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In vitro and In vivo Anti-cancer Effects of Tillandsia recurvata (Ball Moss) from Jamaica
Abstract
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 ofBall Moss.
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.
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 microg/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.
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.
... The Jamaican ball moss (T. recurvata) was collected at Kingston, Jamaica and processed as previously reported (7,8). A voucher specimen of the plant was identified at the Institute of Jamaica Herbarium where it is deposited under Accession Number: IJ 3411. ...
... The bioactivity demonstrated by the Jamaican ball moss against the leukemia cell lines, as well as the activity of its cycloartanes, demonstrate their broad anticancer activity, considering previous findings showing that the Jamaican ball moss has anticancer activity against other cell lines including prostate and breast cancers and melanoma (7,8). Ball moss has also exhibited activity in other assays, helping to explain its possible mechanism of anticancer action. ...
... Ball moss has also exhibited activity in other assays, helping to explain its possible mechanism of anticancer action. Notable amongst these is its antiangiogenic activity (13), inhibition of FMS-like tyrosine kinase 3 (FLT3)(9), as well as induction of cell death via apoptosis (7). The inhibition of FLT3 kinase validates the activity of ball moss against the Molm-14 leukemia cell line in this study, as FLT3 kinase has been found to be expressed in acute myeloid leukemia cell lines and its mutations are usually associated with poor prognosis (14,15). ...
Background:
Approximately 250,000 deaths were caused by leukemia globally in 2012 and about 40%-50% of all leukemia diagnoses end-up in death. Medicinal plants are a rich source for the discovery of new drugs against leukemia and other types of cancers. To this end, we subjected the Jamaican ball moss (Tillandsia recurvata) and its cycloartanes, as well as some analogs, to in vitro screening against a number of leukemia cell lines. The WST-1 anti-proliferation assay was used to determine the anticancer activity of ball moss and two cycloartanes isolated from ball moss and four of their analogs against four leukemia cell lines (HL-60, K562, MOLM-14, monoMac6). Ball moss crude methanolic extract showed activity with a 50% inhibition concentration (IC50) value of 3.028 μg/ml against the Molm-14 cell line but was ineffective against HL-60 cells. The six cycloartanes tested demonstrated varying activity against the four leukemia cancer cell lines with IC50 values ranging from 1.83 μM to 18.3 μM. Five out of the six cycloartanes demonstrated activity, while one was inactive against all four cell lines. The preliminary activity demonstrated by the Jamaican ball moss and its cycloartanes against selected leukemia cell lines continues to throw light on the broad anticancer activity of ball moss. Further studies to evaluate the efficacy of these molecules in other leukemia cell lines are required in order to validate the activity of these molecules, as well as to determine their mechanisms of action and ascertain the activity in vivo in order to establish efficacy and safety profiles.
... In addition, other research has reported T. usneoides as anti-hypertensive and active in rheumatism, hemorrhoids, cholagogue, diuretic, renal and ophthalmic illnesses [38]. Other Tillandsia genera exhibit anti-inflammatory and cytotoxic activity in vitro against different tumor cells [39][40][41]. Crude ethanolic extract of T. recurvata inhibits the growth of Kaposi's sarcoma in mice [41] and its activity has been attributed to the presence of 1,3-di-O-Cinnamoylglycerol and (E)-3-(cinnamoyloxy)-2-hydroxypropyl 3-(3,4-dimethoxyphenyl)acrylate [40]. A flavone (5,3 -dihydroxy-6,7,8,4 -tetramethoxyflavanone) with broad in vitro activity against tumor cells has been isolated and could be useful in glioblastoma multiforme and acute myeloid leukemia in addition to other cancers [39]. ...
... Other Tillandsia genera exhibit anti-inflammatory and cytotoxic activity in vitro against different tumor cells [39][40][41]. Crude ethanolic extract of T. recurvata inhibits the growth of Kaposi's sarcoma in mice [41] and its activity has been attributed to the presence of 1,3-di-O-Cinnamoylglycerol and (E)-3-(cinnamoyloxy)-2-hydroxypropyl 3-(3,4-dimethoxyphenyl)acrylate [40]. A flavone (5,3 -dihydroxy-6,7,8,4 -tetramethoxyflavanone) with broad in vitro activity against tumor cells has been isolated and could be useful in glioblastoma multiforme and acute myeloid leukemia in addition to other cancers [39]. ...
