Isobavachalcone (IBC) is a natural prenylated chalcone with a broad spectrum of pharmacological properties. In this work, we newly synthesized and investigated the antibacterial activity of IBC against Gram-positive, Gram-negative and mycobacterial species. IBC was active against Gram-positive bacteria, mainly against Methicillin-Susceptible Staphylococcus aureus (MSSA) and Methicillin-Resistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL, respectively. On the other hand, IBC was not able to act against Gram-negative species (MIC > 400 µg/mL). IBC displayed activity against mycobacterial species (MIC = 64 µg/mL), including Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. IBC was able to inhibit more than 50% of MSSA and MRSA biofilm formation at 0.78 µg/mL. Its antibiofilm activity was similar to vancomycin, which was active at 0.74 µg/mL. In order to study the mechanism of the action by fluorescence microscopy, the propidium iodide (PI) and SYTO9 fluorophores indicated that IBC disrupted the membrane of Bacillus subtilis. Toxicity assays using human keratinocytes (HaCaT cell line) showed that IBC did not have the capacity to reduce the cell viability. These results suggested that IBC is a promising antibacterial agent with an elucidated mode of action and potential applications as an antibacterial drug and a medical device coating.

Background: Aedes aegypti is currently controlled with synthetic larvicides; however, mosquitoes have become highly resistant to these larvicides and difficult to eradicate. Studies have shown that insecticides derived from fungal extracts have various mechanisms of action that reduce the risk of resistance in these mosquitoes. One possible mechanism is uncontrolled production of reactive oxygen species (ROS) in the larvae, which can cause changes at the cellular level. Thus, the crude extract of Xylaria sp. was evaluated to investigate the oxidative effect of this extract in A. aegypti larvae by quantifying the oxidative damage to proteins and lipids. Methods:The larvicidal potential of the crude extract of Xylaria sp. Was evaluated, and the extract was subsequently tested in human lung fibroblasts for cytotoxicity and ROS production. ROS level was quantified in the larvae that were killed following exposure to the extract in the larvicide test. Results:The crude extract of Xylaria sp. Caused cytotoxicity and induced ROS production in human lung fibroblasts and A. aegypti larvae, respectively. In the larvicide trial, the extract showed an LC 50 of 264.456 ppm and an LC90 of 364.307 ppm, and was thus considered active. The extract showed greater oxidative damage to lipids and proteins, with LC 90 values of 24.7 µmol MDA/L and 14.6278 ×10 -3 nmol carbonyl/ mg protein, respectively.Conclusions: Crude extracts of Xylaria sp. induced oxidative stress that may have caused the mortality of A. aegypti larvae.

: Neglected tropical diseases are a serious global public health problem and they are one of the main causes of mortality and morbidity, especially in underdeveloped countries. These diseases have several implications for health and they are considered a priority in global eradication programs for disease control. The aim of this mini-review is to report recent studies on the fight against neglected diseases, namely dengue fever, chikungunya, zika, malaria protozoa, Chagas disease, leishmaniasis, schistosomiasis helminths, filariasis, and tuberculosis bacteria using extracts and isolated substances of endophytic fungi based on their bioactivity profiles in relation to these diseases.

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