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1.
Biomed Pharmacother ; 153: 113475, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36076500

RESUMO

BACKGROUND: Cancer remains one of the leading causalities of several morbidity and mortality with negative impact on global economy due to low workforce and management/treatment cost. A number of conventional therapies have been explored in the management/treatment of cancer including chemotherapeutic intervention, radiotherapy, and surgery. Among these treatment modalities, chemotherapy remains the most popular first line of intervention in management/treatment of cancer, and natural products have been implicated as the main source of antineoplastic agents with phenomenal efficacy. However, current antineoplastic agents suffer from lack of selectivity and specificity necessitating the need for further research in the search for novel anticancer drug molecules. METHODS: In this present study, the anticancer activity of Hoslundia opposita leaves extracts were tested against a number of cell lines including human hepatoma cell line (HepG2), human breast cancer cell lines (MDA-MB-231), intestinal epithelial cell lines (Caco-2), and human keratinocyte HACAT cell lines. A bio-guided fractionation assay and the structural elucidation of the pure isolate (hoslundin) was conducted by 1D and 2D NMR spectroscopy. The cell viability, colony formation, and apoptotic activities were investigated using MTT assay, clonogenic assay, and caspase - 3 and - 7 kits respectively. Flow cytometry was employed in assessing the altered cell cycle expression. The production of the intracellular reactive oxygen species (ROS) levels and the reduction of the mitochondrial membrane potential (MMP) was determined at the cellular level using fluorescent probe dyes dihydro-fluorescin diacetate (DCFH-DA) and tetramethylrhodamin (TMRE), respectively. RESULTS: The H. opposita fractions and its pure isolate (hoslundin) demonstrated a potent cytocidal activity against the tumorigenic cells (HepG2, MDA-MB-231, Caco-2) at concentration ranging from 25 to 100 µg/mL. The inhibition of the colony formation was significantly observed in HepG2 cell lines. More so, the cellular viability of the normal cells (HaCaT) was relatively unchanged in the presence of H. opposita fractions and its isolate proving the selectivity of the compounds towards tumourigenic cells. The H. opposita fractions and hoslundin exerted their anticancer activity via cell cycle arrest with the accumulation of the DNA content at the S-phase, activation of apoptosis in the caspase 3,7 activities and depolarized mitochondrial membrane potential mediated by mitochondrial-dependent ROS generation in the treated tumor cells. CONCLUSION: The anticancer activities of Hoslundia opposita Vahl and hoslundin exhibited significant efficacy against tumor cells and well tolerated in the presence of normal cells making them a potential antineoplastic agent.


Assuntos
Antineoplásicos Fitogênicos , Lamiaceae , Neoplasias , Antineoplásicos Fitogênicos/farmacologia , Apoptose , Células CACO-2 , Linhagem Celular Tumoral , Humanos , Potencial da Membrana Mitocondrial , Neoplasias/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo
2.
J Ethnopharmacol ; 127(3): 786-8, 2010 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-19833182

RESUMO

AIM OF THE STUDY: This study evaluated wound healing activity of the chloroform and aqueous fractions of the methanolic extract of Flabellaria paniculata leaf on infected wounds in rats as a follow up to an initial study of the crude extract. MATERIALS AND METHODS: Wounds were inflicted on Wistar rats using excision model. Local infection was introduced into rat abdominal wounds with Staphylococcus aureus and Pseudomonas aeruginosa using a 10(8)cells/ml inoculum. Rate of wound healing was assessed by contraction and period of epithelization. RESULTS: Chloroform fraction exhibited significant wound healing potency (p<0.05) as compared with controls. The test drug achieved 100% wound contraction on day 14 in non-infected group, on day 16 in Staphylococcus aureus infected group and on day 18 in Pseudomonas aeruginosa group. CONCLUSIONS: Chloroform extract of Flabellaria paniculata proves to be a potential anti-infective and wound healing agent. Its in vitro antibacterial and in vivo wound healing activities are in good agreement with the local medicinal use of the plant for skin diseases and sores.


Assuntos
Antibacterianos/uso terapêutico , Malpighiaceae , Fitoterapia , Extratos Vegetais/uso terapêutico , Cicatrização/efeitos dos fármacos , Ferimentos e Lesões/tratamento farmacológico , Animais , Antibacterianos/farmacologia , Masculino , Casca de Planta , Extratos Vegetais/farmacologia , Folhas de Planta , Infecções por Pseudomonas/tratamento farmacológico , Pseudomonas aeruginosa , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Pele/patologia , Infecções Cutâneas Estafilocócicas/tratamento farmacológico , Staphylococcus aureus
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