The main limits of current antitumor therapies are chemoresistance, relapses, and toxicity that impair patient quality of life. Therefore, the discovery of therapeutic alternatives, such as adjuvants to conventional therapy that modulate the intracellular oxidation state or the immune response, remains a challenge. Owing to traditional medicine, several uses of plants are known, indicating a promising antitumor and immunomodulatory effect. We evaluated the effect of ethanolic extract of T. usneoides in vitro and in vivo in models of 4T1 breast cancer and B16-F10 melanoma. In vitro evaluations with both cell lines showed that the extract has cytotoxic activity and induces apoptotic cell death. However, its effect on ROS production and glucose uptake was opposite. In vivo, only in the 4T1 model, a significant decrease in tumor size was found in animals treated with the extract, accompanied by an increase in dendritic cells and activated CD8+ T cells, and a decrease in myeloid-derived suppressor-like cells (MDSC-LC) and Tregs in the tumor microenvironment. These results suggest that T. usneoides extract antagonistically regulates tumor metabolism of 4T1 vs. B16-F10, impacting the tumor microenvironment and effective antitumor immune response, leading to a reduction in 4T1 tumor size but not on B16-F10.
... Better IPSS scores and UFM than placebo [137] In admixture with Sabal palm, improvement of obstructive symptoms in those with severe and moderate symptomatology [138] In admixture with P. africanum, no effect compared to placebo [139] Cucurbita pepo Seed oil reduces prostate size in rat model [140] In admixture with E. parviflorum, lycopene, P. africanum, and S. repens shown to have good effects on BPH symptoms after 3 month treatment [141] Roystonea regia Extract prevents the impairment of micturition and histological prostate changes induced by phenylephrine [142] Prostatic carcinoma Serenoa repens Extract in admixture with carotenoid axthathanthin inhibit 5α reductase in prostatic carcinoma cell line LNCap-FGC [143]. Extract decreased expression of anti-inflammatory related genes in 2 PC cell lines LNCaP and PC3 [144] Tillandsia recurvata Inhibit proliferation of cancer cell lines [145] Flavonone HLBT-100 showed broad effect against prostate cancer at doses as low as 0.003 μg/mL [146] RCT, randomized controlled trial. ...
... Although a beneficial effect on BPH has not been shown yet, Tillandsia recurvata, commonly known as Jamaican Ball Moss, which belongs to the Bromeliaceae family, has demonstrated to inhibit human cancer cell-line proliferation (IC50) at low concentrations of 3.75 μg/mL [145]. The in vitro anticancer effects were also tested in a rat model, in which 75% of Kaposi sarcoma were inhibited at a dosage of 200 mg/kg with no toxic effect [176]. ...
Native American populations have been using herbs for millennia to treat ailments and diseases. Male sexual and reproductive health has also been addressed by traditional American herbal medicine using mainly native plants. As a megadiverse zone, the materia prima of this therapeutic approach is vast. In recent years, scientific methods have been used to test the validity of traditional knowledge and to find novel pharmacological agents to treat the ever-growing demand for andrological therapies. This chapter aims to gather evidence of American herbs with attributed effects in andrological issues. Species from North America, Central America, and the Caribbean and South America are reviewed. The majority of studies have been done with in vitro and in vivo models and lack human trials to confirm reliably their properties but enough evidence to justify further research is provided, especially in species such as Lepidium meyenii (Maca), Serenoa repens, and Cucurbita pepo.
... Subsequently, Spjut et al. 1986 [15] summarised the results of the first comprehensive study by NCI on the antitumour properties of extracts from 123 mosses, 13 liverworts, and 1 hornwort species, and reported that 75 species showed varying degrees of cytotoxicity against P388 lymphocytic leukaemia cells. From that time onwards, numerous studies have found that mosses [16][17][18][19][20][21][22][23][24][25][26] and crude liverwort extracts [25,[27][28][29] are cytotoxic for several cancer cell lines (Tables 1 and 2). The molecules responsible for the antiproliferative activity have been identified as terpenoids, bibenzyls, and macrocyclic (bis)bibenzyls, which are reported by various studies as cytotoxic for a wide range of cancer cells (Tables 1 and 2). ...
Bryophytes are a poorly studied group of land plants that have been used in traditional medicine as a multipurpose remedy for centuries. Due to their peculiar morphology and physiology, bryophytes synthesize a multitude of secondary metabolites with a wide range of nutraceutical and pharmaceutical activities. Research has highlighted that secondary metabolites in bryophytes can also act as antitumour agents. Several studies have shown that bryophyte extracts and pure metabolites are cytotoxic against many cancer cell lines. Interestingly, some of these molecules and their derivatives are capable of acting on a specific target in cancer cells. Some macrocy-clic(bis)bibenzyls from bryophytes can inhibit P-glycoprotein, reverting multidrug resistant cancer cell phenotypes, induce depolymerization of tubulin, stimulate apoptotic pathways, and inhibit an-giogenesis. This brief review aims to collect recent knowledge on secondary metabolites of bryo-phytes and their derivatives, which have demonstrated an interaction with different molecular processes in cancer cells.
