Showing papers in "Medicines in 2015"
TL;DR: Evidence is provided that many plant secondary metabolites have a broad spectrum of bioactivities, which can explain the medical application of complex extracts from medicinal plants for more health disorders which involve several targets.
Abstract: Plants produce a wide diversity of secondary metabolites (SM) which serve them as defense compounds against herbivores, and other plants and microbes, but also as signal compounds. In general, SM exhibit a wide array of biological and pharmacological properties. Because of this, some plants or products isolated from them have been and are still used to treat infections, health disorders or diseases. This review provides evidence that many SM have a broad spectrum of bioactivities. They often interact with the main targets in cells, such as proteins, biomembranes or nucleic acids. Whereas some SM appear to have been optimized on a few molecular targets, such as alkaloids on receptors of neurotransmitters, others (such as phenolics and terpenoids) are less specific and attack a multitude of proteins by building hydrogen, hydrophobic and ionic bonds, thus modulating their 3D structures and in consequence their bioactivities. The main modes of action are described for the major groups of common plant secondary metabolites. The multitarget activities of many SM can explain the medical application of complex extracts from medicinal plants for more health disorders which involve several targets. Herbal medicine is not a placebo medicine but a rational medicine, and for several of them clinical trials have shown efficacy.
557 citations
TL;DR: Exosomes are powerful progenitors in altering target cell phenotypes, particularly in tumorigenesis and cancer progression, with the ability to alter tumor microenvironments and to assist in establishing the pre-metastatic niche.
Abstract: Exosomes are membrane-bound, intercellular communication shuttles that are defined by their endocytic origin and size range of 30-140 nm. Secreted by nearly all mammalian cell types and present in myriad bodily fluids, exosomes confer messages between cells, proximal and distal, by transporting biofunctional cargo in the form of proteins, nucleic acids, and lipids. They play a vital role in cellular signaling in both normal physiology and disease states, particularly cancer. Exosomes are powerful progenitors in altering target cell phenotypes, particularly in tumorigenesis and cancer progression, with the ability to alter tumor microenvironments and to assist in establishing the pre-metastatic niche. Many aspects of exosomes present them as novel means to identify cancer biomarkers for early detection and therapeutic targets, and using intrinsic and engineered characteristics of exosomes as therapeutic devices to ameliorate the progression of the disease. This review outlines some of the recent and major findings with regard to exosomes in cancer, and their utilization as therapeutic tools.
82 citations
TL;DR: To increase the usefulness and lower the health risk of Panax ginseng to customers, clinical trials on a larger scale and with a higher standard are necessary to define its efficacy and safety as a dietary supplement or complementary medicine.
Abstract: Background:Panax ginseng C.A. Meyer is one of the most frequently used herbs in the world. The roots of Panax ginseng have been used as a traditional tonic and medicine for thousands of years in Korea and China. Today, ginseng root is used as a dietary supplement and complementary medicine and for adjuvant therapeutics worldwide. The efficacy of ginseng has been studied in a wide range of basic research and clinical studies. However, it has been reported that the results from clinical studies are conflicting, and they depend on the parameters of the protocol design including the conditions of the participants and the types of ginseng used such as red ginseng, white ginseng, fermented ginseng and cultured ginseng. [...].
54 citations
TL;DR: Since the effects of dietary supplements on coagulation and platelet function are difficult to predict, it is prudent to advise their discontinuation before surgery.
