Abstract Mormodica charantia (Curcubitaceae) is a plant with great medicinal potential, also used as an alternative of mosquitoes control as demonstrated by previous studies. We evaluated the larvicidal activity of crude extracts of ethyl acetate, methanol and hexane from flowers and fruits of M. charantia against Aedes aegypti (Culicidae). Flowers and fruits were macerated in methanol, ethyl acetate and hexane. Bioassays were performed with application of the extracts at final concentrations of 1 - 200 µg/mL in the middle of the third instar larvae of A. aegypti (L3). The results showed high toxicity to ethyl acetate extracts from flowers and fruits at concentrations of 200 µg/mL and 100 µg/mL, with 97% and 87% of larvae mortality (L3), respectively. Hexane extract demonstrated low toxicity, while methanol extract exhibited 78% larval mortality. The data suggested that the ethyl acetate extracts of flowers and fruits of M. charantia can effectively contribute to larvicidal activity. In addition, purification of M. charantia extracts may lead to a promising larvicidal activity to control the A. aegypti population.
Toxicity of micro or nanoplastics (MP/NP) in aquatic life is well-documented, however, information about the consequences of exposure to these particles in terrestrial species is scarce. This study was used to evaluate the uptake and/or toxicity of polystyrene MP/NP in human gastric cells, comparing doses, particle sizes (50, 100, 200, 500, 1000 or 5000 nm) and surface functionalization (aminated, carboxylated or non-functionalized). In general, the uptake of 50 nm particles was significantly higher than 1000 nm particles. Among the 50 nm particles, the aminated particles were more avidly taken up by the cells and were cytotoxic at a lower concentration (≥ 7.5 μg/mL) compared to same sized carboxylated or non-functionalized particles (≥ 50 μg/mL). High toxicity of 50 nm aminated particles corresponded well with significantly high rates of apoptosis-necrosis induced by these particles in 4 h (29.2% of total cells) compared to all other particles (≤ 16.8%). The trend of apoptosis-necrosis induction by aminated particles in 4 h was 50 > 5000 > 1000 > 500 > 200 > 100 nm. The 50 nm carboxylated or non-functionalized particles also induced higher levels of apoptosis-necrosis in the cells compared to 100, 1000 and 5000 nm particles with same surface functionalization but longer exposure (24 h) to 50 nm carboxylated or non-functionalized particles significantly (p<0.0001) increased apoptosis-necrosis in the cells. The study demonstrated that the toxicity of MP/NP to gastric cells was dependent on particle size, dose surface functionalization and exposure period.
Background: Andrographolide (Andro) is a diterpenoid component of the plant Andrographis paniculata that is known for its anti-tumor activity against a variety of cancer cells. Methods: We studied the effects of Andro on the viability of the human leukemia monocytic cell line THP-1 and the human multiple myeloma cell line H929. Andro was compared with cytosine arabinoside (Ara-C) and vincristine (VCR), which are well-established therapeutics against hematopoietic tumors. The importance of reactive oxygen species (ROS) production for the toxicity of each agent was investigated by using an inhibitor of ROS production, N-acetyl-L-cysteine (NAC). Results: Andro reduced the viability of THP-1 and H929 in a dose-dependent manner. H929 viability was highly susceptible to Andro, although only slightly susceptible to Ara-C. The agents Andro, Ara-C, and VCR each induced apoptosis, as shown by cellular shrinkage, DNA fragmentation, and increases in annexin V-binding, caspase-3/7 activity, ROS production, and mitochondrial membrane depolarization. Whereas Ara-C and VCR increased the percentages of cells in the G0/G1 and G2/M phases, respectively, Andro showed little or no detectable effect on cell cycle progression. The apoptotic activities of Andro were largely suppressed by NAC, an inhibitor of ROS production, whereas NAC hardly affected the apoptotic activities of Ara-C and VCR. Conclusions: Andro induces ROS-dependent apoptosis in monocytic leukemia THP-1 and multiple myeloma H929 cells, underlining its potential as a therapeutic agent for treating hematopoietic tumors. The high toxicity for (thus forming: The high toxicity for H929 cells, by a mechanism that is different from that of Ara-C and VCR, is encouraging for further studies on the use of Andro against multiple myeloma.) H929 cells, by a mechanism that is different from that of Ara-C and VCR, is encouraging for further studies on the use of Andro against multiple myeloma.
The utility of clinically available antifungals is limited by their narrow spectrum of activity, high toxicity, and emerging resistance. Antifungal drug discovery has always been a challenging area, since fungi and their human host are eukaryotes, making it difficult to identify unique targets for antifungals. Novel antifungals in clinical development include first-in-class agents, new structures for an established target, and formulation modifications to marketed antifungals, in addition to repurposed agents. Membrane interacting peptides and aromatherapy are gaining increased attention in the field. Immunotherapy is another promising treatment option, with antifungal antibodies advancing into clinical trials. Novel targets for antifungal therapy are also being discovered, allowing the design of new promising agents that may overcome the resistance issue. In this mini review, we will summarize the current status of antifungal drug pipelines in clinical stages, and the most recent advancements in preclinical antifungal drug development, with special focus on their chemistry.