... Jamaica has a wide array of selfmedicated herbs and medicinal plants in use against illnesses [7], with some displaying anti-cancer properties. Petiveria alliacea and key phytochemical, dibenzyl trisulfide [8] and the Jamaican ball moss (Tillandsia recurvata L.) [9] exemplifies use in prostate cancer, among other biodiversity with disparate cytotoxic properties [10]. A recent survey among cancer patients in the country [11] helped identify common ethnomedical practices in the island nation and Annona muricata L. emerged as a popular ingredient, in line with findings emerging from Indonesia, [12] and Trinidad [13]. ...
Background
Annona muricata L. was identified as a popular medicinal plant in treatment regimens among cancer patients in Jamaica by a previously conducted structured questionnaire. Ethnomedically used plant parts, were examined in this study against human prostate cancer cells for the first time and mechanisms of action elucidated for the most potent of them, along with the active phytochemical, annonacin.
Methods
Nine extracts of varying polarity from the leaves and bark of A. muricata were assessed initially for cytotoxicity using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay on PC-3 prostate cancer cells and the ethyl acetate bark (EAB) extract was identified as the most potent. EAB extract was then standardized for annonacin content using High-performance Liquid Chromatography - Mass Spectrometry (HPLC-MS) and shown to be effective against a second prostate cancer cell line (DU-145) also. The mode of cell death in DU-145 cells were assessed via several apoptotic assays including induction of increased reactive oxygen species (ROS) production, reduction of mitochondrial membrane potential, activation of caspases and annexin V externalization combined with morphological observations using confocal microscopy. In addition, the potential to prevent metastasis was examined via inhibition of cell migration, vascular endothelial growth factor (VEGF) and angiogenesis using the chorioallantoic membrane assay (CAM).
Results
Annonacin and EAB extract displayed selective and potent cytotoxicity against the DU-145 prostate carcinoma cells with IC50 values of 0.1 ± 0.07 μM and 55.501 ± 0.55 μg/mL respectively, without impacting RWPE-1 normal prostate cells, in stark contrast to chemotherapeutic docetaxel which lacked such selectivity. Docetaxel’s impact on the cancerous DU-145 was improved by 50% when used in combination with EAB extract. Insignificant levels of intracellular ROS content, depolarization of mitochondrial membrane, Caspase 3/7 activation, annexin V content, along with stained morphological evaluations, pointed to a non-apoptotic mode of cell death. The extract at 50 μg/mL deterred cell migration in the wound-healing assay, while inhibition of angiogenesis was displayed in the CAM and VEGF inhibition assays for both EAB (100 μg /mL) and annonacin (0.5 μM).
Conclusions
Taken together, the standardized EAB extract and annonacin appear to induce selective and potent cell death via a necrotic pathway in DU-145 cells, while also preventing cell migration and angiogenesis, which warrant further examinations for mechanistic insights and validity in-vivo.
... The molecules in T. buseri, β-sitosterol, 4methylcholesterol, and lanosterol, showed utility as biomarkers for the reconstruction of vegetation in the past (Jansen et al., 2007). More recently, Lowe et al. (2008Lowe et al. ( , 2012aLowe et al. ( , 2013bLowe et al. ( , 2014a reported T. recurvata organic extracts against leukemia and prostate cancer that is the sixth leading cause of death in men (Stennett & White 2013), conferring biological activity to the cycloartane triterpenes, to the phenolics compounds and the soyasaponin molecule (compounds 68-101). ...
Tillandsia L. genus comprises 649 species, with different uses at different times. T. usneoides L. uses are reported since the late-archaic and pre-Columbian cultures. In XIX-XX centuries, T. usneoides was used in some manufactured products, as polish and packing fruit. Tillandsia has a favorable reputation as medicine: for leucorrhea, rheumatism, ulcers, hemorrhoid treatment, as an anti-diabetic remedy, emetic, analgesic, purgative, contraceptive, antispasmodic and diuretic. Tillandsia chemical composition includes cycloartane triterpenes and hydroxy-flavonoids, which are present in at least 24 species. Several extracts and compounds from Tillandsia spp. have been reported with pharmacological actions, as anti-neoplasia, hypolipidemic, antifungal, anti-HSV-1, hypoglycemic and microbicide. This review communicates the economic importance, ethnobotany, chemistry composition and biological activities of the Tillandsia genus, and analyze its biological and economic perspective. Tillandsia genus has cultural, economic and pharmacological relevance, with a high potential in many essential aspects of the modern society. Resumen: El género Tillandsia L. comprende 649 especies, con diferentes usos en diferentes épocas. T. usneoides L. se han reportado desde el arcáico tardío hasta las culturas precolombinas. En los siglos XIX-XX, T. usneoides se usó en productos manufacturados: como abrasivo y embalaje de fruta. Como medicina tradicional, el género Tillandsia se reporta para leucorrea, reumatismo, úlceras, hemorroides, remedio antidiabético, emético, analgésico, purgante, anticonceptivo, antiespasmódico y diurético. Su composición química incluye triterpenos de tipo ciclo-artano e hidroxi-flavonoides, presentes en al menos 24 especies. Los extractos y compuestos del género Tillandsia se han reportado con propiedades antineoplásicas, hipolipidémicas, antifúngicas, anti-HSV-1, hipoglucemiantes y microbicidas. Esta revisión comunica la importancia económica, etnobotánica, composición química y las actividades biológicas del género Tillandsia, y analiza su perspectiva biológica y potencial económica. Tillandsia tiene importancia cultural, económica y farmacológica, con gran potencial en muchos aspectos esenciales de la sociedad moderna.
