Bio-efficacy of aluminum phosphide and cypermethrin against some physiological and biochemical aspects of Chrysomya megacephala maggots.

Carrion flies play a significant role in forensic entomotoxicology, where they are employed as alternative samples when traditional samples are unavailable. In situations of poisoned death, these toxins disrupt insect development and affect forensic entomology analyses. So, forensic entomotoxicologists must be aware of this impact. The present study aimed to determine the effects of aluminum phosphide (AlP) and cypermethrin (CP) on the biochemical parameters and antioxidant enzymes of the third instar of Chrysomya megacephala maggots. C. megacephala was reared on normal and poisoned rabbit carcasses with aluminum phosphide and cypermethrin. The third larval instar of C. megacephala was studied using by spectrophotometer for detection of total protein, (TP), aspartate aminotransferase (AST), alanine aminotransferase (ALT), total antioxidant capacity (TAC), superoxide dismutase (SOD), glutathione s-transferase (GST), catalase (CAT) and malondialdehyde (MDA). The results indicated to significantly decrease of TP, TAC, SOD, GST and CAT and increase of AST, ALT and MDA in the maggots reared on the poisoned carcasses with AlP or CP compared with control group. In conclusion, the tested insecticides brought about a decrease antioxidant enzyme activity and increase of MDA could be involved in free radicals in C. megacephala larvae leading to oxidative stress by these insecticidal components.

Design, synthesis, molecular docking, in silico ADMET profile and anticancer evaluations of sulfonamide endowed with hydrazone-coupled derivatives as VEGFR-2 inhibitors.

A new series of sulfonamide endowed with hydrazone coupled to dimethyl and/or diethyl malonates were prepared. Various sulfa drugs were diazotized and followed by coupling with active methylene of dimethyl and/or diethyl malonate to afford the new intermediates hydrazones 3a-c and 4a-c. The reactivity of hydrazone derivatives towards hydrazines was investigated. Thus, a novel series of 3,5-dioxopyrazolidine7a-cwere obtained by treatment with hydrazine hydrate. When hydrazones were allowed to react with phenyl hydrazine, the alkyl 2-((4-(N-(substituted)sulfamoyl)phenyl)diazenyl)-3-oxo-3-(2-phenylhydrazinyl)propanoateswere obtained 8a-c and/or 10a-c. Their anticancer activities were evaluated against HepG2, HCT-116 and MCF-7. HepG2 was the most sensitive one. In particular, compounds 7c, 7b and 10c were found to be the most potent derivatives with IC50 = 6.43 ± 0.5, 9.66 ± 0.8, 10.57 ± 0.9 µM, 8.65 ± 0.7, 7.49 ± 0.6, 14.29 ± 1.3 µM and 8.97 ± 0.7, 10.13 ± 0.9, 13.82 ± 1.1 µM respectively. Sorafenib and doxorubicin were used as reference drugs. The most potent derivatives 7a, 7b, 7c, 8c and 10c were tested for their cytotoxicity against normal VERO cell lines. Compounds 7a, 7b, 7c, 8c and 10c are respectively, 2.41, 4.85, 4.08, 3.23 and 5.89 fold times more toxic in HCT116 than in VERO normal cells. Moreover, the most active anti-proliferative derivatives 7a, 7b, 7c, 8c and 10c were subjected to further biological study to evaluate their inhibitory potentials against VEGFR-2. The tested compounds displayed high to good inhibitory activity with IC50 values ranging from 0.14 ± 0.02 to 0.23 ± 0.03 µM. Among them, compounds 7c, 7b and 10c were found to be the most potent derivative that inhibited VEGFR-2 at IC50 values of 0.14 ± 0.02, 0.15 ± 0.02 and 0.15 ± 0.02 µM respectively. sorafenib was used as reference drug. Furthermore, ADMET profile was evaluated for the four most active compounds in comparison to doxorubicin as a reference drug. The data obtained from docking studies were highly correlated with that obtained from the biological screening.

Antiviral and virucidal activities of Lucilia cuprina maggots' excretion/secretion (Diptera: Calliphoridae): first work.

Maggots of Lucilia sericata and L. cuprina are a backbone of the maggot debridement therapy. Further, the excretion/secretion (E/S) of these maggots has antibacterial and antifungal activities, nevertheless the antiviral activity of E/S for these maggots still out the focus. This study aimed to evaluate the E/S of L. cuprina maggots against the Rift Valley Fever (RVF) and Coxsackie B4 (CB4) viruses for first time. After collection of the E/S, its cytotoxicity on Vero cells was evaluated and the safe concentration was determined which used to investigate the antiviral and virucidal effect of E/S on the selected viruses. The E/S decreased the titers of the tested viruses compared with that of untreated viruses. The outcome data refer to that the E/S of L. cuprina consider as a promising antiviral and virucidal agent.