Ciguatera poisoning is caused by the ingestion of fish or shellfish contaminated with ciguatoxins produced by dinoflagellate species belonging to the genera Gambierdiscus and Fukuyoa. Unlike in the Pacific region, the species producing ciguatoxins in the Atlantic Ocean have yet to be definitely identified, though some ciguatoxins responsible for ciguatera have been reported from fish. Previous studies investigating the ciguatoxin-like toxicity of Atlantic Gambierdiscus species using Neuro2a cell-based assay identified G. excentricus as a potential toxin producer. To more rigorously characterize the toxin profile produced by this species, a purified extract from 124 million cells was prepared and partial characterization by high-resolution mass spectrometry was performed. The analysis revealed two new analogs of the polyether gambierone: sulfo-gambierone and dihydro-sulfo-gambierone. Algal ciguatoxins were not identified. The very low ciguatoxin-like toxicity of the two new analogs obtained by the Neuro2a cell-based assay suggests they are not responsible for the relatively high toxicity previously observed when using fractionated G. excentricus extracts, and are unlikely the cause of ciguatera in the region. These compounds, however, can be useful as biomarkers of the presence of G. excentricus due to their sensitive detection by mass spectrometry.
Hexavalent chromium (Cr(VI)) is a critical pollutant with high toxicity, even at trace concentrations. Cr(VI) is possibly carcinogenic and mutagenic and can produce serious health issues. Hence, it is necessary to remove Cr(VI) from the water before releasing it into the environment. Currently, numerous removal techniques were used. Adsorption is the best method compared to others because it is simple, cheap, highly efficient, and can be used in water having trace concentrations of contaminants. Biomass-based waste materials (BMWs) are found as far better adsorbents than commercially and other available adsorbents. In this study, the existing Cr(VI) removal techniques are reviewed and, a broad range of current research studies of Cr(VI) removal from water by using BMWs are evaluated. This review can be helpful to develop a more efficient, cheap, reliable, and environmentally benign bio-adsorbent. It is obvious after the literature review given herein that BMWs exhibited potential adsorbents for the removal of Cr(VI). Also, the chemically modified adsorbents exhibited a higher adsorption capacity than unmodified adsorbents.
The oral mucositis is an adverse event of radiotherapy and/or high toxicity chemotherapy. The Solidago chilensis (Arnica) has been used for its antiseptic, analgesic, healing and anti-inflammatory properties. Objective: The purpose of this study was to evaluate the uses of Arnica for oral mucositis prevention in patients submitted to radiotherapy for head and neck tumors treatment and/or high toxicity chemotherapy. Methodology: The determination of the cytotoxicity index of the aqueous extract was determined in vitro. The oral mucosa was evaluated in days 0, 10 and 14 of patients in the groups: treated with lasertherapy (L, n=18), treated with Arnica (A, n=24) and, treated with lasertherapy associated with Arnica (LA, n=4). It was considered significant p<0.05. Results: It was determined IC50=90,74 μg/mL of Arnica’s aqueous extract in SCC-4 cells. The development of oral mucositis was associated with the type of treatment for oral mucositis prevention: L, A, and LA (χ2 = 24,72, p<0.0001). The level of oral mucositis had significant interaction with the type of prevention treatment [F(2) = 9.545, p<0.0001] and, within 14 days [F(2) = 11.995, p<0.0001]. Conclusions: The results obtained suggest which the use of Solidago chilensis (Arnica) can be an important therapeutic option for treatment with low-level laser therapy for oral mucositis prevention in patients submitted of head and neck radiotherapy and/or high toxicity chemotherapy.
Although both beryllium and its compounds display high toxicity, little attention has been focused on the removal of beryllium from wastewaters. In this research, magnetically modified biochar obtained from poor-quality wheat with two distinct FexOy contents was studied as a sorbent for the elimination of beryllium from an aqueous solution. The determined elimination efficiency was higher than 80% in both prepared composites, and the presence of FexOy did not affect the sorption properties. The experimental qmax values were determined to be 1.44 mg/g for original biochar and biochar with lower content of iron and 1.45 mg/g for the biochar with higher iron content. The optimum pH values favorable for sorption were determined to be 6. After the sorption procedure, the sorbent was still magnetically active enough to be removed from the solution by a magnet. Using magnetically modified sorbents proved to be an easy to apply, low-cost, and effective technique.
It has been known for years that the phenolic compounds are able to exert harmful effects toward living organisms including humans due to their high toxicity. Living organisms were exposed to these phenolic compounds as they were released into the environment as waste products from several fast-growing industries. In this regard, tremendous efforts have been made by researchers to develop sensing methods for the detection of these phenolic compounds. Graphene and conducting polymers-based materials have arisen as a high potential sensing layer to improve the performance of the developed sensors. Henceforth, this paper reviews the existing investigations on graphene and conducting polymer-based materials incorporated with various sensors that aimed to detect hazardous phenolic compounds, i.e., phenol, 2-chlorophenol, 2,4-dichlorophenol, 2,4,6-trichlorophenol, pentachlorophenol, 2-nitrophenol, 4-nitrophenol, 2,4-dinitrophenol, and 2,4-dimethylphenol. The whole picture and up-to-date information on the graphene and conducting polymers-based sensors are arranged in systematic chronological order to provide a clearer insight in this research area. The future perspectives of this study are also included, and the development of sensing methods for hazardous phenolic compounds using graphene and conducting polymers-based materials is expected to grow more in the future.