ABSTRACT
Background: More than half of traditional medicines are of natural origin and research has shown that these are associated with fewer side effects than the synthetic ones, since less than 10% of the 350,000 identified plant species have been exposed to some amount of bioactive screens, it is now the aim of researchers to screen more plants and also identify the active ingredients responsible for detected bioactivities. These we believe may provide the foundation for identifying new drug leads that may prove useful against chronic lifestyle diseases. This review takes a look at the work that has currently been conducted on Tillandsia recurvata commonly known as ball moss which is believed to assist with future research. Results: The chloroform, methanol and water extracts of ball moss have shown cytotoxicity against several human cancer cell lines and the methanol extract induces apoptosis in some. Further the chloroform extract was shown to reduce angiogenesis and the methanol extract inhibited particular kinases (CSNK2A2, MEK5, GAK, FLT and DRAK1) of which MEK5 and GAK have been implicated in prostate cancer. The same extract was further shown to display promising anti-diabetic properties via a reduction in fasting blood glucose (P<0.05), fructosamine levels (P<0.05), serum CRP and insulin levels when compared to the control mice. Phytochemical screens identified a novel glycoside and several cycloartanes and dicinnamtes; 1,3-di-O-Cinnamoyl-glycerol and (E)-3-(cinnamoyloxy)-2-hydroxypropyl 3-(3,4-dimethoxyphenyl)acrylate. Further bioactive screens on these isolates showed that cycloartane-3,24,25-triol reduced the viability of prostate PC-3 and DU145 cell lines. This isolate was further shown to inhibit MRCKα kinase implicated in the initiation and progression of prostate cancer. Conclusions: This review confirms the promising efficacy of the T. recurvata plant and so its worth for further research which may prove useful in the pharmaceutical and nutraceutical industries. Such benefits have already begun with the introduction of the alpha prostate formula, now on the market for improved prostate health.
ABSTRACT
Aim: The role of Kinases in cancer onset and progression has made kinases a target for the control of some cancers. Recent discoveries that kinases are most effectively inhibited by small molecules have also resulted in an increased search for small molecule kinase inhibitors. Cycloartanes are small molecules found in many medicinal plants including the Jamaican Ball Moss (Tillandsia recurvata). Recent studies on T. recurvata have demonstrated that it possesses anticancer activity. Cycloartane-3,24,25- triol, an analog of a cycloartane identified in Ball moss was also shown to have inhibitory activity against MRCKα kinase. This study was as such set up to determine the MRCKα/β kinase inhibition activity of other cycloartanes in Ball Moss and their analogs. MRCKα/β kinases has been identified as an important kinase implicated in cancer onset and progression and as such a potential drug target. Methodology: Kinase inhibition activity of 6 cycloartanes was investigated using the ligand-kinase binding assay. The WST-1 reagent assay was also used to determine the antiproliferation activity of the cycloartanes against some prostate and breast cancer cell lines. Results: Cycloart-23-ene-3,25-diol (1), Cycloartane-3,24,25-triol (2), Cycloart-25-ene- 3,24-diol (3), 3,23-Dioxo-9,19-cyclolanost-24-en-26-oic acid (4), 24,25- Dihydroxycycloartan-3-one (5) inhibited the MRCKα kinase with Kd of 0.21 μM, 0.25μM, 0.36 μM, 3.0 μM and 2.1 μM respectively. Hydroxycycloart-23-en-3-one,25, (6) showed no inhibition against the MRCKα kinase. Compounds 1, 3, 4, 5 inhibited the MRCKβ kinase with Kd of 4.7 μM, 1.10 μM, 3.2 μM and 9.8 μM, respectively. Three of the six cycloartanes exhibited antiproliferation activity against two prostate and breast cancer cell lines each. Conclusion: Cycloart-23-ene-3,25-diol (1) showed the most promising activity against the MRCKα/β kinase out of the 6 cycloartanes screened demonstrating an interesting structure activity relationship profile when compared with the other molecules. Cycloart- 23-ene-3,25-diol (1) deserves further studies to determine its in vivo activity as well.
ABSTRACT
A cobertura superior das florestas tropicais, formada pelas copas das árvores, constitui um ambiente de extrema diversidade vegetal. Contribuindo com a grande riqueza dessas florestas encontram-se as espécies botânicas epífitas, cuja importância pode ser observada do ponto de vista ecológico, faunístico, etnobotânico e até mesmo farmacológico. Dentre as espécies adaptadas à vida epifítica podemos citar as bromeliáceas, que compõem uma das famílias mais representativas dessa flora com elevada variabilidade genética. Tillandsia recurvata é uma espécie epífita cosmopolita, nativa, adaptada a habitats áridos, utilizada para o tratamento de diversas doenças, mas pouco se tem publicado a respeito das comprovações científicas de suas propriedades. O presente trabalho revisa os aspectos etnofarmacológicos, atividades biológicas e compostos químicos relacionados à espécie em questão, pertencente à Bromeliaceae. A partir do levantamento de dados realizado, observa-se que esta se trata de uma espécie de conhecido uso popular no tratamento de diferentes distúrbios, com alguns estudos farmacológicos que comprovam suas propriedades terapêuticas. Do ponto de vista químico observa-se a presença de terpenos, flavonoides e derivados cinâmicos em sua constituição, em que alguns compostos isolados ilustram a potencialidade desta espécie como fonte de biomoléculas de interesse. Todos estes aspectos considerados nesta revisão contribuem para o conhecimento a respeito da importância biológica e o potencial terapêutico acerca dos metabólitos desta promissora espécie.
