Antimicrobial indole alkaloids from Tabernaemontana corymbosa / 中国天然药物

Four unreported monoterpene indole alkaloids, tabernaecorymines B-E (1-4), together with twenty-one known indole alkaloids (5-25) were obtained from the stem bark of Tabernaemontana corymbosa. Their structures and absolute configurations were elucidated by extensive spectroscopy, quantum chemical calculations, DP4+ probability analyses and Mo2(OAc)4-induced electronic circular dichroism experiment. The antibacterial and antifungal activities of these compounds were evaluated and some of them showed significant activity against Staphylococcus aureus,Bacillus subtilis, Streptococcus dysgalactiae and Candida albicans.

Preliminary evaluation of In vitro and In vivo antioxidative and antitumor activities of flavonoid extract of Tabernaemontana divaricata leaves in Ehrlich's lymphoma and Dalton's lymphoma ascites model

Aims: In the present study, the flavonoid fraction of Tabernaemontana divaricata flavonoid fraction(TdFf) leaves was investigated for its in vitro and in vivo antioxidative and antitumor activity. Subjects and Methods: The flavonoid fraction of ethyl acetate extract was assessed for their in vitro antioxidant activity by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), superoxide radicals, ferric reducing antioxidant power (FRAP), hydrogen peroxide, hydroxyl radicals and nitric oxide and in vivo antioxidative activity by enzymic and nonenzymic antioxidants in the liver of intraperitoneally implanted Ehrlich's lymphoma (EAC) and Dalton's lymphoma ascites (DLAs) model. The in vitro cytotoxicity was assessed using trypan blue exclusion assay and in vivo antitumor activity was assessed by screening the ILS, serum liver marker enzymes and histopathology of the liver. Statistical Analysis Used: The data were expressed as the mean ± standard deviation of the means, and statistical analysis was carried out employing one-way and two-way analysis of variance using Web Agri Stat Package 2.0. Results: The dose-dependent percentage scavenging of ABTS, DPPH, FRAP, OH, superoxide radical, and nonradical NO and H2O2 by TdFf indicated their antioxidative potential. Incubation of EAC/DLA tumor cells with TdFf showed a concentration-dependent cytotoxic effect, and the extract killed 50% of EAC/DLA tumor cells at a concentration of 80 μg of TdFf. Coadministration of TdFf with EAC/DLA-induced mice showed a significant increase in the liver enzymic and nonenzymic antioxidants and significant decrease in the serum liver marker enzymes to prove the in vivo antioxidative and antitumor activity of TdFf. It was also confirmed by the histopathology of the liver. Conclusions: It may be concluded that the flavonoid fractions of Td possess considerable antioxidative and antitumorigenic activity against the tested DLA/EAC in both in vitro and in vivo system"

Enzymatic and Non Enzymatic Antioxidant Activity of Tabernaemontana divaricate R.Br. against DEN and Fe-NTA Induced Renal Damage in Wistar Albino Rats.

Plant derived drugs have been a part of the evolution of human healthcare for thousands of years. The present study was carried out to evaluate the antioxidant potential of ethanolic extract of Tabernaemontana divaricata on DEN initiated and Fe-NTA promoted renal damage in rats. Fe-NTA was induced after 10 days of DEN (200mg/kg body weight) initiation at a dose level of 9mg Fe-NTA/kg body weight twice a week for one month. The biochemical parameters were analyzed in serum and the antioxidant assays were carried out in kidney. Lipid peroxidation level was increased due to the administration of Fe-NTA, which caused the reduction of enzymatic antioxidant such as SOD, GPx, Catalase, G6PD, and also the non-enzymatic antioxidants vitamin C and GSH. The levels of urea, uric acid, creatinine, blood urea nitrogen were increased and protein level decreased on Fe- NTA intoxication. The secondary metabolites present in the plant increased the synthesis of antioxidant enzymes and its free radical scavenging properties helped to scavenge all free radicals thereby decreasing lipid peroxidation. Thus, the present study indicates that the plant may clinically valuable agent in the prevention of renal failure caused by DEN and Fe-NTA intoxication.

Assessment of Thrombolytic Activity of Five Bangladeshi Medicinal Plants: Potential Source for Thrombolytic Compounds.