... Es importante destacar que T. recurvata tiene promisorias aplicaciones médicas en el campo de la oncología (Lowe et al., 2012(Lowe et al., , 2013(Lowe et al., , 2014(Lowe et al., , 2017. Es también una planta que puede ser utilizada como bioindicadora de polución ambiental (Graciano et al., 2003;Zambrano García et al., 2009;Bermúdez & Pignata, 2011). ...
Introducción y objetivos: la distribución geográfica de Tillandsia recurvata (L.) L. abarca desde el sur de Estados Unidos hasta el centro de la República Argentina. El objetivo de este trabajo es reportar la presencia de esta especie 200 km al sur de su distribución conocida y discutir las causas que puedan haber conducido a esta expansión de rango.
M&M: Se colectaron especímenes en diferentes localidades de la provincia de
Buenos Aires. Se analizaron colecciones de herbario, bases de datos on-line y
bibliografía para corroborar la identificación taxonómica y el límite de distribución de la especie.
Resultados: Se presentan registros novedosos de Tillandsia recurvata (L.) L. que amplían su distribución geográfica 200 km hacia el Sur, siendo la localidad de Tandil el sitio más austral de ocurrencia.
Discusión: Debido a que las fechas de colecta y observaciones son recientes,
consideramos que este avance ocurrió en las últimas décadas. Se discuten las
posibles causas, como el cambio climático y la lignificación de las Pampas.
... The cellular response to most chemotherapeutic agents is generally low and is associated with high cell resistance, mainly when diagnosed at an advanced stage [3,[5][6][7]14]. In this context, the search for natural products for the prevention and treatment of cancer has grown considerably, since some molecules extracted from these compounds have shown anti-inflammatory, proapoptotic, and antiangiogenic effects [1,11,15]. In this review, the main compounds found were phenolic compounds, mainly flavonoids, phenolic acids, and tannins, followed by terpenes, alkaloids, curcumin, and saponins. ...
Melanoma is the most aggressive form of skin cancer and arises from melanocyte gene mutation. This disease is multifactorial, but its main cause is the excessive exposure to ultraviolet radiation. Currently, available chemotherapy has shown little expressive results, which may justify the high use of natural products to treat this cancer. We performed a systematic review to compile the results of studies carried out in murine models and investigated the effect of plant extracts on melanoma treatment. Papers were selected in MEDLINE/Pubmed and Scopus according to the PRISM statement. Search filters were developed using three parameters: plant extract, melanoma, and animal model. The 35 identified studies were all submitted to the criteria described in the ARRIVE guidelines. The different extracts showed antiangiogenic, antimetastatic, antioxidant, and anti-inflammatory activity, and also proved to be effective in cell cycle modulation and apoptosis evasion. Bias analysis evidenced the absence of standardized experimental designs, as well as failures in statistical tests and in the presentation of results. The analysis of the studies suggests that the use of plant extracts is effective for the treatment of melanoma in murine models.
... Previous studies by our group found T. recurvata to be having various chemical constituents including terpenoids and flavonoids [12,13]. Screening of the extracts of T. recurvata also revealed that the plant possesses several pharmacological properties including, anticancer activity [14,15]. Some of the specific compounds previously isolated from the plant includes cycloartanes, cinnamoyl diccinamates and phenolic compounds [12,13,15]. ...