Abstract: Background: Patients who undergo surgery appear to use dietary supplements significantly more frequently than the general population. Because they contain pharmacologically active compounds, dietary supplements may affect coagulation and platelet function during the perioperative period through direct effects, pharmacodynamic interactions, and pharmacokinetic interactions. However, in this regard, limited studies have been conducted that address the pharmacological interactions of dietary supplements. To avoid possible bleeding risks during surgery, information about the potential complications of dietary supplements during perioperative management is important for physicians. Methods: Through a systematic database search of all available years, articles were identified in this review if they included dietary supplements and coagulation/platelet function, while special attention was paid to studies published after 1990. Results: Safety concerns are reported in commercially available dietary supplements. Effects of the most commonly used natural products on blood coagulation and platelet function are systematically reviewed, including 11 herbal medicines (echinacea, ephedra, garlic, ginger, ginkgo, ginseng, green tea, kava, saw palmetto, St John’s wort, and valerian) and four other dietary supplements (coenzyme Q10, glucosamine and chondroitin sulfate, fish oil, and vitamins). Bleeding risks of garlic, ginkgo, ginseng, green tea, saw palmetto, St John’s wort, and fish oil are reported. Cardiovascular instability was observed with ephedra, ginseng, and kava. Pharmacodynamic and pharmacokinetic interactions between dietary supplements and drugs used in the perioperative period are discussed. Conclusions: To prevent potential problems associated with the use of dietary supplements, physicians should be familiar with the perioperative effects of commonly used dietary supplements. Since the effects of dietary supplements on coagulation and platelet function are difficult to predict, it is prudent to advise their discontinuation before surgery.
44 citations
TL;DR: The antimicrobial activities of A. cordifolia and C. subcordatum fruit essential oils are a function of their distinct chemical profiles; their volatiles and biological activities are reported for the first time.
Abstract: Bacterial resistance has been increasingly reported worldwide and is one of the major causes of failure in the treatment of infectious diseases. Natural-based products, including plant secondary metabolites (phytochemicals), can be exploited to ameliorate the problem of microbial resistance. The fruit essential oils of Alchornea cordifolia and Canthium subcordatum were obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC-MS). The essential oils were subjected to in vitro antibacterial, antifungal and cytotoxic activity screening. Thirty-eight compounds comprising 97.7% of A. cordifolia oil and forty-six constituents representing 98.2% of C. subcordatum oil were identified. The major components in A. cordifolia oil were methyl salicylate (25.3%), citronellol (21.4%), α-phellandrene (7.4%), terpinolene (5.7%) and 1,8-cineole (5.5%). Benzaldehyde (28.0%), β-caryophyllene (15.5%), (E,E)-α-farnesene (5.3%) and methyl salicylate (4.5%) were the quantitatively significant constituents in C. subcordatum fruit essential oil. A. cordifolia essential oil demonstrated potent in vitro antibacterial activity against Staphylococcus aureus (MIC = 78 μg/mL) and marginal antifungal activity against Aspergillus niger (MIC = 156 μg/mL). C. subcordatum showed antibacterial activity against Bacillus cereus and S. aureus (MIC = 156 μg/mL) and notable antifungal activity against A. niger (MIC = 39 μg/mL). However, no appreciable cytotoxic effects on human breast carcinoma cells (Hs 578T) and human prostate carcinoma cells (PC-3) were observed for either essential oil. The antimicrobial activities of A. cordifolia and C. subcordatum fruit essential oils are a function of their distinct chemical profiles; their volatiles and biological activities are reported for the first time.
44 citations
TL;DR: A survey of several aromatic plants used in traditional medicine in Yemen, their traditional uses, their volatile chemical compositions, and their biological activities are presented.
Abstract: Yemen is a small country located in the southwestern part of the Arabian Peninsula. Yemen's coastal lowlands, eastern plateau, and deserts give it a diverse topography, which along with climatic factors make it opulent in flora. Despite the introduction of Western medicinal system during the middle of the twentieth century, herbal medicine still plays an important role in Yemen. In this review, we present a survey of several aromatic plants used in traditional medicine in Yemen, their traditional uses, their volatile chemical compositions, and their biological activities.
43 citations
TL;DR: The present review provides the current understanding of the cancer chemopreventive pharmacology of sulforaphane towards its potential as an anticancer agent.
