Anemone nemorosa is part of the Ranunculaceae genus Anemone (order Ranunculales) which comprises more than 150 species. Various parts of the plant have been used for the treatment of numerous medical conditions such as headaches, tertian agues, rheumatic gout, leprosy, lethargy, eye inflammation as well as malignant and corroding ulcers. The Anemone plants have been found to contain various medicinal compounds with anti-cancer, immunomodulatory, anti-inflammatory, anti-oxidant and anti-microbial activities. To date there has been no reported evidence of its use in the treatment of cancer. However, due to the reported abundance of saponins which usually exert anti-cancer activity via cell cycle arrest and the induction of apoptosis, we investigated the mode of cell death induced by an aqueous A. nemorosa extract by using HeLa cervical cancer cells. Cisplatin was used as a positive control. With a 50% inhibitory concentration (IC50) of 20.33 ± 2.480 µg/mL, treatment with A. nemorosa yielded a delay in the early mitosis phase of the cell cycle. Apoptosis was confirmed through fluorescent staining with annexin V-FITC. Apoptosis was more evident with A. nemorosa treatment compared to the positive control after 24 and 48 h. Tetramethylrhodamine ethyl ester staining showed a decrease in mitochondrial membrane potential at 24 and 48 h. The results obtained imply that A. nemorosa may have potential anti-proliferative properties.
The use of some very well-known chemotherapeutic agents, such as cisplatin, is limited by toxicity in normal tissues and the development of drug resistance. In order to address drug resistance and the side-effects of anti-cancer agents, recent research has focused on finding novel combinations of anti-cancer agents with non-overlapping mechanisms of action. The cytotoxic effect of the synthetic 5-aminopyrazole derivative N-[[3-(4-bromophenyl)-1H-pyrazol-5-yl]-carbamothioyl]-4-chloro-benzamide (BC-7) was evaluated by the bis-Benzamide H 33342 trihydrochloride/propidium iodide (Hoechst 33342/PI) dual staining method against HeLa, MeWo, HepG2, Vero, and MRHF cell lines. Quantitative fluorescence image analysis was used for the elucidation of mechanism of action and synergism with cisplatin in HeLa cells. BC-7 displayed selective cytotoxicity towards HeLa cells (IC50 65.58 ± 8.40 μM) and induced apoptosis in a mitochondrial- and caspase dependent manner. This was most likely preceded by cell cycle arrest in the early M phase and the onset of mitotic catastrophe. BC-7 increased the cytotoxic effect of cisplatin in a synergistic manner with combination index (CI) values less than 0.9 accompanied by highly favourable dose reduction indices. Therefore, the results obtained support the implication that BC-7 has potential anti-cancer properties and that combinations of BC-7 with cisplatin should be further investigated for potential clinical applications.
Flavonoids are a class of biologically active compounds with various proven nutraceutical benefits. In flavonoid C-glycosides, the aglycones are attached to sugar residues via cleavage-resistant C-C bonds which alter typical flavonoid pharmacokinetic properties. In these compounds, the combination of biological activities from the flavonoid moieties and sugar residues create unique and more diverse biological functions than those of O-glycosylated and unsubstituted flavonoids. Through a series of reverse phase chromatography techniques and various spectroscopic methods, the phytochemical investigation of Drimia altissima (L.F.) Ker Gawl., a specie from the Asparagaceae family, led to the isolation and chemical characterisation of a novel C-glucosylflavonoid, altissimin, with a unique apioglucoside arrangement to the apigenin aglycone. Altissimin was found to possess strong in vitro anti-proliferative activity against HeLa cervical cancer cells.
Zebrafish have become a popular alternative to higher animals in biomedical and pharmaceutical research. The development of stable mutant lines to model target specific aspects of many diseases, including diabetes, is well reported. However, these mutant lines are much more costly and challenging to maintain than wild-type zebrafish and are simply not an option for many research facilities. As an alternative to address the disadvantages of advanced mutant lines, wild-type larvae may represent a suitable option. In this review, we evaluate organ development in zebrafish larvae and discuss established methods that use wild-type zebrafish larvae up to seven days post fertilization to test for potential drug candidates for diabetes and its commonly associated conditions of oxidative stress and inflammation. This provides an up to date overview of the relevance of wild-type zebrafish larvae as a vertebrate antidiabetic model and confidence as an alternative tool for preclinical studies. We highlight the advantages and disadvantages of established methods and suggest recommendations for future developments to promote the use of zebrafish, specifically larvae, rather than higher animals in the early phase of antidiabetic drug discovery.
Ethnopharmacological relevance: Lippia javanica leaves are popular in traditional food, medicine and for insecticidal uses in various Africa countries and North-East India. Anecdotal evidence suggests that it is safe to use but limited animal studies suggested potential toxicity at high dosages, including hepatotoxicity. Aim of the study: To screen for potential hepatotoxicity of L. javanica leaf extracts in vitro, thereby contributing to its toxicological profile for safe use in food and topical applications. Materials and methods: High content analysis techniques and fluorescent dyes were used to monitor C3A hepatocarcinoma cells for changes in morphological features that are associated with development of mitotoxicity, steatosis, oxidative stress, and lysosomal dysfunction. Results: No changes were observed in cell viability, reactive oxygen species or lysosomal content at concentrations up to 200 μg/ml in C3A cells. Mitochondrial membrane potential was reduced by approximately 10% but this effect was not dose-dependent nor was it accompanied by a reduction in mitochondrial content. A dose-dependent decrease was observed in neutral lipid content. Conclusion: The results from this in vitro study suggest that L. javanica leaf extracts is not anticipated to be hepatotoxic at concentrations in the range that is assumed for food or topical use.
Post-meal hyperglycaemia is considered a prominent therapeutic target to attenuate the progression of diabetes and its associated complications. The present study identified fruit extract of Diospyros lotus Linnaeus, of the Ebenaceae family, as an inhibitor of starch digestion through the inhibition of both alpha amylase and alpha glucosidase. The extract inhibits porcine and human pancreatic amylase with IC50 values of 82.5±2.0 and 130.4±24 μg/ml respectively. The inhibition of intestinal sucrase and maltase activity was however considerably weaker. In vitro hydrolysis of solubilised potato starch into glucose yielded comparable inhibition kinetics for 100 μg/ml D. lotus L. extract and 3.5 μM acarbose. Screening the major phenolic constituents revealed that quercetin and myricetin were the strongest alpha amylase inhibitors. D. lotus L. extract showed strong antioxidant activity; however, this provided no meaningful protection against 2-deoxy-ribose induced oxidative stress in INS-1 cells. Taken together these findings identify D. lotus L. fruit as a multi-component functional food with potential to dampen the onset and development of diabetes through the inhibition of post meal hyperglycaemia.
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