Preparation, characterization and in vitro antioxidant and cytotoxicity studies of some 2,4-dichloro-N-[di(alkyl/aryl)carbamothioyl]benzamide derivatives

Abstract In the present study, three biologically active, substituted acyl thiourea compounds (1–3) have been synthesized from 2,4-dichlorobenzoyl chloride, potassium thiocyanate and the corresponding secondary amine in dry acetone. As analytical and spectral data of 1 and 3 have already been discussed in the literature, only the compound 2 was characterized by elemental analyses, UV–Visible, FT–IR, 1H & 13C NMR spectroscopic techniques. The molecular structures of 1–3 were determined by single crystal X-ray crystallography which shows twists of up to 70° about the (S=)C–NC(=O) bonds. All the synthesized compounds show good antioxidant property and cytotoxic potential against Ehrlich Ascites Carcinoma (EAC) cancer cell line

Reduction in Ophthalmic Presentations to Australian Emergency Departments During the COVID-19 Period: Are We Seeing the Full Picture?

Purpose: To examine changing patterns of ophthalmic presentations to emergency departments (EDs) during the lockdowns associated with the first wave of the COVID-19 pandemic in Australia and the two months immediately following lockdown relaxation. Patients and Methods: This was a retrospective audit of triage coding and ICD-10-AM coding for all patient presentations to four Australian EDs from March 29 to May 31 in 2019 and 2020 (the COVID-19 lockdown period and the corresponding period in 2019), and from June 1 to July 31 in 2019 and 2020 (the post-lockdown period and the corresponding period in 2019). Number of ophthalmic presentations triaged per day and number of seven common and/or time-sensitive, vision threatening ophthalmic diagnoses were examined. Differences in mean daily presentation numbers were assessed with non-paired Student's t-test with Bonferroni correction. Results: Total ophthalmic presentations per day during COVID-19 lockdowns fell by 16% compared to the corresponding period in 2019 (13.0 ± 4.0 in 2019 vs 10.8 ± 3.3 in 2020, mean ± standard deviation; p=0.01). There was also a significant decrease in presentations of atraumatic retinal detachment, conjunctivitis, and eye pain. In the two months following easing of lockdown restrictions, total ophthalmic presentations per day returned to the same level as that of the corresponding period in 2019 (12.2 ± 4.3 in 2019 vs 12.3 ± 4.1 in 2020, p=0.97). Conclusion: Total ophthalmic presentations and presentations of atraumatic retinal detachment, conjunctivitis and, eye pain to EDs fell during the lockdowns associated with the first wave of COVID-19 in Australia. These may represent delays in patients seeking appropriate medical attention and may have implications on patient morbidity long after the COVID-19 pandemic

Glomerella cingulata endophthalmitis

Purpose: To report a case of an exogenous endophthalmitis caused by the fungal species Glomerella cingulata. Observations: A 71-year-old male presented with an infectious keratitis that evolved into endophthalmitis. Combined cataract extraction and pars plana vitrectomy was performed and the vitreous specimen cultured Glomerella cingulata, a variant of the Colletotrichum gloeosporioides fungal species. Despite early treatment with topical, systemic and intravitreal doses of both voriconazole and amphotericin B, the patient had a poor visual and anatomical outcome. Conclusions and Importance: Glomerella cingulata may rarely cause endophthalmitis with devastating visual outcomes

The major plant-derived cannabinoid 9-tetrahydrocannabinol promotes hypertrophy and macrophage infiltration in adipose tissue

Synthetic cannabinoid receptor agonists activate lipoprotein lipase and the formation of lipid droplets in cultured adipocytes. Here we extend this work by examining whether Δ(9)-tetrahydrocannabinol (THC), a major plant-derived cannabinoid, increases adipocyte size in vivo. Further, possibly as a consequence of hypertrophy, we hypothesize that THC exposure promotes macrophage infiltration into adipose tissue, an inflammatory state observed in obese individuals. Rats repeatedly exposed to THC in vivo had reduced body weight, fat pad weight, and ingested less food over the drug injection period. However, THC promoted adipocyte hypertrophy that was accompanied by a significant increase in cytosolic phosphoenolpyruvate carboxykinase (PEPCK-C) expression, an enzyme important in packaging triglycerides. We also showed that THC induced macrophage infiltration and increased expression of the inflammatory cytokine tumor necrosis factor alpha (TNF-α) in adipose tissue but did not induce apoptosis as measured by TUNEL staining. That THC increased adipocyte cell size in the absence of greater food intake, body weight and fat provides a unique model to explore mechanisms underlying changes in adipocyte size associated with a mild inflammatory state in fat tissue

Cannabidiol potentiates Δ9-tetrahydrocannabinol (THC) behavioural effects and alters THC pharmacokinetics during acute and chronic treatment in adolescent rats

Rationale The interactions between Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) during chronic treatment, and at equivalent doses, are not well characterised in animal models. Objectives The aim of this study is to examine whether the behavioural effects of THC, and blood and brain THC levels are affected by pre-treatment with equivalent CBD doses. Methods Adolescent rats were treated with ascending daily THC doses over 21 days (1 then 3 then 10 mg/kg). Some rats were given equivalent CBD doses 20 min prior to each THC injection to allow examination of possible antagonistic effects of CBD. During dosing, rats were assessed for THC and CBD/THC effects on anxiety-like behaviour, social interaction and place conditioning. At the end of dosing, blood and brain levels of THC, and CB1 and 5- HT1A receptor binding were assessed. Results CBD potentiated an inhibition of body weight gain caused by chronic THC, andmildly augmented the anxiogenic effects, locomotor suppressant effects and decreased social interaction seen with THC. A trend towards place preference was observed in adolescent rats given CBD/THC but not those given THC alone.With both acute and chronic administration, CBD pre-treatment potentiated blood and brain THC levels, and lowered levels of THC metabolites (THC-COOH and 11-OH-THC). CBD co-administration did not alter the THC-induced decreases in CB1 receptor binding and no drug effects on 5-HT1A receptor binding were observed. Conclusions CBD can potentiate the psychoactive and physiological effects of THC in rats, most likely by delaying the metabolism and elimination of THC through an action on the CYP450 enzymes that metabolise both drugs. Keywords THC . Cannabidiol . Cannabis . Adolescent . Anxiety . Reward . Pharmacokinetic