Abstract: The International Agency for Research on Cancer (IARC) in its latest World Cancer Report (2014) has projected the increase in the global cancer burden from 14 million (2012) to 22 million incidence annually within the next two decades. Such statistics warrant a collaborative engagement of conventional and complementary and alternative therapies to contain and manage cancer. In recent years, there has been a shift in the cancer chemoprevention paradigm with a significant focus turning towards bioactive components of human diets for their anticancer properties. Since diet is an integral part of lifestyle and given that an estimated one third of human cancers are believed to be preventable though appropriate lifestyle modification including dietary habits, the current shift in the conventional paradigm assumes significance. Several epidemiological studies have indicated that consumption of broccoli is associated with a lower risk of cancer incidence including breast, prostate, lung, stomach and colon cancer. The edible plant belonging to the family of cruciferae such as broccoli is a rich source of glucoraphanin, a precursor of isothiocyanate sulforaphane which is considered to be a potent anti-cancer agent. Plant-based dietary agents such as sulforaphane mimic chemotherapeutic drugs such as vorinostat, possessing histone deacetylase inhibition activity. Evidence from epidemiological and experimental studies have emerged, enhancing the clinical plausibility and translational value of sulforaphane in cancer chemoprevention. The present review provides the current understanding of the cancer chemopreventive pharmacology of sulforaphane towards its potential as an anticancer agent.
37 citations
TL;DR: The potential of various plant-derived compounds for reducing toxin production in foodborne and other microbes is discussed and studies highlighting their anti-toxigenic mechanism are discussed.
Abstract: Many pathogenic bacteria and fungi produce potentially lethal toxins that cause cytotoxicity or impaired cellular function either at the site of colonization or other locations in the body through receptor-mediated interactions. Various factors, including biotic and abiotic environments, competing microbes, and chemical cues affect toxin expression in these pathogens. Recent work suggests that several natural compounds can modulate toxin production in pathogenic microbes. However, studies explaining the mechanistic basis for their effect are scanty. This review discusses the potential of various plant-derived compounds for reducing toxin production in foodborne and other microbes. In addition, studies highlighting their anti-toxigenic mechanism(s) are discussed.
37 citations
TL;DR: Results support traditional claims for A. muricata and A. reticulata in the treatment of malaria given their limited cytotoxicity profile, and qualify as promising starting points for antimalarial drug discovery.
Abstract: The aim of this work was to screen extracts from Annona muricata and Annona reticulata in vitro against Plasmodium falciparum. Crude ethanolic extracts, methylene chloride fractions, aqueous fractions, subfractions and isolated compounds (stigmasterol-3-O-β-d-glucopyranoside, lichexanthone, gallic acid and β-sitosterol-3-O-β-d-glucopyranoside) were tested for cytotoxicity on erythrocytes and Human Foreskin Fibroblasts cells and against the W2 strain of P. falciparum in culture. Results indicated that none of the extracts was cytotoxic at concentrations up to 10 µg/mL. Most of the extracts, fractions and subfractions inhibited the growth of P. falciparum with IC50 values ranging from 0.07 to 3.46 µg/mL. The most potent was the subfraction 30 from A. muricata stem bark (IC50 = 0.07 µg/mL) with a selectivity index of ˃ 142. Subfraction 3 from A. muricata root also exhibited very good activity (IC50 = 0.09 µg/mL) with a high selectivity index (SI ˃ 111). Amongst the isolated compounds, only gallic acid showed activity with IC50 of 3.32 µg/mL and SI > 10. These results support traditional claims for A. muricata and A. reticulata in the treatment of malaria. Given their limited cytotoxicity profile, their extracts qualify as promising starting points for antimalarial drug discovery.
27 citations
TL;DR: Results from the screening of bio-guided fractionated extracts alone and combinations of Terminalia catappa, Terminalia mantaly and Monodora tenuifolia harvested in Cameroon support further investigation of medicinal plant Extracts alone and in combination as starting points for the development of alternative antifungal therapy.