Aim: The aim of our project work was to assess the thrombolytic activity of five common Bangladeshi plant extract in different solvent. Five plants are Geodorum densiflorum (Shankhamul), Pistia stratiotes (Topa Pana), Smilax zeylanica (Kumarilata), Pandanus foetidus (Keya) & Tabernaemontana coronaria (Tagar). Plants were collected and air dried separately for three weeks. They were ground into a coarse powder. Cold extractions were performed for all plants by using different solvents. Place and Duration of Study: Department of Pharmacy, University of Chittagong and University of Science and Technology Chittagong, November, 2013. Methodology: Fresh blood was collected from healthy individuals ten volunteers (n=10). Blood was allowed to form clots in a pre-weighed sterile micro-centrifuge eppendorf tubes. After clot serum was removed and blood clot was weighed then blood clot was allowed to lysis by streptokinase. After lysis fluid was removed and the remaining of blood clot was again weighed along with the tube. Percentage of blood clot lysis was calculated on the basis of the weight difference. Weight difference of tubes obtained by weighing before and after clot lyses of blood. % clot lysis=(Weight after clot lysis/ Weight of clot before lysis)×100. This method was repeated for all extracts. Result: Among the herbs studied Pandanus foetidus (C), Pandanus foetidus (PE), Smilax zeylanica (E) and Pistia stratiotes-Root (M) showed significant % of clot lysis 47.54% 41.49%, 43.35% and 35.85% respectively with reference to standard, streptokinase (70.24%). Conclusion: These extracts lyse the blood clots In-vitro, however, we need to know In-vivo clot dissolving property. Further systemic research on these plants and may be a potential source of thrombolytic agent in future.

Effect of various extracts of Tabernaemontana divaricata on haloperidol induced catalepsy in rats.

Parkinson’s disease (PD) is one of the neurodegenerative diseases with selective loss of dopamine neurons of the substantia nigra pars compacta. In the present study, anti-cataleptic activity of Tabernaemontana divaricata leaves extracts viz. aqueous and ethanolic at different doses (50, 100 and 150 mg/kg i.p.) were studied using haloperidol (1 mg/kg, i.p.) induced catalepsy in rats which is a useful animal model for screening drugs for Parkinson’s disease. Both the extracts were found to reduce catalepsy significantly (P<0.001) as compared to the haloperidol treated rats showing greater effect at 150 mg/kg i.p. dose. Thus the present study reveals the anti-cataleptic activity of Tabernaemontana divaricata evaluating the traditional folklore medicinal use of the plant.

Effect of various extracts of Tabernaemontana divaricata on haloperidol induced catalepsy in rats.

Parkinson’s disease (PD) is one of the neurodegenerative diseases with selective loss of dopamine neurons of the substantia nigra pars compacta. In the present study, anti-cataleptic activity of Tabernaemontana divaricata leaves extracts viz. aqueous and ethanolic at different doses (50, 100 and 150 mg/kg i.p.) were studied using haloperidol (1 mg/kg, i.p.) induced catalepsy in rats which is a useful animal model for screening drugs for Parkinson’s disease. Both the extracts were found to reduce catalepsy significantly (P<0.001) as compared to the haloperidol treated rats showing greater effect at 150 mg/kg i.p. dose. Thus the present study reveals the anti-cataleptic activity of Tabernaemontana divaricata evaluating the traditional folklore medicinal use of the plant.

Anxiogenic effects of Tabernaemontana solanifolia A. DC. (Apocynaceae) extracts in rats tested in the elevated plus-maze / Determinación mediante la prueba del laberinto elevado en cruz del efecto ansiogénico en ratas de extractos de Tabernaemontana solanifolia A. DC. (Apocynaceae)

Introduction: Tabernaemontana solanifolia A. DC. (Apocynaceae) grows in the Cerrado (savanna), Caatinga (shrublands), and Atlantic Forest of Brazil. Objective: to investigate the potential anxiolytic activity of the crude extracts and ß-amyrin acetate obtained from the leaves of Tabernaemontana solanifolia in the elevated plus-maze (EPM) test for anxiety in rats. Methods: the crude extracts (aqueous, ethanol, and hexane), as well as ß-amyrin acetate, obtained from Tabernaemontana solanifolia leaves were evaluated for possible anxiolytic effects in rats tested in the elevated plus-maze. Acute toxicity in rats was determined by OECD 423 guidelines. The leaves of T. solanifolia specimens collected in Brasília, Brazil, were air dried at 40 °C and macerated with hexane or ethanol. After filtration, the solvents were removed under reduced pressure, yielding the crude hexane and ethanolic extracts (5.96 and 18.62 % yield, respectively). The crude aqueous extract was obtained by infusion, followed by lyophilization (13.5 % yield). Thirty minutes before the elevated plus-maze experiments, the animals were treated with the crude ethanol extract (1 000 mg/kg of body weight [bw], p.o.), the crude hexane extract (1 000 mg/kg bw, p.o.), the crude extract (1 000 mg/kg bw, p.o.), or ß-amyrin acetate (21 mg/kg bw, p.o.). Results: the extracts cauded no mortality up to 2 000 mg/kg, so half of DL50 doses were selected for the present study. The crude extracts (hexane, ethanolic and aqueous) (1.0 g/kg) as well as the substance ß-amyrin acetate (21 mg/kg) were administered once, increasing the number of entries into and the time spent in the closed arms of the elevated plus-maze. Conclusion: the oral administration of the extracts and ß-amyrin acetate obtained from Tabernaemontana solanifolia had an anxiogenic effect in rats. Further studies are needed in order to identify and characterize the anxiogenic properties of Tabernaemontana solanifolia and to understand the anxiogenic mechanisms of the extracts.

