Among the triterpenoids, oleanolic acid (OA) and its isomer, ursolic acid (UA) are promising therapeutic candidates, with potential benefits in the management of melanoma. In this study, we aimed to examine the in vitro and in vivo anti-invasive and anti-metastatic activity of OA and UA to determine their possible usefulness as chemopreventive or chemotherapeutic agents in melanoma. For the in vitro experiments, the anti-proliferative activity of the triterpenic compounds on SK-MEL-2 melanoma cells was examined. The anti-invasive potential was assessed by testing the effects of the active compound on vascular cell adhesion molecule (VCAM) and intercellular adhesion molecule (ICAM) adhesion to melanoma cells. Normal and tumor angiogenesis were evaluated in vivo by chicken embryo chorioallantoic membrane (CAM) assay. The two test triterpenoid acids, UA and OA, exerted differential effects in vitro and in vivo on the SK-MEL-2 melanoma cells. UA exerted a significant and dose-dependent anti-proliferative effect in vitro, compared to OA. The cytotoxic effects in vitro on the melanoma cells were determined by the examining alterations in the cell cycle phases induced by UA that lead to cell arrest in the S phase. Moreover, UA was found to affect SK-MEL-2 melanoma cell invasiveness by limiting the cell adhesion capacity to ICAM molecules, but not influencing their adhesion to VCAM molecules. On the whole, in this study, by assessing the effects of the two triterpenoids in vivo, our results revealed that OA had a greater potential to impair the invasive capacity and tumor angiogenesis compared with UA.
Fluconazole is a bistriazole derivative with antifungal activity. The major weak points of fluconazole are the development of antifungal resistance and low water solubility, which impairs its administration. Binary systems between fluconazole and beta-cyclodextrin were prepared with the aim of obtaining a new delivery system that will overcome the limitations of fluconazole administration. Using two feasible laboratory methods, inclusion complexes between fluconazole and beta-cyclodextrin were obtained. Thermal and spectroscopic analyses were used to characterize the inclusion complexes.
Dental pathology remains a global health problem affecting both children and adults. The most important dental diseases are dental caries and periodontal pathologies. The main cause of oral health problems is overpopulation with pathogenic bacteria and for this reason, conventional therapy can often be ineffective due to bacterial resistance or may have unpleasant side effects. For that reason, studies in the field have focused on finding new therapeutic alternatives. Special attention is paid to the plant kingdom, which offers a wide range of plants and active compounds in various pathologies. This review focused on the most used plants in the dental field, especially on active phytocompounds, both in terms of chemical structure and in terms of mechanism of action. It also approached the in vitro study of active compounds and the main types of cell lines used to elucidate the effect and mechanism of action. Thus, medicinal plants and their compounds represent a promising and interesting alternative to conventional therapy.
Melissa officinalis is a medicinal herb with an extensive pharmacological profile that has been proven to have beneficial effects in oral and gastrointestinal disorders. However, the effects of this plant in oral, pharyngeal, and colorectal malignancies, types of cancer with an increased incidence in recent years, are less investigated. The present study aims to evaluate the pharmacological profile of a Melissa officinalis total extract for potential benefits in oral, pharynx and colorectal carcinoma. The LC-MS profile of MO total extract (MOte) indicated a rich content in polyphenols, data that support the potent antioxidant capacity exhibited and the antimicrobial activity against both Gram-negative and Gram-positive bacteria. In addition, MOte triggered a dose-dependent and selective decrease in the viability of tumor cells (tongue and pharynx squamous cell carcinomas, and colorectal adenocarcinoma), with the most significant effect being recorded at 100 µg/mL. At the same concentration, MOte exhibited an antiangiogenic effect by inhibiting the process of angiogenesis in ovo. Overall, our findings support the potential benefits of Melissa officinalis leaf total extract as a valuable candidate for the prophylaxis of oral, pharyngeal and colorectal neoplasms.
The cloves are antiseptic, antiparasitic, antibacterial, antifungal, antiviral, anesthetic, analgesic, anti-inflammatory, tonic, carminative, anti-ulcer, antithrombotic, antioxidant and anti-cancerous. They contain eugenol, tannins and flavonoids that also help to strengthen the vein wall. This paper presents the obtaining and the characterization of a polyurethane drug delivery system which can be used for the transmembrane transport of eugenol in oral therapies. The products were analyzed by pH and solubility measurements, thermal decomposition and zetasizer tests and they were applied on mice skin to evaluate their harmfulness. The results suggest that were obtained neutral pH structures with low solubility and a good thermal stability, with sizes between 241 and 289 nm and no toxicity effect was found in the case of studied samples.
In the present research, ethanolic and methanolic extracts of Teucrium polium (germander) were studied regarding the content of biologically active substances - in particular polyphenols - antioxidant activity and antibacterial activity. The extracts have been found to be rich in polyphenolic compounds, kaempferol and epichatechin have been found to be present in the highest concentrations. The antioxidant activity evaluated by the method of capturing the free radicals with DPPH revealed values close to those produced by the ascorbic acid. Antimicrobial activity was evaluated by the diffusimetric method and S. aureus and E. coli microorganisms were found to be the most sensitive while P. aeruginosa and fungal species were not sensitive.
Malignant melanoma represents the deadliest type of skin cancer with narrow treatment options in advanced stages. Herbal constituents possessing anticancer properties occupy a particular spot in melanoma research as potential chemotherapeutics. Rutin (RUT) is a natural compound exerting antioxidant, antimicrobial, anti-inflammatory, UV-filtering, and SPF-enhancing activities that are beneficial to the skin; however, its effect as an anti-melanoma agent is less investigated. The current study is focused on assessing the cytotoxic potential of RUT against two different human melanoma cell lines: RPMI-7951 and SK-MEL-28 by evaluating its impact in terms of cell viability, cells’ morphology, and nuclear aspect assessment, and senescence-inducing properties. The results indicate a dose-dependent decrease in the viability of both cell lines, with calculated IC50 values of 64.49 ± 13.27 μM for RPMI-7951 cells and 47.44 ± 2.41 μM for SK-MEL-28, respectively, accompanied by a visible reduction in the cell confluency and apoptotic features within the cell nuclei. RUT exerted a senescence-inducing property highlighted by the elevated expression of senescent-associated beta-galactosidase (SA-β-gal) in SK-MEL-28 cells. Despite the in vitro anti-melanoma effect revealed by our results, further studies are required to elucidate the mechanisms of RUT-induced cytotoxicity and senescence in melanoma cells.
Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.
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