Abstract: Mycoses caused by Candida and Cryptococcus species, associated with the advent of antifungal drug resistance have emerged as major health problems. Improved control measures and innovative therapies are needed. This paper describes results from the screening of bio-guided fractionated extracts alone and combinations of Terminalia catappa, Terminalia mantaly and Monodora tenuifolia harvested in Cameroon. Crude ethanolic, hydro-ethanolic and aqueous extracts and bio-guided fractions were screened for antifungal activity against isolates of C. albicans, C. glabrata, C. parapsilosis and Cr. neoformans and the reference strain C. albicans NR-29450. Minimal inhibitory concentrations (MIC) were determined using a broth micro dilution method according to the Clinical & Laboratory Standards Institute (CLSI). Time kill kinetics of extracts alone and in combination were also evaluated. Extracts from T. mantaly stem bark were the most active with the best MIC values ranging from 0.04 mg/mL to 0.16 mg/mL. Synergistic interactions were observed with combinations of sub-fractions from M. tenuifolia, T. mantaly and T. catappa. Combination of sub-fractions from M. tenuifolia and T. mantaly (C36/C12) showed synergistic interaction and fungicidal effect against four out of five tested yeasts. These results support further investigation of medicinal plant extracts alone and in combination as starting points for the development of alternative antifungal therapy.
26 citations
TL;DR: The ar-turmerone-rich leaf essential oil of C. longa from Nigeria has shown potent biological activity and therapeutic promise and has been revealed to be a new essential oil chemotype of C., longa.
Abstract: Curcuma longa (turmeric) has been used in Chinese traditional medicine and Ayurvedic medicine for many years. Methods: The leaf essential oil of C. longa from southern Nigeria was obtained by hydrodistillation and analyzed by gas chromatography–mass spectrometry (GC-MS). The essential oil was screened for in vitro antibacterial, antifungal, and cytotoxic activities. The major components in C. longa leaf oil were ar-turmerone (63.4%), α-turmerone (13.7%), and β-turmerone (12.6%). A cluster analysis has revealed this to be a new essential oil chemotype of C. longa. The leaf oil showed notable antibacterial activity to Bacillus cereus and Staphylococcus aureus, antifungal activity to Aspergillus niger, and cytotoxic activity to Hs 578T (breast tumor) and PC-3 (prostate tumor) cells. The ar-turmerone-rich leaf essential oil of C. longa from Nigeria has shown potent biological activity and therapeutic promise.
TL;DR: A summary of the uses of 18 aromatic medicinal plants from Tajikistan and their compositions of secondary metabolites is presented.
Abstract: Tajikistan is a small country located in Central Asia. The mostly mountainous terrain with a continental, subtropical, and semiarid climate, is characterized by diverse flora. Many people in Tajikistan rely on medicinal plants as their traditional form of medicine to prevent and cure health disorders. Aromatic medicinal plants, in particular, have played an important role for the local people. In this review, we present a summary of the uses of 18 aromatic medicinal plants from Tajikistan and their compositions of secondary metabolites.
TL;DR: The effects on CYPs and PXR indicate that vinpocetine may not affect CYP-mediated metabolism of drugs, as the inhibitory concentrations are much greater than the expected plasma concentrations in humans.