Introducción: Tabernaemontana solanifolia A. DC. (Apocynaceae) crece en el Cerrado (sabana), Caatinga (matorrales) y la Mata Atlántica de Brasil. Objetivo: investigar la posible actividad ansiolítica de los extractos crudos y el acetato de ß-amirina obtenidos de las hojas de Tabernaemontana solanifolia en la prueba del laberinto elevado en cruz (EPM) para la ansiedad en ratas. Métodos: los extractos crudos (etanol acuoso y hexano), así como el acetato de ß-amirina, se evaluaron para posibles efectos ansiolíticos en ratas mediante la prueba del laberinto elevado en cruz. La toxicidad aguda en ratas se determinó por las directrices OCDE 423. Las hojas de Tabernaemontana solanifolia se secaron al aire a 40 °C y fueron maceradas con hexano y etanol. Después de la filtración, los disolventes se eliminaron bajo presión reducida, produciendo los extractos crudos hexano y etanólico (5,96 y 18,62 % de rendimiento, respectivamente). El extracto acuoso bruto se obtuvo por infusión, seguida por liofilización (13,5 % de rendimiento). A 30 min antes de los experimentos de laberinto elevado en cruz, los animales se trataron con el extracto de etanol crudo (1 000 mg/kg de peso corporal [bw], p.o.), el extracto de hexano crudo (1 000 mg/kg de peso corporal, por vía oral), el extracto acuoso (1 000 mg/kg de peso corporal, por vía oral) o ß-amirina acetato (21 mg/kg de peso corporal, por vía oral). Resultados: los extractos no produjeron mortalidad hasta 2 000 mg/kg, por lo que para el presente estudio se seleccionó la mitad de la dosis DL50. Los extractos crudos (hexano, etanol y acuoso) (1 000 mg/kg), así como la sustancia acetato de ß-amirina (21 mg/kg) se administraron una vez, aumentando el número de entradas y el tiempo pasado en los brazos cerrados de la prueba del laberinto elevado en cruz. Conclusión: la administración oral de los extractos y el acetato de ß-amirina obtenidos de Tabernaemontana solanifolia tuvo un efecto ansiogénico en ratas. Se necesitan estudios adicionales para identificar y caracterizar las propiedades ansiogénicas de Tabernaemontana solanifolia y para entender los mecanismos ansiogénicos de los extractos.

In vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice / 中国天然药物

AIM@#To study the in vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.@*METHODS@#Aqueous decoction and methanol leaf extracts were tested for their ability to reduce croton oil-induced edema in the mouse ear after topical application. The methanol leaf extract dose-dependently inhibited the croton oil-induced ear edema in mice (ID50 <500 μg·cm(-2)). A bioassay-guided liquid-liquid fractionation of this methanol extract gave four active fractions: water insoluble (F1), hexane (F2), ethyl acetate (F3) and water (F4).@*RESULTS@#The hexane fraction showed a very high activity (42.1% inhibition at 0.7 μg·cm(-2)) as compared to the control. The other fractions were less active (F1: 56.1% at 506.2 μg·cm(-2); F3: 57.3% at 289.3 μg·cm(-2); and F4: 31.9% for 203.8 μg·cm(-2)) while indomethacin gave 48.8% of inhibition at 90 μg·cm(-2). The activity of F1 and F3 may be at least in part explained by the presence of anti-inflammatory flavonoids, while the activity was not correlated to the tannin contents. No compounds were detected in the most active F2 fraction.@*CONCLUSIONS@#The results give a rational support to the traditional use of T. divaricata in tropical India as anti-inflammatory agent.