Background
The incidence and mortalities from cancers remain on the rise worldwide. Despite significant efforts to discover and develop novel anticancer agents, many cancers remain in the unmet need category. As such, efforts to discover and develop new and more effective and less toxic agents against cancer remain a top global priority. Our drug discovery approach is natural products based with a focus on plants. Tillandsia recurvata (L.) L. is one of the plants selected by our research team for further studies based on previous bioactivity findings on the anticancer activity of this plant. Methods
The plant biomass was extracted using supercritical fluid extraction technology with CO2 as the mobile phase. Bioactivity guided isolation was achieved by use of chromatographic technics combined with anti-proliferative assays to determine the active fraction and subsequently the pure compound. Following in house screening, the identified molecule was submitted to the US National Cancer Institute for screening on the NCI60 cell line panel using standard protocols. Effect of HLBT-100 on apoptosis, caspase 3/7, cell cycle and DNA fragmentation were assessed using standard protocols. Antiangiogenic activity was carried out using the ex vivo rat aortic ring assay. ResultsA flavonoid of the flavanone class was isolated from T. recurvata (L.) L. with potent anticancer activity. The molecule was code named as HLBT-100 (also referred to as HLBT-001). The compound inhibited brain cancer (U87 MG), breast cancer (MDA-MB231), leukemia (MV4-11), melanoma (A375), and neuroblastoma (IMR-32) with IC50 concentrations of 0.054, 0.030, 0.024, 0.003 and 0.05 µM, respectively. The molecule also exhibited broad anticancer activity in the NCI60 panel inhibiting especially hematological, colon, CNS, melanoma, ovarian, breast and prostate cancers. Twenty-three of the NCI60 cell lines were inhibited with GI50 values <0.100 µM. In terms of potential mechanisms of action, the molecule demonstrated effect on the cell cycle as evidenced by the accumulation of cells with <G1 DNA content, activation of caspase 3/7, DNA fragmentation and culminating in apoptotic cell death. HLBT-100 also demonstrated antiangiogenic potential by inhibiting capillary sprout and tube formation in a dose dependent manner in the ex vivo rat aortic ring. Conclusion
This paper describes for the first time the anticancer activity of HLBT-100 isolated from T. recurvate (L.) L. The broad and selective anticancer activity of HLBT-100 as evidenced by its potent activity against IMR-32, CNS cancer cell line while not active against neuro-2a, a normal CNS cell line. The activity demonstrated by HLBT-100 in these studies makes the molecule a potential candidate for further development targeting especially those cancers that remain in the unmet need category such as glioblastoma multiforme and acute myeloid leukemia in addition to other cancers.
... The michellamine series of alkaloids, derivatives of betulinic acid and other classes of natural products are amongst some of the molecules isolated from plants with anti HIV activity [8][9][10]. Jamaica is endowed with several medicinal plant species and is credited for being the source of the Catharanthus roseus plant which yielded vinca alkaloids that were later developed for the treatment of leukemia [11,12].Our research has recently identified a number of Jamaican plants with varying degrees of both anticancer and anti-HIV activity [13,14]. ...
... Respecto de este tipo de neoplasias, el trabajo de Suarez et al. [36], demostró la actividad antitumoral del extracto etanólico de bejuco peruano (Bomarea cornigera) contra sarcoma T180 de modelo murino, lo que lo posiciona como promisorio en el trabajo contra este agresivo tipo de cáncer. Se suma a esto el estudio realizado con bromelia (Tillandsia recurvata) sobre sarcoma de Kaposi, cuya inhibición fue sobre 75% [37], entre otras neoplasias estudiadas. ...
Resumen
El cáncer es una de las pandemias más relevantes. Existe una clara predominancia de esta patología con características epidemiológicas entre países en vías de desarrollo y países desarrollados. Es necesario diseñar estrategias de tratamiento y profilaxis efectivas, de bajo costo y mínimos efectos secundarios. El presente trabajo se enfoca en una breve revisión de las investigaciones que han dado luz del gran potencial que albergan las plantas, destacando aquellas realizadas en y con plantas de Latinoamérica considerando que es un universo de estudio aún incipiente. La gran batería de compuestos orgánicos y otras sustancias como proteínas indican que siguen siendo una alternativa confiable en la búsqueda de nuevos actores en la batalla contra el cáncer.
... In vitro research conducted in our lab showed that a crude chloroform extract of the Jamaican ball moss was cytotoxic against five human cancer cell lines; A375 (melanoma), BC (breast), DU-124 (prostate), MCF-7 (breast) and PC-3 (prostate cancer), [32]. Additionally, more recent studies have showed that the methanol extracts were cytotoxic against five histogenic cancer cell lines; PC-3 (prostate), MCF-7 (breast), Kaposi sarcoma, B-16 melanoma and a B-cell lymphoma from a transgenic mouse strain with IC50s > µg/ml with apoptotic mechanistic cell viability reduction [33]. ...
Plants are an everlasting inspiration source of biologically active compounds. Among these medicinal plants, the biological activity of extracts from some species of the Tillandsia genus has been studied, but the phytochemistry of the hardy species Tillandsia bergeri remains unknown. The aim of the present study was to perform the first phytochemical study of T. bergeri and to identify the compounds responsible for the antibacterial activity of T. bergeri extracts. Soxhlet extraction of predried and grinded leaves was first performed using four increasing polarity solvents. A bio-guided fractionation was performed using agar overlay bioautography as a screening method against 12 Gram-positive, Gram-negative, sensitive, and resistant bacterial strains. The results showed the inhibition of Gram-positive methicillin-sensitive Staphylococcus aureus ATCC 29213 (MSSA), methicillin-resistant S. aureus N-SARM-1 (MRSA), and Staphylococcus caprae ATCC 35538 by the dichloromethane fraction. A phytochemical investigation led to the isolation and identification by high-resolution mass spectrometry and nuclear magnetic resonance of the two flavones penduletin and viscosine, responsible for this antibacterial activity. For viscosine, the minimum inhibitory concentration (MIC) value is equal to 128 μg/mL against MSSA and is equal to 256 μg/mL against MRSA and S. caprae. The combination of these compounds with vancomycin and cloxacillin showed a decrease in MICs of the antibiotics. Penduletin showed synergistic activity when combined with vancomycin against MSSA (FICI < 0.258) and S. caprae (FICI < 0.5). Thus, unexplored Tillandsia species may represent a valuable source for potential antibiotics and adjuvants.