Abstract: Background: Vinpocetine, a semi-synthetic derivative of vincamine, is a popular dietary supplement used for the treatment of several central nervous system related disorders. Despite its wide use, no pharmacokinetic drug interaction studies are reported in the literature. Due to increasing use of dietary supplements in combination with conventional drugs, the risk of adverse effects is on the rise. As a preliminary step to predict a possibility of drug interaction during concomitant use of vinpocetine and conventional drugs, this study was carried out to evaluate the effects of vinpocetine on three main regulators of pharmacokinetic drug interactions namely, cytochromes P450 (CYPs), P-glycoprotein (P-gp), and Pregnane X receptor (PXR). Methods: Inhibition of CYPs was evaluated by employing recombinant enzymes. The inhibition of P-gp was determined by calcein-AM uptake method in transfected and wild type MDCKII cells. Modulation of PXR activity was monitored through a reporter gene assay in HepG2 cells. Results: Vinpocetine showed a strong inhibition of P-gp (EC50 8 µM) and a moderate inhibition of recombinant CYP3A4 and CYP2D6 (IC50 2.8 and 6.5 µM) with no activity towards CYP2C9, CYP2C19 and CYP1A2 enzymes. In HLM, competitive inhibition of CYP3A4 (IC50 54 and Ki 19 µM) and non-competitive inhibition of CYP2D6 (IC50 19 and Ki 26 µM) was observed. Activation of PXR was observed only at the highest tested concentration of vinpocetine (30 µM) while lower doses were ineffective. Conclusion: Strong inhibition of P-gp by vinpocetine is indicative of a possibility of drug interactions by altering the pharmacokinetics of drugs, which are the substrates of P-gp. However, the effects on CYPs and PXR indicate that vinpocetine may not affect CYP-mediated metabolism of drugs, as the inhibitory concentrations are much greater than the expected plasma concentrations in humans.
TL;DR: Results from a program that sought to develop such gamma secretase modulators based on novel natural products identified in the extract of Actaea racemosa, the well-known botanical black cohosh are summarized.
Abstract: Alzheimer's disease is characterized by pathogenic oligomerization, aggregation, and deposition of amyloid beta peptide (Aβ), resulting in severe neuronal toxicity and associated cognitive dysfunction. In particular, increases in the absolute or relative level of the major long form of Aβ, Aβ42, are associated with increased cellular toxicity and rapidity of disease progression. As a result of this observation, screening to identify potential drugs to reduce the level of Aβ42 have been undertaken by way of modulating the proteolytic activity of the gamma secretase complex without compromising its action on other essential substrates such as Notch. In this review we summarize results from a program that sought to develop such gamma secretase modulators based on novel natural products identified in the extract of Actaea racemosa, the well-known botanical black cohosh. Following isolation of compound 1 (SPI-014), an extensive medicinal chemistry effort was undertaken to define the SAR of 1 and related semisynthetic compounds. Major metabolic and physicochemical liabilities in 1 were overcome including replacement of both the sugar and acetate moieties with more stable alternatives that improved drug-like properties and resulted in development candidate 25 (SPI-1865). Unanticipated off-target adrenal toxicity, however, precluded advancement of this series of compounds into clinical development.
TL;DR: This will be the first attempt to explore the impact of mindfulness intervention on the adherence of a behavioral intervention, and the effectiveness of intermittent fasting on lowering blood pressure has not been supported by large-sample randomized controlled trials.
Abstract: Background: With the increasing availability of Smartphones and wearable tracking devices, it is now feasible and affordable to apply such mobile devices to delivering mindfulness-based stress reduction (MBSR) and intermittent fasting (IF) to lower blood pressure, as traditional MBSR and IF incur the burden of commuting to the intervention sites for the patients. Our study will develop and scientifically evaluate an MBSR app, an IF app and an MBSR + IF app in terms of their effectiveness for lowering blood pressure. We will further explore the possible interaction effect (synergistic effect) between MBSR and IF intervention: will improved mindfulness enhance patients' adherence to the IF protocol? Methods: We will develop an MBSR app, an IF app, and an MBSR+IF app. We will then conduct an 8-week randomized controlled trial with a factorial design to evaluate the efficacy of these new apps, especially the interaction effect between MBSR and IF. Eligible individuals will be randomly assigned to Group 1 (MBSR app), Group 2 (IF app), Group 3 (MBSR + IF app) or Group 4 (usual care). Discussion: This will be the first attempt to explore the impact of mindfulness intervention on the adherence of a behavioral intervention. Nevertheless, our protocol is limited in that the effectiveness of intermittent fasting on lowering blood pressure has not been supported by large-sample randomized controlled trials. Thus if there is no significant effectiveness we cannot determine whether it is due to the intermittent fasting intervention itself or it is due to the limit of smartphone as a vehicle.