Actividad larvicida de extractos etanólicos de Tabernaemontana cymosa y Trichilia hirta sobre larvas de estadio III y IV de Aedes aegypti (Diptera: Culicidae) / Larvicidal activity of ethanol extracts of Tabernaemontana cymosa and Trichilia hirta against III and IV stage larvae of Aedes aegypti (Diptera: Culicidae)

Introducción: el mosquito Aedes aegypti es el principal vector de los virus del dengue y la fiebre amarilla. Una de las formas actuales para combatir estas enfermedades es el control del vector. Sin embargo, los problemas causados por los insecticidas sintéticos y la resistencia adquirida por los mosquitos, hacen cada vez más difícil esta lucha. Las plantas constituyen una fuente alternativa al uso de insecticidas sintéticos. Objetivos: evaluar la actividad larvicida para el mosquito Aedes aegypti, de los extractos etanólicos y fracciones activas, de diferentes órganos vegetales de las especies Trichilia hirta L. y Tabernaemontana cymosa Jacq. Métodos: en este estudio se utilizaron larvas de Aedes aegypti en estadios III y IV. Los extractos etanólicos totales se obtuvieron por maceración del material vegetal seco y molido, durante una semana y posterior secado a presión reducida con un rotoevaporador. La obtención de fracciones y subfracciones, se realizó por cromatografía de columna abierta, usando solventes de diferentes polaridades. La actividad larvicida se evaluó bajo protocolos recomendados por la Organización Mundial de la Salud. Resultados: los extractos etanólicos de corteza de Trichilia hirta y flores, corteza y hojas de Tabernaemontana cymosa, no mostraron actividad larvicida. El extracto de semillas de Trichilia hirta mostró una actividad moderada con una CL50 y CL90 de 219,2 y 331,4 mg/L respectivamente. El extracto etanólico de semillas de Tabernaemontana cymosa, la fracción F008 y la subfracción F011, mostraron una buena actividad larvicida con CL50 de 35,1; 20,9, y 14,98 mg/L, respectivamente. Conclusiones: según los resultados, se consideró como promisorio el extracto de semillas de Tabernaemontana cymosa para la obtención de metabolitos secundarios con actividad larvicida.

Introduction: Aedes aegypti is the main vector of dengue and yellow fever. One way to combat these diseases today is the vector control. However, the problems caused by synthetic insecticides and the acquired resistance by mosquitoes, turn this control into a more difficult struggle every day. The plants offer an alternative source to the use of synthetic insecticides. Objectives: the objective of this study was to evaluate the larvicidal activity of the ethanol extracts and active fractions of different organs of Trichilia hirta L. and Tabernaemontana cymosa Jacq. Methods: in this study, Aedes aegypti larvae in III and IV stages were used. The total ethanol extracts were obtained by maceration of dried and ground plant material for a week and then dried at reduced pressure. The fractionation was performed by open column chromatography with the use of different polarity solvents. The larvicidal activity was assessed following protocols recommended by the World Health Organization. Results: the ethanol extracts from Trichilia hirta bark and flowers, and Tabernaemontana cymosa bark and leaves showed no larvicidal activity. The Trichilia hirta seed extract showed a moderate activity with an LC50 and LC90 of 219.2 and 331.4 mg/L respectively. The ethanol extract from Tabernaemontana cymosa seeds, the fraction F008 and the subfraction F011, showed good larvicidal activity with LC50 of 35.1, 20.9, and 14.98 mg/L, respectively. Conclusions: according to the results obtained in this study, the extract from Tabernaemontana cymosa seeds could be considered as a potential source of secondary metabolites with larvicidal activity.

In vitro antibacterial and antifungal activities of Tabernaemontana heyneana Wall. leaves.

Medicinal plants are the oldest source of pharmacologically active compounds and provided virtually the only source of medicinally useful compounds for centuries. They contain physiologically active principles that over the years have been exploited in traditional medicine for the treatment of various ailments. The increased likelihood of acute infections and inflammatory conditions in early humans could have set the stage for the natural selection of the use of medicinal herbs high in antimicrobial and anti-inflammatory components. In the present study, the in vitro antibacterial and antifungal activities of different solvent leaf extracts of T. heyneana Wall. was investigated. K. pneumoniae (26±1.0 mm) and S. typhii (9.0±2.0 mm) were proved to be inhibited maximally and minimally by the leaves of T. heyneana. Similarly, the maximum and minimum antifungal effect was observed against Rhizopus mucor (25±0.0 mm) and Trichoderma viridins (6.0±1.0 mm), respectively. Among the solvents methanol was proved to be the best one in the extraction of antimicrobial compounds. Ethanol and aqueous systems were proved to be moderate and chloroform as poor solvent in extracting antimicrobial components. Overall results has proved that T. heyneana leaves possess significant antibacterial and poor antifungal activities.

