Aedes aegypti is the main vector for dengue, chikungunya, yellow fever, Zika, and other arboviruses of public health importance. The presence of Ae. aegypti has never been systematically assessed in Zanzibar, including its preferred larval habitats. In 2016 we conducted a cross-sectional entomological survey to describe the preferred larval habitats of Ae. aegypti in Zanzibar City, the main urban area of the Zanzibar archipelago. The surveys for container habitats were conducted for a 17-wk period beginning in January 2016. Immature stages (larvae and pupae) were collected, reared to adulthood, and identified to species. The positive and potential habitats were categorized on the basis of physical, biological, and chemical parameters. A total of 200 samples were collected, of which 124 (62.0%) were positive for immature stages of mosquitoes and 114 (92%) for Ae. aegypti larvae and pupae. Presence of vegetation (odds ratio [OR] ¼ 2.11, 95% confidence interval [CI] ¼ 1.19-3.74), organic matter (OR ¼ 2.37, 95% CI ¼ 1.21-4.60), inorganic matter (OR ¼ 1.78, 95% CI ¼ 1.01-3.13), and sun exposure (OR ¼ 2.34, 95% CI ¼ 1.24-4.36) were all significantly associated with the presence of immature stages of Ae. aegypti, suggesting that these conditions promote colonization of containers. Plastic containers supported 64% of the immature stages and produced approximately 50% of the pupae. Although immature counts were the highest in discarded artifacts, higher pupal counts were found in domestic water storage containers. Our observations suggest that effective control of Ae. aegypti in Zanzibar City must include improved solid waste management (collection and proper disposal of potential container habitats) and reliable supply of domestic water to minimize water-storing practices that provide larval habitats for Ae. aegypti.
Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites that are reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity. In addition, heterocyclic compounds having nitrogen such as isoquinolines are of considerable interest as they constitute the core structural element of many alkaloids that have enormous pharmacological activities. Objective: The objective of this study is the synthesis and biological activity of novel chalcones incorporating thiadiazolyl isoquinoline as potential anticancer candidates. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Methods: An efficient one pot synthesis of novel chalcones incorporating thiadiazolyl isoquinoline has been developed. The cytotoxic activity of the novel synthesized compounds was performed against four different kinds of cancer cell lines. Results: Among all the tested derivatives, chalcone 3 has the best cytotoxic profile against A549, MCF7, and HeLa cell lines, with IC50s (66.1, 51.3, and 85.1μM, respectively). Molecular docking studies for chalcone 3 revealed that CDK2, and EGFRTK domains have strong binding affinities toward the novel chalcone 3, while tubulin-colchicine-ustiloxin, and VEGFRTK domains illustrated moderate mode of binding. Conclusion: We have developed an efficient method for the synthesis of novel chalcones incorporating thiadiazolyl isoquinoline. All compounds showed better cytotoxicity results against four kinds of cancer cell lines (A549, MCF7, HCT116, and HELA cells). The results depicted that chalcone 3 has a high and promising cytotoxic effect against HELA cell line and the mechanism of cytotoxicity was widely studied through different theoretical and experimental tools. Thus, the newly synthesized derivative 3 can be utilized as a novel chemotherapeutic compound for cervical carcinoma.
Background In Zanzibar, little is known about the arboviral disease vector Aedes aegypti in terms of abundance, spatio-temporal distribution of its larval habitats or factors associated with its proliferation. Effective control of the vector requires knowledge on ecology and habitat characteristics and is currently the only available option for reducing the risk of arboviral epidemics in the island nation of Zanzibar. Methodology We conducted entomological surveys in households and surrounding compounds from February to May 2018 in the urban (Mwembemakumbi and Chumbuni) and rural (Chuini and Kama) Shehias (lowest government administrative unit) situated in the Urban-West region of Unguja island, Zanzibar. Larvae and pupae were collected, transported to the insectary, reared to adult, and identified to species level. Characteristics and types of water containers were also recorded on site. Generalized linear mixed models with binomial and negative binomial distributions were applied to determine factors associated with presence of Ae. aegypti immatures (i.e. both larvae and pupae) or pupae, alone and significant predictors of the abundance of immature Ae. aegypti or pupae, respectively. Results The survey provided evidence of widespread presence and abundance of Ae. aegypti mosquitoes in both urban and rural settings of Unguja Island. Interestingly, rural setting had higher numbers of infested containers, all immatures, and pupae than urban setting. Likewise, higher House and Breteau indices were recorded in rural compared to the urban setting. There was no statistically significant difference in Stegomyia indices between seasons across settings. Plastics, metal containers and car tires were identified as the most productive habitats which collectively produced over 90% of all Ae. aegypti pupae. Water storage, sun exposure, vegetation, and organic matter were significant predictors of the abundance of immature Ae. aegypti. Conclusions Widespread presence and abundance of Ae. aegypti were found in rural and urban areas of Unguja, the main island of Zanzibar. Information on productive habitats and predictors of colonization of water containers are important for the development of a routine Aedes surveillance system and targeted control interventions in Zanzibar and similar settings.