TL;DR: Complementary and alternative medical treatments like acupuncture, moxibustion, and massage are becoming more and more attractive because of their effectiveness, fewer side effects, and reliable safety.
Abstract: Gastroparesis is a common gastrointestinal complication in diabetes, induced by hyperglycemia and characterized by delayed gastric emptying and upper abdominal symptoms, such asnausea, vomiting, early satiety, bloating and epigastric pain. Diabetic gastroparesis (DGP) affects life quality and glycemic control, and is a challenge to treat in both Western and Eastern medicine. Routine treatment in Western medicine includes gastric emptying promoted by prokinetic agents, gastric pacemaking, or surgery combined with lifetime hormono-therapy, all of which have unavoidable side effects and limitations, and are very expensive. Complementary and alternative medical treatments like acupuncture, moxibustion, and massage are becoming more and more attractive because of their effectiveness, fewer side effects, and reliable safety. This article aims to introduce representative methods of complementary and alternative medicine to treat DGP, which were searched in English through Pubmed and in Chinese through CNKI (China Knowledge Resource Integrated Database). Several lines of evidence demonstrated the effects of single or combined complementary alternative therapies on DGP outcomes; however, the mechanisms were rarely investigated. Randomized controlled trials are undoubtedly required in future studies.
TL;DR: It is strongly suggested that CAM education for women compromised by the disease and treatment associated with ovarian cancer would best be delivered in the convenient-access format that allowed remote access to live and recorded discussions of specific topics.
Abstract: The purpose of this pilot study was to assess the feasibility of on-site complementary and alternative medicine (CAM) education sessions to maximize quality of life for women with ovarian cancer. The pilot intervention consisted of four weekly sessions, each focusing the techniques and benefits of a particular CAM topic (e.g., nutrition, massage, relaxation). Participants were recruited from the Center for Women’s Oncology at H. Lee Moffitt Cancer Center from 2010 to 2012. Eligible participants had an ovarian cancer diagnosis with a life expectancy of at least 12 months, and were 18 years or older. The Gynecologic Oncology research nurse invited women in the outpatient clinic who matched the eligibility criteria. The research nurse explained the study and provided an informed consent form and return envelope. Because ovarian cancer is not only a rare cancer but, also, most patients seen at Moffitt have recurrent or advanced disease, many women did not have an adequate ECOG score. Many women who consented had rapid changes in health status, with morbidity and mortality outpacing recruitment of the 20 needed to proceed with the four education sessions. Baseline and follow-up surveys were conducted to assess changes in QOL, knowledge, and satisfaction with the intervention. While 27 women consented and 24 women completed the baseline survey, only five women participated in the intervention. The five women who participated were all white, and at time of consenting had a mean age of 60 (SD 9.08) and an average of 102 months (SD 120.65) since diagnosis, and were all on active treatment, except for one. The intervention pilot did not encounter difficulties with regard to recruitment, but suffered problems in achieving an adequate number of women to launch the on-site sessions because of rapidly changing morbidity and significant mortality. The team recognized that a larger-scaled intervention comprised of on-site sessions was impractical and compared attendance rates with a more convenient format currently underway in the Women’s Oncology program at Moffitt. While low participation prevented an intervention analysis of scientific merit, the study data is informative with regard to barriers, facilitators, and alternative methods for sharing useful information to women with advanced ovarian cancer. The comparison strongly suggested that CAM education for women compromised by the disease and treatment associated with ovarian cancer would best be delivered in the convenient-access format that allowed remote access to live and recorded discussions of specific topics.
