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Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
Pyrrole derivatives also showed antineoplastic activity. Many pyrrole derivatives reported as anti-microbial and anti-cancer drugs (Biava et al., 2003). A pyrrole derivative derived from Staphylococcus, pyrrole (1, 2a) pyrazine 1,4-dioneheahydro-3-(2-methyl propyl), is an antagonist to some bacteria that affect humans (Khazir et al., 2014). These derivatives also showed antitumor efficacy. These compounds also promote apoptosis. Induction of apoptosis is a safer and less harmful method as it produces less toxic and debilitating side effects. This certain strain (pyrrole derivative) could have some serious implications (Lalitha et al., 2016). These implications could increase the life expectancy by reducing the harmful side effects, produced due to chemotherapy and radiation. These pyrrole-based new drugs could eventually replace harsh chemotherapy and invasive radiation therapy as a go-to treatment for cancer (Regina et al., 2014).
The Widening Panorama of Natural Products Chemistry in Brazil
Published in Luzia Valentina Modolo, Mary Ann Foglio, Brazilian Medicinal Plants, 2019
Maria Fátima das Graças Fernandes da Silva, João Batista Fernandes, Moacir Rossi Forim, Michelli Massaroli da Silva, Jéssica Cristina Amaral
Silva-Junior et al. (2018), aiming to understand the relationship between the bacterium Serratia marcescens 3B2 and cutter ants of the genus Atta sexdens rubropilosa, carried out the chemical study of the bacteria and isolated several pyrazines (25–30, Figure 3.7). Some of these compounds were identified as alarm and trail pheromones of leafcutter ants. This work will help in the elaboration of future studies that aim at the control of these ants.
How Differences in Chemical Constituents in Ginseng Affect Medicinal Effects
Published in Joseph P. Hou, The Healing Power of Ginseng, 2019
Other principles isolated from the root include acetylenic compounds panaxynol, panaxydol, panaxytriol, and heptadeca-1-ene-4,6-diyn-3,9-diol.16–20 From the volatile fraction of the root, a series of sesquiterpenes such as eremophilene, β-gurjunene, trans- and cis-caryophyllene, ε-muurolene, γ-patchoulene, β-eudesmol, β-farnesene, β-bisabolene, aromadendrene, alloaromadendrene, β-guaiene, γ-elemene, mayurone, pentadecane, and 2,5-dimethyltridecane were also isolated.21 Some pyrazine derivatives including 3-sec-butyl-2-methoxy-5-methylpyrazine and 3-isopropyl-2-methoxy-5-methylpyrazine were identified in the basic fraction of the volatile extract of the root (Table 14.1).22
Boswellic acids: privileged structures to develop lead compounds for anticancer drug discovery
Published in Expert Opinion on Drug Discovery, 2021
Hidayat Hussain, Iftikhar Ali, Daijie Wang, Faruck L. Hakkim, Bernhard Westermann, Luay Rashan, Ishtiaq Ahmed, Ivan R. Green
In another study, Huang et al. [66] prepared a library of BA derivatives and screened them for their cytotoxic effects toward PC-3 cells. Among the tested compounds, KBA derivatives 18–20 (Figure 3) possess good effects toward PC-3 with IC50: values ranging from 9.4 to 7.8 μM. Futhermore, compound 21 was the most potent with (IC50: 1.82 μM) followed by 22 (IC50: 3.29 μM). In this study, the parent AKBA cytotoxic effects were not promising and had IC50: values of 13.9 μM [66]. Quite recently we prepared AKBA derivative 23 and this compound displayed cytotoxic effects toward LNCaP with IC50: 3.29 μM [67]. In another report, our group also prepared the pyrazine analog 24 and its semithiocarbazone analog 25 both of which possess cytotoxic effects for the two cancer cell lines, e.g. A375 (EC50 = 2.1 µM) and A2780 (EC50 = 9.3 µM) [68].
Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents
Published in Drug Delivery, 2020
Fengyi Zhao, Xu Sun, Wen Lu, Li Xu, Jiuzhou Shi, Shilong Yang, Mengyi Zhou, Fan Su, Feng Lin, Fuliang Cao
Recently, nitrogen heterocycles have also been reported to exhibit therapeutics anticancer (Azuine et al., 2004; Lei et al., 2019a,c) and anti-microbial (Nomiya et al., 2000; Mathew et al., 2006) activities. Among them, the pyrazine heterocycles have widespread application in food science, materials, and medicinal chemistry (Mondal et al., 2010; Saito et al., 2010; Badrinarayanan & Sperry, 2011; Zitko et al., 2011). For example, pyrazinamide, a pyrazine derivative, is an antimicrobial agent that is most commonly used for treatment of active tuberculosis during the initial phase of therapy in combination with other agents. Quinoxaline compounds have been reported to possess a wide range of interesting biological properties such as anticancer, antiviral, antimicrobial, antifungal, antitubercular, anti-inflammatory, and anti-angiogenesis agents (Seitz et al., 2002; Smits et al., 2008; Vicente et al., 2009; Lee et al., 2010; Sridevi et al., 2010; Ingle et al., 2013; Aissi et al., 2014; Soozani et al., 2018), containing pyrazine motif. Ahmed et al. (2018) have synthesized several compounds and evaluated anticancer effects against three cancer lines (HCT-116, MCF-7, and HepG2), and the results revealed that pyrazine derivatives were the most active compounds with IC50 value of 1.89 and 2.05 Μm. Another pyrazine derivative, pyrazin-2(1H)-one, has attracted considerable attention due to its biological activities, such as anti-viral, antibacterial, anti-inflammatory, and anticancer (colon cancer therapies) activities (Lindsley et al., 2005).
Determining bacterial and host contributions to the human salivary metabolome
Published in Journal of Oral Microbiology, 2019
Alexander Gardner, Harold G. Parkes, Po-Wah So, Guy H. Carpenter
WMS and stimulated PS were prepared unmodified in a 5 mm OD NMR tube (500 µl sample) with a coaxial 3 mm OD NMR tube containing 300 µl 1 mM trimethylsilyl-[2,2,3,3,-2H4]-propionate (TSP) standard with 50% deuterium oxide. Due to plasma collection by finger prick and the naturally low flow rate of unstimulated PS and plasma, the lower sample volumes of these fluids required different preparation. Unstimulated PS was analysed by putting the sample in the 3 mm OD NMR tube and the standard in the 5 mm OD tube. In most cases, plasma samples were limited to 100 µl, therefore samples were prepared in a 1:2 plasma: buffer ratio as described by Beckonert et al. [30] and analysed in a 3 mm NMR tube. The same protocol recommends formate as an internal standard as opposed to TSP, however, endogenous formate was observed in preliminary plasma samples. Pyrazine was therefore chosen as an internal standard at a concentration of 0.33 mM [31,32]. The pH was adjusted to 7.4. A spectrum of the tartaric acid stimulus was also acquired to ensure there was no contamination of stimulated PS.