In the wood destroying fungus Schizophyllum commune, a well known subject for genetic studies, fruit bodies are produced not only in the course of the sexual cycle but also asexually. Sexual fruiting requires the establishment of a dikaryon which is under the control of the incompatibility factors A and B. Asexual fruiting, however, starts directly from a monokaryon. The initiation of monokaryotic fruiting requires the presence of a single gene leading to the differentiation of fruit body initials. The action of at least two more genes is required for the further morphogenetic steps resulting eventually in the production of fruit bodies which differ in shape from dikaryotic fruit bodies. As a consequence of a mitosis their basidia produce two spores only. The three genes responsible for monokaryotic fruiting are pleiotropic and determine synergistically the timing of dikaryotic fruiting within a range between 6 to 20 d or longer. A fourth gene was found which codes epistatically for the formation of dome-like masses of stromatic tissue, thus directing morphogenesis into a side track.
Understanding the dynamics of larval habitat utilization by mosquito communities is crucial for the design of efficient environmental control strategies. The authors investigated the structure of mosquito communities found at hotel compounds in Zanzibar, networks of mosquito interactions with larval habitats and robustness of mosquito communities to elimination of larval habitats. A total of 23 698 mosquitoes comprising 26 species in six genera were found. Aedes aegypti (n = 16 207), Aedes bromeliae/Aedes lillie (n = 1340), Culex quinquefasciatus (n = 1300) and Eretmapodites quinquevitattus (n = 659) were the most dominant species. Ecological network analyses revealed the presence of dominant, larval habitat generalist species (e.g., A. aegypti), exploiting virtually all types of water holding containers and few larval habitat specialist species (e.g., Aedes natalensis, Orthopodomyia spp). Simulations of mosquito community robustness to systematic elimination of larval habitats indicate that mosquito populations are highly sensitive to elimination of larval habitats sustaining higher mosquito species diversity. This study provides insights on potential foci of future mosquito-borne arboviral disease outbreaks in Zanzibar and underscores the need for detailed knowledge on the ecological function of larval habitats for effective mosquito control by larval sources management.
Twelve novel chalcone derivatives were prepared using the Claisen–Schmidt condensation reaction. The reaction of 4‐acetyl‐5‐furan/thiophene‐pyrazole derivatives 5 with the corresponding aldehydes 6 afforded the targeted chalcone derivatives 7a–l in good yields. The newly synthesized chalcones were fully characterized by spectrometric and elemental analyses. The in vitro anticancer activities of the novel compounds 7a–l were evaluated against four human cancer cell lines: HepG2 (human hepatocellular carcinoma), MCF7 (human Caucasian breast adenocarcinoma), A549 (lung carcinoma), and BJ1 (normal skin fibroblasts). Compound 7g emerged as the most promising compound, with IC50 = 27.7 µg/ml against A549 cells compared to the reference drug doxorubicin (IC50 = 28.3 µg/ml), and IC50 = 26.6 µg/ml against HepG2 cells compared to the reference drug doxorubicin (IC50 = 21.6 µg/ml). The gene expression and DNA damage values and the DNA fragmentation percentages for compound 7g were determined on the lung and liver cell lines. The expression levels of the AMY2A and FOXG1 genes increased significantly (p < 0.01) in the negative samples of lung cancer cells compared with treated cells. Also, the expression values of the PKM and PSPH genes improved significantly (p < 0.01) in the negative samples compared with treated samples of liver cancer cells. The DNA damage values increased significantly (p < 0.01) in treated lung cell line samples (7g) and the positive control. The results showed a significant decrease (p < 0.05) in DNA damage values in the negative samples of liver cancer cells compared to those treated with 7g. However, the DNA fragmentation values increased significantly (p < 0.01) in the treated lung and liver cell line samples compared with the negative control.
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