Antioxidant and cytotoxic potential of methanol extract of Tabernaemontana divaricata leaves.

The methanolic extract obtained from the leaves of Tabernaemontana divericata (Family: Apocynaceae) was evaluated for in vitro antioxidant potential by determination of total antioxidant capacity, assay of nitric oxide scavenging activity and reducing power test. The extract was also screened for its cytotoxic effect using brine shrimp lethality bioassay. The results revealed potent antioxidant property in all antioxidant assays compared to the reference antioxidant, ascorbic acid in a dose dependent manner. Further, the methanolic extract of Tabernaemontana divericata showed significant cytotoxic effect (LC50: 3.12μg/ml) compared with positive control, Vincristine Sulphate (LC50: 0.331μg/ml).

Antioxidant and cytotoxic potential of methanol extract of Tabernaemontana divaricata leaves.

The methanolic extract obtained from the leaves of Tabernaemontana divericata (Family: Apocynaceae) was evaluated for in vitro antioxidant potential by determination of total antioxidant capacity, assay of nitric oxide scavenging activity and reducing power test. The extract was also screened for its cytotoxic effect using brine shrimp lethality bioassay. The results revealed potent antioxidant property in all antioxidant assays compared to the reference antioxidant, ascorbic acid in a dose dependent manner. Further, the methanolic extract of Tabernaemontana divericata showed significant cytotoxic effect (LC50: 3.12μg/ml) compared with positive control, Vincristine Sulphate (LC50: 0.331μg/ml).

Gastroprotective Effect of Tabernaemontana divaricata (Linn.) R.Br. Flower Methanolic Extract in Wistar Rats.

Tabernaemontana divaricata (L.) R.Br belonging to Apocynaceae family is traditionally used by people in many parts of the world to treat various disorders. The present study was undertaken to investigate anti-ulcer property of Tabernaemontana divaricata flower methanolic extract (TDFME 500 mg/kg, p.o) by pyloric ligation induced gastric ulceration model using Omeprazole (8mg/kg, p.o) as a standard drug in wistar rats. Five parameters i.e., volume of gastric juice, pH, free & total acidities and ulcer index were assessed. The test extract significantly (p< 0.01) decreased volume of gastric juice, free & total acidities and ulcer index. Like standard, it also raised pH of gastric acid. The observed percentage protection for standard and test were 89.84% and 79.53%, respectively. Thus, TDFME 500 mg/kg had a positive effect on all the parameters under study and the results were similar to that of standard. From the above results, it can be concluded that TDFME exhibits remarkable gastroprotective effect.

Reversible acetylcholinesterase inhibitory effect of Tabernaemontana divaricata extract on synaptic transmission in rat CA1 hippocampus.

Background & objectives: Acetylcholinesterase inhibitors (AChE-Is) are used for the treatment of Alzheimer’s disease (AD). These drugs including galanthamine have been shown to modulate synaptic activity in hippocampus and improve memory processes. Although Tabernaemontana divaricata extract (TDE) has been used as traditional medicine for various pharmacological effects, its effect in enhancing cholinergic activity provides additional benefit to its known effects. We investigated whether TDE can modulate the synaptic function in hippocampus and compared its effects to those of galanthamine. Methods: Hippocampal slices were prepared from male wWistar rats, functional effects of TDE were characterized by using pharmacological tools and extracellular recordings of field excitatory postsynaptic potentials (fEPSPs). Results: TDE significantly reduced fEPSPs. The fEPSPs reduction was prevented by atropine, but not pancuronium. These TDE effects were similar to those of galanthamine. Interpretation & conclusions: Our findings indicate that TDE can effectively modulate synaptic responses in the hippocampus similar to galanthamine, suggesting that this traditional medicine could be beneficial in ageing with ACh deprivation in the brain.

Atividade alelopática de extratos aquosos de plantas medicinais na germinação de Lactuca sativa L. e Bidens pilosa L. / Allelopathic activity of aqueous extracts of medicinal plants on the germination of Lactuca sativa L. and Bidens pilosa L.

