Nael Abutaha

Synthesis, Characterization, and Anti-Cancer Activity of Some New N′-(2-Oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazones Derivatives

Eight novel N′-(2-oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazone derivatives 4a–h were synthesized and fully characterized by IR, NMR (1H-NMR and 13C-NMR), elemental analysis, and X-ray crystallography. The cyto-toxicity and in vitro anti-cancer evaluation of the prepared compounds have been assessed against two different human tumour cell lines including human liver (HepG2) and leukaemia (Jurkat), as well as in normal cell lines derived from human embryonic kidney (HEK293) using MTT assay. The compounds 3e, 3f, 4a, 4c, and 4e revealed promising anti-cancer activities in tested human tumour cells lines (IC50 values between 3 and 7 μM) as compared to the known anti-cancer drug 5-Fluorouracil (IC50 32–50 μM). Among the tested compounds, 4a showed specificity against leukaemia (Jurkat) cells, with an IC50 value of 3.14 μM, but this compound was inactive in liver cancer and normal cell lines.

Biological activity of Xanthium strumarium seed extracts on different cancer cell lines and Aedes caspius, Culex pipiens (Diptera: Culicidae)

Effects of methanol extracts of Xanthium strumarium on different cancer cell lines and on the mortality rates of Aedes caspius, Culex pipiens (Diptera: Culicidae) were investigated. Among the cell lines tested, the Jurkat cell line was the most sensitive to the methanol extract and ethyl acetate fraction, with reported LC50 values of 50.18 and 48.73 μg/ml respectively. Conversely, methanol extracts were not that toxic to the A549 cell line though the toxicity increased on further purification. The percentage of growth inhibition was dose dependent for the methanol extract and ethyl acetate fraction. The ethyl acetate fraction showed higher toxicity to all cell lines tested when compared to the methanol extract. The results showed that methanol extracts of plant seeds caused 100% mortality of mosquito larvae at a concentration of 1000 μg/ml after 24 h of treatment. The LC50 and LC90 values of X. strumarium were found to be 531.07 and 905.95 μg/ml against Ae. caspius and 502.32 and 867.63 μg/ml against Cx. Pipiens, respectively. From the investigations, it was concluded that the crude extract of X. strumarium showed a weak potential for controlling the larval instars of Ae. caspius and Cx. pipiens. However, on further purification the extract lost the larvicidal activity. The ethyl acetate fraction showed higher toxicity to all cell lines tested when compared to the methanol extract. The ethyl acetate fraction investigated in this study appears to have a weak larvicidal activity but a promising cytotoxic activity. Future studies will include purification and investigation in further detail of the action of X. strumarium on Cancer Cell Lines and mosquitoes.

Insecticidal Effect of Solenostemma argel Extracts Against Culex pipiens

Of the various plant extracts from 10 plant species tested against larvae of Culex pipiens in the laboratory, only extracts from Solenostemma argel exhibited larvicidal activity. A chloroform leaf extract of S. argel exhibited relatively high activity with a lethal concentration causing 50% mortality (LC50) of 15.89 ppm, while chloroform and ethyl acetate extracts of S. argel fruits were 19.70 and 19.52 ppm, respectively. The chloroform fruit extract at 10 ppm reduced the hatchability of Cx. pipiens eggs by 20%, whereas the chloroform leaf extract was found to be less effective (5% reduction). At 10 ppm, adult emergence was reduced by 84% and 75% for chloroform and ethyl acetate extracts of fruits, respectively. Metamorphosis of larvae exposed to chloroform fruit extract (10 ppm) was extended to 15 days, as compared to 10 days for control larvae. It took 12 days at 1 ppm, and 15 days at 6 and 10 ppm for chloroform fruit extract-treated embryos to develop into adult mosquito while it took 10 days in the control treatment. However, 100% toxicity was observed in the embryos of zebrafish, Danio rerio, treated with the ethyl acetate fruit extracts (LC50 of 20 ppm and LC100 of 40 ppm) and chloroform leaf extract (LC50 of 30 ppm and LC100 of 60 ppm). These findings emphasize the need to further isolate the bioactive molecules in S. argel crude extracts that may still be mosquitocidal but produce no, or minimal, adverse effects on nontarget organisms such as zebrafish.

Larvicidal potency of selected xerophytic plant extracts on Culex pipiens (Diptera: Culicidae): Effect of Plant Extracts on Culex pipiens

Chemical insecticides released into the environment may have adverse biological effects. Therefore, there is a need for ecofriendly insecticides for mosquito control. Xerophytic plant extracts that may provide more ecofriendly active component were evaluated against Culex pipiens 4th instars. Plant extracts prepared using different solvents with a Soxhlet apparatus and different concentrations were tested against Culex pipiens larvae. The effects were observed at 24 h and 72 h intervals and LD50 and LD90 values determined. Chloroform (CHCl3) and ethyl acetate (EtOAc) extracts of Althaea ludwigii were the most effective against Cx. pipiens 4th instars, but were highly dependent on extract concentrations and exposure time. Results suggest that A. ludwigii extracts contain bioactive compounds, such as phenols and saponins, that may provide effective Cx. pipiens larval control. However, the extract was found to be toxic to zebrafish larvae, and may be toxic to other aquatic fauna. Further studies to determine the active components and toxicity to other fauna are needed.

Efficacy of entomopathogenic fungi isolated from the nest of the samsum ant, Pachycondyla sennaarensis against larvae of the mosquitoes Aedes caspius and Culex pipiens

The use of entomopathogenic fungi is a promising alternative to chemical control against mosquitoes. In February 2013, two fungi were isolated from the Samsum ant, Pachycondyla sennaarensis, Mayr, (Hymenoptera: Formicidae) collected in Riyadh, KSA. One of these fungi, identified as Fusarium solani was highly pathogenic against larvae of the mosquito, Aedes caspius (Diptera: Culicidae). F. solani killed 100% of Ae. caspius within 5 days of exposure to the concentration of 5 × 107 cfu/ml. Also, results indicated that F. solani was more virulent to the mosquito larvae than F. chlamydosporum at the concentration of 8 × 107 cfu/ml. The histopathological examination indicated that spores of F. solani are invasive to the wall of Ae. caspius larvae. Both F. solani and F. chlamydosporum were not affected against Ae. caspius and Culex pipiens. These results suggested that F. solani could be an effective tool to manage Ae. caspius proliferation and hence diseases transmission.