Clinical pharmacology of opioids: basic pharmacology
Nigel Sykes, Michael I Bennett, Chun-Su Yuan in Clinical Pain Management, 2008
Compounds in this class bind to the receptor with great affinity; however, the stimulated response is not as potent as that with a pure agonist. In fact, if administered with a pure agonist, such a chemical acts as a competitive antagonist that blocks the effect of a pure agonist. Semi-synthetic alkaloids: – phenanthrene derivatives: codeine, dihydrocodeine.Synthetic opioids: – diphenylheptanes: dextropropoxyphene;– other: tramadol (also exerts analgesic effect by inhibition of monoamine reuptake).46
A Comparative Study of Organic Pollutants in Seawater, Sediments, and Oyster Tissues at Hab River Delta, Balochistan Coast, Pakistan
Se-Kwon Kim in Marine Biochemistry, 2023
In both oyster samples, several PAHs were identified. The PAHS are present in petroleum fractions, and they are formed during thermal cracking taking place in some processes of crude oil processing (Gilgenast et al., 2011; Boczkaj et al., 2014; Makoś et al., 2018a, 2018b). This indicates a health risk for humans in this region because PAHs are carcinogenic. However, Gardner et al. (1991) has well documented the concentrations of organic contaminates in eastern oyster, Crassostrea virginica, and in sediments with reference to evidence scale as carcinogens. He gave a scale of carcinogens to different contaminants. According to his scale, Chrysene has limited evidence as carcinogens. Phenanthrene has inadequate evidence while anthracene and fluoranthene have no evidence of being carcinogenic. The only cancer promoter we detected in our results is pyrene. Bender et al. (1988) examined the distribution of PAHs in eastern oysters from the Elizbeth River, Virginia, and conducted laboratory studies compared the uptake and depuration of PAHs by eastern oysters and hard clam, Mercenaria mercenaria, with exposure to contaminated sediments from the Elizabeth River. Animals were exposed to contaminated sediments for 28 days, followed by a 28-day depuration phase. Oysters accumulated three to four times more total PAH than clams with similar uptake rates. Bioconcentration factors for oysters ranged from 1600 for phenanthrene to 36,000 for methyl-pyrene (Capuzzo, 1996).
In Vitro Skin Metabolism
Rhoda G. M. Wang, James B. Knaak, Howard I. Maibach in Health Risk Assessment, 2017
Recently, the percutaneous absorption and metabolism of phenanthrene have been studied in the hairless guinea pig.38 Good agreement was obtained between absorption values from in vivo studies (80% applied dose absorbed) and values from, viable skin in flow-through diffusion cells (89.7%). Phenanthrene was metabolized in vitro to phenanthrene 9,10-di-hydrodiol, 3,4-dihydrodiol, and 1,2-dihydrodiol, and to traces of hydroxyphenanthrenes. No Bay-region 3,4-dihydrodiol epoxide or its rearranged product was found, which is consistent with the negative cancer bioassay data for phenanthrene reported in the literature. Based on the total radioactivity in vitro, the absorbed material contained 92% parent compound and 7% dihydrodiol metabolites.
Levels of polyaromatic hydrocarbons (PAHs) in sediment samples from selected Jordanian dams
Published in Toxin Reviews, 2021
Sharif Arar, Mahmoud Alawi, Ali Alnawaiseh, Mohanad Masad
Comparing the results of the studied samples from the five Jordanian dams for the 13 PAH compounds as shown in Table 4, we found that acenaphthylene was found in the concentration range from 0.0 ng/g (Wadi ElArab, Karamah, and Mujib) to 12.3 ng/g (King Tala dam). Fluorene was found in the concentration range from 10.4 ng/g (King Talal dam) to 22.0 (Wadi ElArab). Phenanthrene was found in the concentration range from 0.0 ng/g (Mujib and Tannur) to 2.8 ng/g (King Talal dam). Anthracene was found in the concentration range from 0.0 ng/g (Tannur) to 13.6 ng/g (Mujib). Pyrene was found in the concentration range from 0.0 ng/g (Tannur) to 7.2 ng/g (Mujib). Benzo(a)anthracene was found in the concentration range from 0.0 ng/g (Mujib, Tannur, and Karamah) to 2.0 ng/g (Wadi ElArab). Chrysene was found in the concentration range from 0.0 ng/g (Mujib, Tannur, and Karamah) to 5.0 ng/g (King Talal dam). Benzo(b)fluoranthene, dibenzo-(a,h)anthracene, benzo(g,h,i)perylene, and indeno-(1,2,3cd)pyrene were found only in king Talal dam with the concentration 25.3 ng/g, 1.0 ng/g, 0.5 ng/g, and 2.0, respectively. Benzo(k)fluoranthene and benzo(a)pyrene were not found in all studied dams.
Thais savignyi tissue extract: bioactivity, chemical composition, and molecular docking
Published in Pharmaceutical Biology, 2022
Mohamed R. Habib, Ahmed A. Hamed, Rasha E. M. Ali, Khaled M. Zayed, Rasha M. Gad El-Karim, Rehab Sabour, Hanaa M. Abu El-Einin, Mosad A. Ghareeb
Furthermore, pyridazine derivatives have been reported to have diverse biological activities, including antiviral, anticancer, and antimicrobial properties (Butnariu and Mangalagiu 2009). Quinoline derivatives have diverse biological activities and constitute an important class of compounds for new drug development (Orhan Puskullu et al. 2013). Various synthetic quinoline derivatives were screened for their biological activities. Some derivatives showed antibacterial (Narender et al. 2006; Reddy et al. 2009; Matada et al. 2021), antifungal (Musiol et al. 2006), and cytotoxic activity (Costa et al. 2020). Phenanthrenes are a relatively small group of natural products derived primarily from plants. Almost all of the phenanthrene compounds isolated from plants demonstrated a variety of biological activities, including antioxidants (Behery et al. 2013; Woo et al. 2014), antimicrobial (Guo et al. 2016; Tóth et al. 2016), and cytotoxicity (Ma et al. 2016). Other chemical classes represented in Ts-EtOAc extract, such as ketones, monoterpenes, fatty acid esters, stilbenoids, and sesquiterpenoids, have been shown to have beneficial biological activities (Mallesha et al. 2012; Abdel-Aziz et al. 2018; Akinwumi et al. 2018; Mothana et al. 2018; Ghareeb et al. 2019; Elkhouly et al. 2020). Hamed et al. 2020;
In vivo assessment of respiratory burst inhibition by xenobiotic exposure using larval zebrafish
Published in Journal of Immunotoxicology, 2020
Drake W. Phelps, Ashley A. Fletcher, Ivan Rodriguez-Nunez, Michele R. Balik-Meisner, Debra A. Tokarz, David M. Reif, Dori R. Germolec, Jeffrey A. Yoder
As the current work in the zebrafish supports the general conclusion that phenanthrene could suppresses the immune system of freshwater fish, future studies should work to better establish the immunomodulatory potential of phenanthrene in mammalian models. Given that both phenanthrene and BaP are polycyclic aromatic hydrocarbons (PAH) identified by the USEPA as “priority pollutants” (Andersson and Achten 2015), and given their environmental ubiquity, future work should more fully characterize the immunotoxicity of various PAH to understand their common/disparate mechanisms of action(s) in order to reduce exposure risks and prevent adverse outcomes.
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