The canopy of tropical forests, formed by the crowns of trees, constitutes a habitat of extreme plant diversity. Contributing to the great richness of these forests are epiphytes, which are of outstanding importance from the ecological, faunal, ethnobotanical and even pharmacological standpoints. Among the species adapted to the epiphytic life (growing on other plants) are the bromeliads, one of the most representative families of that flora, possessing high genetic variability. Tillandsia recurvate is a cosmopolitan epiphyte adapted to arid habitats, traditionally used to treat various diseases, though little has been published on scientific evidence for its properties. This paper reviews its ethnopharmacology and the biological activities and chemical compounds related to this member of the Bromeliaceae. According to the data collected, this species is known for its popular use in the treatment of various disorders, with some pharmacological studies that demonstrate its therapeutic properties. From the chemical point of view, terpenes, flavonoids and cinnamic acid derivatives are found in its constitution and some of the compounds isolated illustrate the potential of this species as a source of interesting biomolecules. All these features reviewed here contribute to what is known about the biological importance and therapeutic potential of metabolites from this promising species.
Subject(s)
Bromelia , Bromeliaceae/chemistry , Tillandsia/chemistryABSTRACT
OBJECTIVE: Tillandsia recurvata, also commonly known as Ball Moss, is endemic to Jamaica and some parts of the Caribbean and South America. The plant, despite being reported to be used in folk medicine, had not previously been evaluated for its anti-cancer potential. The aim of this study was to evaluate the anti-cancer activity of Ball Moss. METHODS: The anti-proliferation activity of the crude methanolic extract of the T recurvata was evaluated in vitro in five different histogenic cancer cell lines (prostate cancer - PC-3, breast cancer, Kaposi sarcoma, B-16 melanoma and a B-cell lymphoma from a transgenic mouse strain) using the trypan blue assay. The crude extract was also evaluated in vivo in tumour-bearing mice. Immunohistochemistry staining with Apoptag was used for histology and determination of apoptosis. RESULTS: The crude methanolic extract of T recurvata demonstrated anti-proliferation activity against all the cell lines, killing > 50% of the cells at a concentration of 2.5 µg/ml. Kaposi sarcoma xenograft tumours were inhibited by up to 75% compared to control in the in vivo study (p < 0.05). There was evidence of DNA fragmentation and a decrease in cell viability on histological studies. The methanolic extract showed no toxic effect in the mice at a dose of 200 mg/kg. CONCLUSIONS: Our data suggest that T recurvata has great potential as an anti-cancer agent and that one of its mechanisms of cell kill and tumour inhibition is by the induction of apoptosis.
OBJETIVO: La Tillandsia recurvata, también conocida como bola de musgo, es endémica en Jamaica, así como en algunas partes del Caribe y América del sur. Si bien se había reportado su uso como parte de la medicina popular, esta planta no había sido evaluada previamente en relación con su potencial para la lucha contra el cáncer. El objetivo de este estudio fue evaluar la actividad anticancerígena de la bola de musgo. MÉTODOS: La actividad antiproliferativa del extracto metanólico crudo de la T recurvata, fue evaluada in vitro en cinco líneas celulares diferentes de cáncer histogenético (cáncer de próstata - PC-3, cáncer de mama, sarcoma de Kaposi, melanoma B-16 y un linfoma de células B de una cepa de ratón transgénico) usando el ensayo con azul de tripano. El extracto crudo también se evaluó in vivo en ratones portadores de tumor. La tinción inmunohistoquímica con ApopTag fue utilizada para la histología y determinación de la apoptosis. RESULTADOS: El extracto metanólico crudo de T recurvata demostró la actividad proliferativa frente a todas las líneas celulares, matando > 50% de las células a una concentración de 2,5 µg/ml. Los tumores de xenoinjerto de sarcoma de Kaposi fueron inhibidos hasta un 75% en comparación con el control en el estudio in vivo (p < 0.05). Hubo evidencia de fragmentación de DNA y una disminución en la viabilidad celular en los estudios histológicos. El extracto metanólico no mostró ningún efecto tóxico en los ratones a dosis de 200 mg/kg. CONCLUSIONES: Nuestros datos sugieren que la T recurvata tiene gran potencial como agente anticanceroso, y que uno de sus mecanismos de inhibición de tumores y muerte de las células tiene lugar mediante la inducción de la apoptosis.