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Herbal Anti-Arthritic Drug Discovery Tool Based on Inflammatory Biomarkers
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Mahfoozur Rahman, Ankit Sahoo, Sarwar Beg
Camellia (family Theaceae) is a species of evergreen shrub or small tree whose leaves and leaf buds are used to produce tea. Extract of green tea shows anti-arthritic potential when given orally at 200 mg/kg. Extract of green tea contains epigallocatechin-3-gallate (EGCG) as active constituents. Whereas its administration into the arthritic rats’ results to retards the release of IL-1 induced glycosaminoglycan via blocking the activity of NF-RB in chondrocytes. Further-more, it also inhibits NO synthase (iNOS) which stimulated by IL-1, JNK action, and NO. These three inflammatory biomarkers induce the destruction of cartilage (Ahmed, 2010; Datta et al., 2012). Whereas the RA synovial fibroblasts contain TNF-a-induced ERK (extracellular signal-regulated kinase), MMP-3, MMP-1, JNK, p38, and AP-1 are promptly inhibited by EGCG and also TNF-a-induced ERK (extracellular signal-regulated kinase), MMP-3, MMP-1, JNK, p38, and AP-1 and inhibits the expression of oncostatin M stimulated CCL2 chemokines in human osteoblasts and significantly lowers the severity of arthritis induced by collagen (CIA). Therefore, in vitro and in vivo evaluation concluded that EGCG reduces cartilage degradation, synovial hyperplasia, and bone resorption through different targets in the affected joints (Min et al., 2015).
Compounds of Plant Origin as AMP-Activated Protein Kinase Activators
Published in Alexander V. Kutchin, Lyudmila N. Shishkina, Larissa I. Weisfeld, Gennady E. Zaikov, Ilya N. Kurochkin, Alexander N. Goloshchapov, Chemistry and Technology of Plant Substances, 2017
Daria S. Novikova, Gleb S. Ivanov, Alexander V. Garabadzhiu, Viacheslav G. Tribulovich
Epigallocatechin-3-gallate (EGCG, Fig. 9.11) is a natural catechin, found in large quantities in green tea. EGCG is widely used as a food supplement due to its beneficial effects on the human organism. It was found that EGCG activates liver AMPK through the CaMKKp stimulation [70]. A low stability of EGCG under physiological conditions and poor bioavailability resulted in further modification to improve the pharmacological characteristics. More active prodrug with improved bioavailability, which showed anti-tumor properties, was obtained by acetylation of free hydroxyl groups (see Fig. 9.11) [71]. In addition, a focused library of analogs was synthesized based on EGCG. Novel compounds (see Fig.9.11) were identified as more effective activators of AMPK compared with metformin and acetylated EGCG among the analogs by screening [72].
Efficient enzymatic modification of epigallocatechin gallate in ionic liquids
Published in Green Chemistry Letters and Reviews, 2021
Song Zhu, Na Meng, Yue Li, Shang-Wei Chen
Epigallocatechin gallate (EGCG), which is mainly derived from green tea, has exhibited excellent antioxidant, anti-diabetic by activated protein kinase (1, 2), anti-cancer (3), anti-virus (4), and anti-angiogenesis (5) activities, which has been widely confirmed. However, its low fat solubility and instability under neutral or alkaline conditions have limited its use in lipid foods and efficient use in vivo. To overcome this limitation, various types of fat-soluble molecular modifications have been made to EGCG, including methylation, esterification, and acylation of phenolic hydroxyl groups. The bioavailabilities of these EGCG derivatives were significantly improved. In some cases, the derivatives showed stronger biological activity than that of natural EGCG. Kazuaki et al (6) showed that palmitoylated EGCG effectively decreased cancer cell growth and inhibited tumor growth in vivo by inhibiting epidermal growth factor receptor (EGFR) activation. In addition, Lam et al (7) showed that the stability of peracetylated EGCG was better than that of unmodified EGCG, and its inhibition activity of the proteasome and apoptosis of MCF7 breast cancer cells in leukemia cell lines was also stronger. Introduction of an alkyl group at the 4"-O position of AcEGCG significantly increased the biological activity (8).