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An Overview of COVID-19 Treatment
Published in Hanadi Talal Ahmedah, Muhammad Riaz, Sagheer Ahmed, Marius Alexandru Moga, The Covid-19 Pandemic, 2023
Saffora Riaz, Farkhanda Manzoor, Dou Deqiang, Najmur Rahman
Flavonoid scutellarein from the base of Scutellaria baicalensis naturally having antiviral compounds has been used to treat SARS-CoV-2. Its antiviral Flavonoids control infection by their ATPase activity. The triterpenes of Camellia japonica were reported for massive antiviral action against the COVID [112].
Marine Algal Secondary Metabolites Are a Potential Pharmaceutical Resource for Human Society Developments
Published in Se-Kwon Kim, Marine Biochemistry, 2023
Somasundaram Ambiga, Raja Suja Pandian, Lazarus Vijune Lawrence, Arjun Pandian, Ramu Arun Kumar, Bakrudeen Ali Ahmed Abdul
Polyphenols are classified into many types. They are phenolic acids, flavonoids, epigallate, epicatechin, anthocyanidins, gallic acids, tannins and catechin. Polyphenols have much potential to reduce the mitotic index. Also, the levels of cellular proteins were decrease which needed for the cancer cell proliferation and colony formation. For instance, due to the cytotoxic activities of compound, Scutellarein 4′-methylether exhibits effect of anticancer in vivo and in vitro. This compound is isolated from the marine algae Osmundea pinnatifida, and it is used in the treatment of choriocarcinoma cancer (Spada et al., 2008).
Scutellaria Species and Cancer Research
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Samantha H. Sherman, Lani Irvin, Prahlad Parajuli, Nirmal Joshee
Another compound, scutellarein, demonstrated significant suppression of human fibrosarcoma cells (HT1080) by inducing apoptosis, while in in vivo experiments using Balb/c mice exhibited a decrease in tumor size and volume. Furthermore, scutellarein showed anti-metastatic activity as depicted by reduced migration and invasion of HT1080 cells, besides suppression of matrix metalloproteinase (MMP)-2, -9 and -14 (Shi et al., 2015).
Application of the Mannich reaction in the structural modification of natural products
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li, Qing-Kun Shen
Oxidative stress plays a key role in ischaemic cerebrovascular disease101. Research shows that Scutellarin can improve microcirculation, dilate blood vessels, inhibit platelet aggregation, and increase cerebral blood flow102. Furthermore, scutellarin is clinically used in China to treat acute cerebral infarction and paralysis caused by cerebrovascular diseases such as hypertension, cerebral haemorrhage, and cerebral thrombosis103. Scutellarein is a hydrolysate of scutellarin that has a strong protective effect against cerebral ischaemia. Docking studies of thrombin (2R2M) with scutellarein indicated that the B- and C-rings of the ligand interacted well with the S1 and S2 pockets, respectively. However, ring A could only partially interact with the S3 pocket of thrombin. Zhong et al.104 synthesised the compound LR3d through the Mannich reaction and evaluated its biological activity. The results showed that morpholinyl aminomethylene substituent derivative LR3d exhibited stronger anticoagulant ability and better antioxidant activity than scutellarein.
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Hongbo Liu, Fei Ye, Qi Sun, Hao Liang, Chunmei Li, Siyang Li, Roujian Lu, Baoying Huang, Wenjie Tan, Luhua Lai
Based on the docking analysis, we searched for baicalein analogues from available flavonoid suppliers and selected eight flavonoids and two glycosides for experimental testing (Table 2). The docking scores are given in Table S1. Four flavonoid compounds were found to be potent SARS-CoV-2 3CLpro inhibitors. Among them, scutellarein is mainly distributed in genus Scutellaria and Erigerontis herba (Dengzhanxixin or Dengzhanhua in Chinese) in its glucuronide form, scutellarin. Scutellarin has long been used in cardiovascular disease treatment for its ability to improve cerebral blood supply37. As shown in Figure 4, scutellarein inhibits SARS-CoV-2 3CLpro with an IC50 value of 5.8 µM, while scutellarin showed mild inhibitory activity at 50 µM concentration. The other three flavonoid compounds, dihydromyricetin, quercetagetin, and myricetin derived from Ampelopsis japonica (Bailian in Chinese), Eriocaulon buergerianum (Gujingcao in Chinese), and Polygoni avicularis (Bianxu in Chinese), respectively, inhibit SARS-CoV-2 3CLpro with IC50 values of 1.20, 1.24, and 2.86 µM. Interestingly, scutellarein and myricetin were reported to inhibit the SARS-CoV, indicating their potential as multi-target anti-SARS-CoV-2 agents38.
Inhibition of CYP3A4 and CYP3A5 expression by scutellarin is not mediated via the regulation of hsa-miR-27a, 27b, 148a, 298 and 451a levels
Published in Xenobiotica, 2020
Weiyao Ding, Change Cao, Yangyang Gao, Xuan Zhou, Yong Lai
This is our preliminary experimental conclusion, and it still exists several limitations. First, MicroRNAs are widely involved in post-transcriptional gene regulation, they recognise target mRNAs and exert their roles predominantly in the cytoplasm and nucleus (Wei et al., 2014). Microamounts of microRNAs have been found in the microblood balloon, and seem to be resistant to rapid degradation by ribonucleases (RNases) in plasma. Both the choice of specimen, the presence of cellular contaminants such as platelets or erythrocytes, and the imprecision introduced from the day-to-day setup of the extraction and amplification procedures will influence the miRNAs level in plasma(McDonald JS et al., 2011). Namely, microRNAs level in human plasma may not equate to that in human liver. Second, scutellarin was absorbed in the form of its hydrolysate scutellarein, after oral administration. Scutellarein is the active metabolite of scutellarin in vivo, it may bind to CYP enzyme and later makes a time-dependent inhibition of scutellarin on CYP enzyme. Therefore, the temporal dependence of scutellarin on CYP3A enzyme should be considered. Our future research will study the role of miRNA in the down-regulation of scutellarin-induced CYP3A expression in HepG2 cells by miRNAs plasmid transfection. At the same time, we will explore whether the inhibition of scutellarin on CYP3A enzyme was related to the time-dependent inhibition, and explore the effect of scutellarein on the expression of CYP3A enzyme. Later, we will study the effect of scutellarin on the post-transcriptional nuclear factors, such as PXR, CAR and VDR, PPARα, to clarify the regulatory mechanism.