The present work explores the use of weed extracts and purified compounds as environmentally friendly antifouling additives with a possible application in marine paints. Two species were selected as case studies: Verbena bonariensis L., Verbenaceae, and Tillandsia tenuifolia L., Bromeliaceae. The extracts of both species showed promising antifouling activity in laboratory experiments (byssal thread formation of the mussel Mytilus edulis) and also in field assays by incorporation to soluble-matrix paints, which were used to coat acrylic tiles that were submerged in the sea for a period of 45 days. In the case of the Verbena extract, it was not possible to identify a major bioactive component, and aralidioside, the main iridoid, did not show antifouling activity. However, in the case of the Tillandsia extract, the main component, which was isolated and identified as cycloartenone, displayed potent antifouling activity in laboratory and field assays. Since both species have high growth rates, these results may help overcome the sustainability issues of the use of natural products as antifoulants. At the same time, the technological use of these untapped biological resources may offer a new possibility for weed management.Graphical abstract
Several medicinal plants are traditionally used in different regions of Africa for the treatment of male infertility, sexual asthenia, erectile dysfunction, and impotency or used as an aphrodisiac. Scientific studies, mostly conducted in vitro or in animals, have proven the acclaimed traditional use of these plants to enhance sexual activities or sperm concentration, motility, and viability. Some of the mechanisms of actions associated with these plants include increased level of testosterone and the relaxation of the smooth cavernosal muscles. However, some plants were also shown to have detrimental effects on the male reproductive system. This may be due to the varying modes of plant extraction, duration of treatment, experimental design, dosage used, quality of the plant, or toxic effects. There is a need to standardize the protocols as well as to better understand the mechanism of actions of the respective plants. Further studies should be conducted using human subjects.
Plants Used for Reproductive Health by Nahua Women in Northern Veracruz, Mexico. This paper reports the use of medicinal plants by Nahua women in the state of Veracruz, Mexico. It documents the women’s
plant knowledge for reproductive purposes, which includes uses such as conception, pregnancy, birth, contraception, menstruation,
post-partum, and general reproductive health. The concept of equilibrium is very important in regaining health among the Nahua;
consequently, many of the medicinal plants have this as their primary purpose. The introduction of biomedical clinics and
hospitals in the region has had a significant effect on the loss of knowledge about medicinal plants. Additionally, the midwives
are not taking any new apprentices and laywomen are not passing on their knowledge to future generations. This generational
gap contributes to the loss of knowledge about medicinal plants. This research contributes to the study of indigenous ethnobotany
by (a) creating a record of the plant knowledge possessed by indigenous women, (b) giving voice to some of their health concerns,
(c) indicating how the introduction of biomedicine has affected their plant use, and (d) providing a framework for understanding
how marginal peoples around the world respond to the impact that globalization and change has on their health needs and local
ethnobotanical knowledge.
For more than 50 yr, natural products have served us well in combating infectious bacteria and fungi. During the 20th century,
microbial and plant secondary metabolites helped to double our life span, reduced pain and suffering, and revolutionized medicine.
The increased development of resistance to older antibacterial, antifungal, and antitumor drugs has been challenged by (1) newly discovered antibiotics (e.g., candins, epothilones); (2) new semisynthetic versions of old antibiotics (e.g., ketolides, glycylcyclines); (3) older underutilized antibiotics (e.g., teicoplainin); and (4) new derivatives of previously undeveloped narrow-spectrum antibiotics (e.g., streptogramins). In addition, many antibiotics
are used commercially, or are potentially useful in medicine for purposes other than their antimicrobial action. They are
used as antitumor agents, enzyme inhibitors including powerful hypocholesterolemic agents, immunosuppressive agents, antimigraine
agents, and so on. A number of these products were first discovered as antibiotics that failed in their development as such,
or as mycotoxins.
Natural products and their derivatives have historically been invaluable as a source of therapeutic agents. However, in the past decade, research into natural products in the pharmaceutical industry has declined, owing to issues such as the lack of compatibility of traditional natural-product extract libraries with high-throughput screening. However, as discussed in this review, recent technological advances that help to address these issues, coupled with unrealized expectations from current lead-generation strategies, have led to a renewed interest in natural products in drug discovery.
