和内膜通透性以及膜去极化的影响。此外,使用定量逆转录聚合酶链反应(qRT-PCR)在体外研究了BRFE对脂多糖(LPS)刺激的外周血单核细胞(PBMC)的免疫调节活性。此外,通过组织病理学检查和qRT-PCR研究了BRFE对吲哚美辛诱导的大鼠胃溃疡的抗炎活性。
LC-ESI-MS/MS首次从植物化学角度鉴定出BRFE中的57种化合物。BRFE对引起胃肠道感染的细菌具有抗菌活性,可增加外膜和内膜通透性。然而,膜去极化未受影响。与未处理的LPS刺激的PBMC相比,BRFE还通过减弱环氧合酶2(COX-2)、诱导型一氧化氮合酶(iNOS)、白细胞介素(IL)-6、肿瘤坏死因子-α(TNF-α)和核因子κB(NF-κB)基因表达的上调,在LPS刺激的PBMC中表现出免疫调节活性。此外,BRFE通过减少中性粒细胞浸润及随后的髓过氧化物酶产生,以及增加谷胱甘肽过氧化物酶(GPx)活性,表现出维持胃黏膜稳态所需的抗炎活性。组织病理学结果显示了BRFE的胃保护作用,因为在治疗的大鼠中发现胃黏膜相对正常。此外,BRFE调节了编码IL-10、NF-κB、GPx和髓过氧化物酶(MPO)的基因表达。
BRFE有望成为治疗胃肠道疾病的治疗药物来源。