TL;DR: In this chapter, acupuncture, manual therapy, and natural healing forLow back pain will be discussed, with special emphasis on the role of the individual in the control and prevention of low back pain.
Abstract: Low back pain may have complex patho-physiological causes leading to chronicity that resists conventional managements. Complementary and alternative treatment options have, therefore, gained popularity. In this chapter, acupuncture, manual therapy, and natural healing for low back pain will be discussed. Special emphasis is given on the role of the individual in the control and prevention of low back pain.
TL;DR: The increasing usage of state-of-art computational, molecular biological, and analytical chemistry techniques will promote the exploration of the pharmacological effect of previously inaccessible sources of herbal medicines and natural products.
Abstract: Herbal medicines and natural products have been the most productive source of drug development and there is a large line of evidence on the applications of herbal medicines and natural products for the management of body function and the treatment of aliments. The multiple bioactive components in herbal medicines and natural products can explain the multiple targets effect in their medical applications. The increasing usage of state-of-art computational, molecular biological, and analytical chemistry techniques will promote the exploration of the pharmacological effect of previously inaccessible sources of herbal medicines and natural products. Notably, with the increasing reports on the safety issues regarding the medical use of herbal medicines and natural products, the awareness of pharmacovigilance in herbal medicines and natural products needs to be strengthened. To prevent the adverse drug reactions related to herbal medicines and natural products, physicians need to be aware of potential risks and alert patients in the use of herbal medicines and natural products.
TL;DR: To ensure the efficacy of Western herbal products sold as health food in Japan, quality control, including disintegration, is recommended, even though these products are not regulated under the Pharmaceutical Affairs Law.
Abstract: For many years now, a number of Western herbs have been widely used in health food products in Japan and as pharmaceuticals in Europe. There are few or no mandated criteria concerning the quality of these herbal health food products, thus clarification is warranted. Here, we performed disintegration tests of 26 pharmaceutical and health food products containing the Western herbs ginkgo leaf and chaste tree fruit, in accord with the Japanese Pharmacopoeia. All eight pharmaceutical herbal products found in the European market completely disintegrated within the defined test time, and 11 of the 18 tested herbal products distributed as health foods in Japan disintegrated. Among the incompatible products identified in the Pharmacopoeia test, some products remained intact after incubation in water for 60 min. To ensure the efficacy of Western herbal products sold as health food in Japan, quality control, including disintegration, is therefore recommended, even though these products are not regulated under the Pharmaceutical Affairs Law.
TL;DR: The leaf essential oil of Montanoa guatemalensis, a small to medium-sized tree in the Asteraceae that grows in Central America from Mexico south through Costa Rica, showed selective in vitro cytotoxic activity to MDA-MB-231 cells and may be a good source of cyclocolorenone.
Abstract: Background: Montanoa guatemalensis is a small to medium-sized tree in the Asteraceae that grows in Central America from Mexico south through Costa Rica. There have been no previous investigations on the essential oil of this tree. Methods: The leaf essential oils of M. guatemalensis were obtained from different individual trees growing in Monteverde, Costa Rica, in two different years, and were analyzed by gas chromatography—mass spectrometry. Results: The leaf oils from 2008 were rich in sesquiterpenoids, dominated by α-selinene, β-selinene, and cyclocolorenone, with lesser amounts of the monoterpenes α-pinene and limonene. In contrast, the samples from 2009 showed no α- or β-selinene, but large concentrations of trans-muurola-4(14),5-diene, β-cadinene, and cyclocolorenone, along with greater concentrations of α-pinene and limonene. The leaf oils were screened for cytotoxic and antimicrobial activities and did show selective cytotoxic activity on MDA-MB-231 breast tumor cells. Conclusion: M. guatemalensis leaf oil, rich in cyclocolorenone, α-selinene, and β-selinene, showed selective in vitro cytotoxic activity to MDA-MB-231 cells. The plant may be a good source of cyclocolorenone.