Natural product compounds are the source of numerous therapeutic agents. Recent progress to discover drugs from natural product sources has resulted in compounds that are being developed to treat cancer, resistant bacteria and viruses and immunosuppressive disorders. Many of these compounds were discovered by applying recent advances in understanding the genetics of secondary metabolism in actinomycetes, exploring the marine environment and applying new screening technologies. In many instances, the discovery of a novel natural product serves as a tool to better understand targets and pathways in the disease process. This review describes recent progress in drug discovery from natural sources including several examples of compounds that inhibit novel drug targets.
The CHCl3 extract of Tillandsia recurvata yielded 5,3′-dihydroxy-6,7,8,4′-tetramethoxyflavanone (1), 1,3-di-O-cinnamoyl-glycerol (2) and ethyl ester of caffeic acid. Their structures were elucidated by means of spectroscopic methods such as mass spectroscopy and 1 and 2D-NMR.
25-Hydroperoxycycloart-23-en-3 beta-ol [1] and an epimeric mixture of 24-hydroperoxpcycloart-25-en-3 beta-ol [2] have been isolated from Tillandsia recurvata. The structures of compounds 1 and 2 have been established by spectral analysis and chemical conversion co the corresponding diols.
Plant-derived compounds have played an important role in the development of several clinically useful anti-cancer agents. These include vinblastine, vincristine, the camptothecin derivatives, topotecan and irinotecan, etoposide, and paclitaxel (Taxol®). Several promising new agents are in clinical development based on selective activity against cancer-related molecular targets, including flavopiridol and Combretastatin A4 phosphate. Recently, plants have yielded several agents showing anti-AIDS activity, and one of these, (+)-calanolide A, is in clinical development.
The medicinal use of natural products—compounds that are derived from natural sources such as plants, animals or micro‐organisms—precedes recorded human history probably by thousands of years. Palaeoanthropological studies at the cave site of Shanidar, located in the Zagros Mountains of Kurdistan in Iraq, have suggested that more than 60,000 years ago, Neanderthals might have been aware of the medicinal properties of various plants, as evidenced by pollen deposits in one of the graves at the site (Solecki, 1975). Over the ensuing millennia, humankind discovered and made use of an enormous range of natural compounds; the latest version of the Dictionary of Natural Products (DNP; http://dnp.chemnetbase.com) has just over 214,000 entries.
Throughout our evolution, the importance of natural products for medicine and health has been enormous. Since our earliest ancestors chewed on certain herbs to relieve pain, or wrapped leaves around wounds to improve healing, natural products have often been the sole means to treat diseases and injuries. In fact, it has only been during the past decades that natural products have taken a secondary role in drug discovery and drug development, after the advent of molecular biology and combinatorial chemistry made possible the rational design of chemical compounds to target specific molecules. The past few years, however, have seen a renewed interest in the use of natural compounds and, more importantly, their role as a basis for drug development. The modern tools of chemistry and biology—in particular, the various ‘‐omics’ technologies—now allow scientists to detail the exact nature of the biological effects of natural compounds on the human body, as well as to uncover possible synergies, which holds much promise for the development of new therapies against many devastating diseases, including dementia and cancer.
> …Throughout our evolution, the importance of natural products for medicine and health has been enormous
Owing …
Natural products have been the single most productive source of leads for the development of drugs. Over a 100 new products are in clinical development, particularly as anti-cancer agents and anti-infectives. Application of molecular biological techniques is increasing the availability of novel compounds that can be conveniently produced in bacteria or yeasts, and combinatorial chemistry approaches are being based on natural product scaffolds to create screening libraries that closely resemble drug-like compounds. Various screening approaches are being developed to improve the ease with which natural products can be used in drug discovery campaigns, and data mining and virtual screening techniques are also being applied to databases of natural products. It is hoped that the more efficient and effective application of natural products will improve the drug discovery process.
Bioactivity-directed fractionation, using brine shrimp lethality and murine hypoglycemia, of an ethanol extract prepared from Tillandsia usneoides, led to the isolation of four apparently bioactive compounds from the water-soluble fraction. The compounds were identified as citric acid, succinic acid, 3-hydroxy-3-methylglutaric acid (HMG), and 3,6,3',5'-tetramethoxy-5,7,4'-trihydroxyflavone-7-O-beta-D-g lucoside. The brine shrimp lethality of the acids was simply due to acidity; however, HMG elicited significant hypoglycemic responses in fasting normal mice. Ethyl and methyl esters of citric acid were prepared and tested in the murine hypoglycemic assay. Five of the predominant sugars were identified by tlc. Free thymidine was also isolated. Further evaluation of HMG and other potential inhibitors of HMG CoA lyase, in the treatment of symptoms of diabetes mellitus, is suggested.
