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1.
Arch Pharm (Weinheim) ; 354(9): e2100120, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34085721

RESUMO

Medicinal plants are valuable sources of different active constituents that are known to have important pharmacological activities including anticancer effects. Lupeol, a pentacyclic triterpenoid, present in many medicinal plants, has a wide range of biological activities. Although the anticancer activity of lupeol was reported, the published data are inconsistent and the clear mechanism of action has never been assigned. The current study aims at investigating the anticancer specificity and mechanism of lupeol isolated from Avicennia marina, which grows in the desert of the United Arab Emirates. The compound was purified by chromatography and identified by spectroscopy. Compared with a negative control, lupeol caused significant (p < .001) growth inhibitory activity on MCF-7 and Hep3B parental and resistant cells by 45%, 46%, 72%, and 35%, respectively. The mechanism of action of lupeol was further explored by measuring its effect on key players in cancer development and progression, BCL-2 anti-apoptotic and BAX pro-apoptotic proteins. Lupeol significantly (p < .01) downregulated BCL-2 gene expression in parental and resistant Hep3B cells by 33 and 3.5 times, respectively, contributing to the induction of apoptosis in Hep3B cells, whereas it caused no effect on BAX. Furthermore, the immunoblotting analysis revealed that lupeol cleaved the executioner caspase-3 into its active form. Interestingly, lupeol showed no significant effect on the proliferation of monocytes, whereas it caused an increase in the sub-G1 population and a reduction in the apoptosis rates of monocytes at 48 and 72 h, indicative of no immuno-inflammatory responses. Collectively, lupeol can be considered as promising effective and safe anticancer agent, particularly against Hep3B cancer cells.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Avicennia/química , Triterpenos Pentacíclicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Regulação para Baixo/efeitos dos fármacos , Feminino , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia , Células MCF-7 , Monócitos/efeitos dos fármacos , Monócitos/metabolismo , Triterpenos Pentacíclicos/isolamento & purificação , Proteínas Proto-Oncogênicas c-bcl-2/genética , Fatores de Tempo
2.
J Ethnopharmacol ; 263: 113179, 2020 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-32768642

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Avicennia marina (Forssk.) Vierh. is a historic plant, well-known for many centuries in traditional and folk use medicine. A. marina is an evergreen tree belongs to Acanthaceae family. The plant is the most widespread mangrove in the tropical and subtropical regions of Indo-West-Pacific area. Current scientific data confirmed the medicinal values of A. marina. The pharmacological activity of the plant is attributed to the presence of several phytochemical classes. AIM OF THE STUDY: To evaluate the link between the traditional use of the plant and the scientific data accumulated over time including both the phytochemical analysis and therapeutic activities. Additionally, to evaluate the usage of obtained data for further development of the plant and its products in the pharmaceutical market. MATERIALS AND METHODS: The data related to traditional medicine, therapeutic uses, phytochemical analysis and market availability of A. marina and its products from different geographical regions were collected. The collected data was compared and the research gaps were identified in order to highlight areas that can be employed to improve plant-based research and development. RESULTS: Although the wide geographical distribution of the plant, its historic traditional use, richness of phytochemicals and diverse pharmacological activities, the utilization of these data has never been exploited for human health and several gaps were identified. These gaps include the lack of phyto-geographical comparison of the plant, the lack of proper mapping of traditional use to the scientific data and inadequate exploration of plant phytochemicals by researchers. CONCLUSIONS: A. marina is an old tree that has evolved over centuries and adapted diverse climates. It contains a pool of potential phytochemicals that can be employed for the discovery of drugs after careful studies. Scientists are required to invest money and time to explore these renewable and natural sources of drugs and design drug formulations to overcome current difficult to treat health issues and fight against the era of drug resistant.


Assuntos
Avicennia , Etnofarmacologia/métodos , Medicina Tradicional/métodos , Compostos Fitoquímicos/uso terapêutico , Fitoterapia/métodos , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/uso terapêutico , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/uso terapêutico , Etnofarmacologia/tendências , Humanos , Medicina Tradicional/tendências , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Fitoterapia/tendências , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico
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