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Nano Delivery of Antiviral Plant Bioactives as Cancer Therapeutics
Published in Devarajan Thangadurai, Saher Islam, Charles Oluwaseun Adetunji, Viral and Antiviral Nanomaterials, 2022
Haripriya Shanmugam, Badma Priya, Manickam Senguttuvan Swetha, Janani Semalaiyappan
Indole derivatives are very common in occurrence (broccoli, cabbage, cauliflower, brussels sprouts, and other cruciferous vegetables), and the indole core is essential for many biosynthetic pathways. Indole-3-carbinol found commonly in Brassicaceae vegetables is an effective antiviral agent against HCV by inhibiting the viral entry and its replication (Zhang et al. 2015). The plant hormone, indole-3-carbinol, also has anti-tumour effects against a wide range of tumours, and it inhibits ligases, thereby combating tumours (Katz et al. 2018).
Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Indole-3-carbinol (Figure 12.27) is found in relatively high amounts in cruciferous vegetables such as brussels sprouts, broccoli, cauliflower, cabbage, and kale. It is produced by the breakdown of the glucosinolate glucobrassicin, which is also found in high concentrations in these cruciferous vegetables. Indole-3-carbinol is reported to have anticarcinogenic, antioxidant, antiatherogenic, and cancer chemoprevention properties.
Chemistry of Essential Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Indole (46) and 2-phenylethanol (47) are both shikimate derivatives. Indole is particularly associated with jasmine. It usually occurs in jasmine absolute at a level of about 3%–5% and makes a very significant odor contribution to it. However, it does occur in many other essential oils as well. 2-Phenylethanol occurs widely in plants and is especially important for rose where it usually accounts for one-third to three-quarters of the oil. The structures of both are shown in Figure 6.10.
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Lamya H. Al-Wahaibi, Anber F. Mohammed, Fatema El-Zahraa S. Abdel Rahman, Mostafa H. Abdelrahman, Xuyuan Gu, Laurent Trembleau, Bahaa G. M. Youssif
On the other hand, the indole skeleton, which can be found in many active ingredients and natural products, is one of the most popular structures with potent antitumor activity14. Many indole derivatives are potent anticancer drugs thus far, and some of them have even been applied in clinics15–17. A large number of indole-based derivatives with TK inhibitory activity were also discovered in the literature review18–21. Li et al. reported compound I to have potent anticancer activity against a panel of four cancer cell lines (IC50 = 1.43–5.48 µM)18. A western blot mechanistic assay of compound I revealed promising EGFR inhibitory activity. Compound II was discovered to be a dual EGFR (T790M)/c-MET inhibitor capable of targeting resistant NSCLC19. Compound II inhibited EGFR (T790M), EGFR (L858R), and c-MET with IC50 values of 0.094, 0.099, and 0.595 µM, respectively (Figure 1).
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Shanbo Yang, Chao Wang, Lingyu Shi, Jing Chang, Yujing Zhang, Jingsen Meng, Wenjing Liu, Jun Zeng, Renshuai Zhang, Yingchun Shao, Dongming Xing
In summary, we replaced the double bond linker between the A and B rings by introducing a pyridine fragment into the CA-4 skeleton. We developed a series of diarylpyridines and evaluated their antiproliferative activity and tubulin polymerisation inhibition. Some synthesised compounds displayed moderate to potent antiproliferative activities with IC50 values at the sub-micromolar level. Among compounds, the existence of indole group was the main factor affecting the biological activity. 10t has broad-spectrum antitumor activity against all tumour cell lines tested with IC50 value of 0.19–0.33 μM. Consistent with its antiproliferative activity, 10t also exhibited potent antitubulin activity, similar to that of CA-4. Further mechanistic studies confirmed that 10t was a microtubule-destabilizing agent that induced the accumulation of cells in the G2/M phase, caused cell mitotic catastrophe and apoptosis. Additionally, the results of docking study showed that 10t may bind to colchicine binding site of tubulin. Our work not only expands the exploration of the linker modification of tubulin inhibitor CA-4 but also provides a set of rigid analogues with moderate to potent antiproliferative activity.
A metabolically engineered bacterium controls autoimmunity and inflammation by remodeling the pro-inflammatory microenvironment
Published in Gut Microbes, 2022
Jugal Kishore Das, Fengguang Guo, Carrie Hunt, Shelby Steinmeyer, Julia A Plocica, Koichi S. Kobayashi, Yufang Ding, Arul Jayaraman, Thomas A Ficht, Robert C. Alaniz, Paul de Figueiredo, Jianxun Song
We have reported that indole, when used at a range of physiologic concentrations, suppresses several inflammatory characteristics in immune and nonimmune cells,21 and also augments Treg differentiation.22 Consistent with our previous reports, we demonstrated that indole suppressed TNF-αproduction in CD11b+ spleen cells after E. coli LPS (eLPS) and heat-inactivated Salmonella Typhimurium [HKST] stimulation (Figure 1a&Figure 1b) and dampened their activation by suppressing Akt and ERK signaling pathways in response to microbial agonists (eLPS and HKST) (Fig. S1a). In addition, indole augmented the differentiation of naive CD4+CD25− T cells into induced Tregs (iTregs) measured by FoxP3 in vitro in a dose dependent manner (Figure 1c&Figure 1d). These findings were consistent with our earlier reports,15 and were comparable to results from studies using the microbiota metabolite butyrate, albeit with distinct dose-dependency.23 Based on these findings, we hypothesized that indole would ameliorate immune-mediated inflammation in autoimmune and pro-inflammatory diseases.