A hemocytometer-based trypan blue dye exclusion cell quantitation and viability assay was compared with a similar assay using simultaneous fluorometric staining with fluorescein diacetate and propidium iodide. Viable and nonviable cell densities were measured, and culture viability was calculated both during the normal growth cycle of a murine hybridoma and in response to the application of millimolar concentrations of either tert-butyl hydroperoxide or ferrous iron. During the early phase of rapid hybridoma cell growth, assay-based differences in viable cell density were not significant. As the culture aged, the trypan blue dye exclusion assay significantly overestimated cell viability, thereby underestimating nonviable cell density and yielding an erroneous estimation of the overall viability of the culture. Because of its lack of ambiguity in the identification of stained, nonviable cells and its resulting increased accuracy in the estimation of culture viability, the fluorometric assay was considered a better choice for the evaluation of cell viability.
Targeting apoptotic cell death pathways provides wide-ranging opportunities for the discovery and development of novel drugs. Some targeted therapies that selectively induce apoptosis in cancer cells are already marketed, and numerous pro-apoptotic drugs for treating cancer are currently being developed. The anti-apoptotic drugs that are most advanced in development are targeting acute disease indications such as stroke, myocardial infarction and sepsis, in which the role of apoptosis has been best defined and inhibitors of the apoptotic pathway have shown activity in various animal models. In the future, novel drugs might also result from an understanding of apoptotic pathways in chronic disorders.
We present the results of an ethnopharmacological research within a Bolivian lowland ethnic group from the dry Chaco, the izoceño-guaraní. Izoceño-guaraní people belong to the extended Chiriguano group. They are actually organised in independent communities, settled down in south-east Bolivia. Struggling very soon for their rights, landowners of their territory, izoceño-guaraní appear to be well organised and maintain a still vivid culture. Medicine is in the hands of Paye who are recognised as specialists in their own group. Ethnopharmacological research leads us to collect approximately over 306 species, 189 of them having medicinal uses. We present here an overview of the izoceño-guaraní ethnomedicine and pharmacopoeia, based on vegetal and animal products.
The CHCl3 extract of Tillandsia recurvata yielded 5,3'-dihydroxy-6,7,8,4'-tetramethoxyflavanone (1), 1,3-di-O-cinnamoyl-glycerol (2) and ethyl ester of caffeic acid. Their structures were elucidated by means of spectroscopic methods such as mass spectroscopy and 1 and 2D-NMR.
Plant-derived compounds have been an important source of several clinically useful anti-cancer agents. These include vinblastine, vincristine, the camptothecin derivatives, topotecan and irinotecan, etoposide, derived from epipodophyllotoxin, and paclitaxel (taxol A number of promising new agents are in clinical development based on selective activity against cancer-related molecular targets, including flavopiridol and combretastin A4 phosphate, while some agents which failed in earlier clinical studies are stimulating renewed interest.
Bacterial intercellular communication, or quorum sensing (QS), controls the pathogenesis of many medically important organisms. Anti-QS compounds are known to exist in marine algae and have the ability to attenuate bacterial pathogenicity. We hypothesized that terrestrial plants traditionally used as medicines may also produce anti-QS compounds. To test this hypothesis, 50 medicinal plants from southern Florida were screened for anti-QS activity using two biomonitor strains, Chromobacterium violaceum and Agrobacterium tumefaciens. Of these plants, six showed QS inhibition: Conocarpus erectus L. (Combretaceae), Chamaecyce hypericifolia (L.) Millsp. (Euphorbiaceae), Callistemon viminalis (Sol. ex Gaertn.) G. Don (Myrtaceae), Bucida burceras L. (Combretaceae), Tetrazygia bicolor (Mill.) Cogn. (Melastomataceae), and Quercus virginiana Mill. (Fagaceae). This study introduces not only a new mode of action and possible validation for traditional plant use, but also a potentially new therapeutic direction for the treatment of bacterial infections.
A survey of the medicinal and poisonous plant diversity in the flora of the Carirí of the State of Paraíba, Brazil, has been made. Medicinal and poisonous properties of 121 plant species belonging to 96 genera and 45 families were recorded. Of these, 119 species belonging 44 families, representing about 98% of the total, are used for medicinal purposes, and five species are considered as poisonous. The Fabaceae (Leguminosae) family has the highest number (16) of medicinal plants diversity in the area, followed by 11 species of Asteraceae and 9 of Solanaceae. Information on these 121 species are presented together with their medicinal uses. This study aims at emphasizing the importance of setting up conservation priorities, and sustained development of various medicinal plants of semi-arid area of Northeast of Brazil.
During the past 15 years, most large pharmaceutical companies have decreased the screening of natural products for drug discovery in favor of synthetic compound libraries. Main reasons for this include the incompatibility of natural product libraries with high-throughput screening and the marginal improvement in core technologies for natural product screening in the late 1980s and early 1990 s. Recently, the development of new technologies has revolutionized the screening of natural products. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. Examples of these new advances and technologies are described in this review.
The biology of the bromeliads
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Anti-tumour and anti-inflammatory extracts of plant biomass and their uses
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