Synthesis and Antidepressant Evaluation of Five Novel Heterocyclic Tryptophan‐Hybrid Derivatives

This study aimed at evaluating the reactivity of L ‐Tryptophan (TRP) 1 towards various chemical reagents to produce new bi‐ and tri‐heterocyclic systems providing basic pharmacological activities. Indol‐3‐yl hydroxyoxazol‐2‐yl acetonitrile derivatives 5 and 6 , indol‐3‐yl‐hydroxyoxazol‐2‐yl‐1,2,4‐triazine derivatives 8 and 9, indol‐3‐yl‐hydroxyoxazol‐2‐yl‐aminopyrazole derivatives 11a, b, and indol‐3‐yl‐hydroxyoxazol‐2‐yl‐aminoisoxazole derivative 12 were synthesized via straightforward and efficient methods. The structures were characterized by spectral data (IR, ¹H‐NMR, ¹³C‐NMR, and MS) and the purity was ascertained by microanalysis. Also, this work was extended to study the potential role of the novel synthesized TRP derivatives 5 , 6 , 9 , 11a , and 12 as antidepressant and sedative agents in comparison with TRP. All compounds showed significant antidepressant activity in the forced‐swimming test at two doses (50 or 100 mg/kg). Also, all tested compounds (at 50 or 100 mg/kg) produced a significant decrease in locomotor activity of mice during a 30 min observation period. The most potent antidepressant and sedative effect was produced by the tri‐heterocyclic compounds 9 and 12 , followed by 11a and TRP.     

Analysis of the essential oil from the aerial parts of Psoralea pubescence (Miq.) Standl and its antibacterial activity

The essential oil from aerial parts of Psoralea pubescence (Miq.) Standl (Leguminoseae) was analyzed by gas chromatography (GC) and GC/mass spectroscopy systems. The major components identified were psoralen (24.8%), bakuchiol (21.3%), β-caryophyllene (8.5%), germacrene D (6.8%), and α-humulene (4.6%). The major volatiles released by β-glucosidase treatment of the aqueous plant residue were δ-pinene (28.3%), germacrene D (13.6%), and tricyclene (10.2%). The oil showed significant antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa, while the β-glucosidase-liberated fraction was inactive.     

Multiple myeloma: a descriptive study of 217 Egyptian patients

Multiple myeloma is a neoplasm of plasma cells that results in the overproduction of light and heavy chain monoclonal immunoglobulins. The incidence rate increases with age, particularly after 40 years, and is higher in men. To determine the clinical and laboratory characteristics and survival of diagnosed Egyptian multiple myeloma patients admitted to the Haemato-Oncology Department between 2000 and 2010. Records of all patients in whom multiple myeloma was diagnosed at the Kasr Al Aini Hospital between 2000 and 2010 were included in this retrospective study. The mean age of patients was 58.5 years (range, 27–80 years). Fifty-nine percent were males. The majority of patients (73 %) had an immunoglobulin G monoclonal band and 70 % were Kappa chain-positive. Mean overall survival was 37.5 months (range, 1–84 months). Survival analysis was statistically insignificant with respect to age, sex, International Staging System and type of treatment (p?>?0.05). Our records were largely comparable to those reported in Chinese studies but different from those noted in Western and Arabic countries.     

The impact of COVID-19 pandemic on rheumatology practice: a cross-sectional multinational study

Clinical Rheumatology - To evaluate the impact of the coronavirus disease 2019 (COVID-19) pandemic on rheumatology practice. A cross-sectional web survey was designed by the members of the Arab...     

Allele and genotype frequencies of polymorphic DCP1, CETP, ADRB2, and HTR2A in the Egyptian population

OBJECTIVE: The goal of this study was to determine the frequencies of important allelic variants of two drug targets, dipeptidyl carboxypeptidase ( DCP1) and cholesteryl ester transfer protein ( CETP), and two other drug receptors, beta-2 adrenergic receptor ( ADRB2) and 5-hydroxy tryptamine 2A receptor ( HTR2A), in the Egyptian population and compare them with the frequencies in other ethnic populations. METHODS: A sensitive real-time polymerase chain reaction assay was developed and successfully applied for genotyping of the consensus (wild-type) alleles plus five variants of four genes: DCP1 [the insertion allele ( I) versus the deletion allele ( D)], CETP*TaqI ( B1 versus B2), ADRB2*R16G, ADRB2*Q27E, and HTR2A*102T>C. This study was carried out in 242 unrelated Egyptian subjects and is the first to describe these allelic variants in the Egyptian population. RESULTS: The frequencies of the tested alleles were found as: DCP1 ( I: D, 0.32:0.68), CETPTaqI ( B1: B2, 0.65:0.35), ADRB2*R16G ( Arg16: Gly16, 0.57:0.43), ADRB2*Q27E ( Gln27: Glu27, 0.76:0.24), and HTR2A*102T>C ( T102: C102, 0.53:0.47). The common Arabian ancestors of the Egyptians, Spanish, Saudi, and Emirate had created a common pattern of distribution of some allelic variants ( DCP1 and CETP). However, in the genotyping of ADRB2, the frequency of the polymorphism at codon 16 was found to be similar to the Chinese population, whereas that at codon 27 was similar to African-Americans with significant differences than other Caucasian populations. The frequency of the HTR2A*102T>C variant appeared to be similar to many Caucasian populations and African-Americans. CONCLUSIONS: We have explored the frequencies of important allelic variants DCP1, CETP, ADRB2, and HTR2A among the Egyptian population focusing on the ethnic diversity in the distribution of the tested mutant alleles. Our results may help in better understanding the observed ethnic variation in angiotensin-converting enzyme inhibition and atherosclerosis therapy. It also may contribute to better characterization of interethnic differences in isoprenaline and clozapine response, which will have implications for the cost effective and rational prescribing of these drugs.