O potencial alelopático de quatro diferentes extratos de plantas medicinais (Eclipta alba, Gomphrena globosa, Tabernaemontana catharinensis e Tithonia diversifolia) foi avaliado na germinação de Bidens pilosa e Lactuca sativa. Dentre os resultados obtidos no teste de germinação, notou-se um maior poder inibitório do extrato de G. globosa sobre sementes e plântulas de Bidens pilosa e Lactuca sativa independente da concentração utilizada e aumento da atividade inibitória de extratos T. catharinensis e de T. diversifolia com aumento da concentração destes. Quanto ao Índice de Velocidade de Germinação, os dados demonstraram redução do índice devido a elevada mortalidade das plântulas submetidas aos extratos de G. globosa e de T. catharinensis e a germinação tardia das sementes submetidas ao extrato de T. diversifolia. Quanto ao vigor das sementes, as menores porcentagens de sobrevivência ocorreram extratos à 2,5 por cento para B. pilosa e 10 por cento para L. sativa.

The allelopathic potential of four different extracts of medicinal plants (Eclipta alba, Gomphrena globosa, Tabernaemontana catharinensis and Tithonia diversifolia) was evaluated on the germination of Bidens pilosa and Lactuca sativa. The results obtained in the germination test indicated a greater inhibitory activity of G. globosa extract on Bidens pilosa and Lactuca sativa seeds and seedlings, regardlessof the used concentration, and an increase in the inhibitory activity of T. catharinensis and T. diversifolia extracts with an increase in their concentrations. As to Germination Speed Index, the data demonstrated a reduction due to the high mortality of seedlings subjected to G. globosa and T. catharinensis extracts and a late germination of seeds subjected to T. diversifolia extracts. As to the vigor of seeds, the smallest survival percentages occur at 2.5 percent for B. pilosa and at 10 percent for L.sativa.

Avaliação da atividade antimicrobiana in vitro do extrato de Tabernaemontana catharinensis A. DC / Evaluation of in vitro antimicrobial activity of Tabernaemontana catharinensis A. DC. extract

Diversas espécies de Tabernaemontana têm sido estudadas devido a diversidade de alcalóides com atividade farmacológica. O objetivo desse trabalho foi avaliar a capacidade antimicrobiana in vitro do extrato das cascas do caule de Tabernaemontana catharinensis A. DC.em cepas de Staphylococcus aureus e Pseudomonas aeruginosa, microrganismos causadores de diversas infecções. Os testes de susceptibilidade bacteriana foram realizados usando o método de Kirby Bauer, consistindo na difusão em disco do antibiótico em meio de cultivo Mueller Hinton. Os testes de inibição foram realizados com soluções do extrato bruto seco de T. catharinensis dissolvido em etanol 70 por cento (v/v) na concentração 1,0 mg mL-1, que aplicada nos discos de área 20 mm², apresentaram concentração de 0,005 mg mm-2. Como controle negativo, realizou-se ensaios com placas contendo P. aeruginosa, e discos com etanol 70 por cento (v/v), e como controle positivo, discos com os antibióticos ceftriaxona sódica (0,25 mg mm-2 de área do disco), tetraciclina (0,005 mg mm-2) e cefalexina (0,005 mg mm-2). A solução do extrato na concentração de 0,005 mg mm-2 inibiu o Staphylococcus aureus, com diâmetro médio do halo de 0,6 cm. O halo de inibição para o Pseudomonas aeruginosa foi em média 1,2 cm. A tetraciclina, a cefalexina, e o controle negativo (etanol 70 por cento v/v) não demonstraram ação antimicrobiana. O halo de inibição usando ceftriaxona foi em média 2,2 cm para P. aeruginosa e 1,0 cm para Staphylococcus aureus.

Several Tabernaemontana species have been studied due to their several alkaloids with pharmacological activity. The aim of this work was to evaluate the in vitro antimicrobial action of the extract from stem barks of Tabernaemontana catharinensis A. DC. against strains of Staphylococcus aureus and Pseudomonas aeruginosa, microorganisms that cause several infections. Bacterial susceptibility tests were performed by the Kirby-Bauer method, consisting in antibiotic disk diffusion in Mueller Hinton medium. Inhibition tests were performed with solutions of T. catharinensis dry crude extract dissolved in ethanol 70 percent (v/v) at 1.0 mg mL-1, which became 0.005 mg mm-2 when applied to 20 mm² disks. As negative control, assays were carried out in plates containing P. aeruginosa and disks with ethanol 70 percent (v/v). Positive control consisted of disks containing the antibiotics ceftriaxone sodium (0.25 mg mm-2 disk area), tetracycline (0.005 mg mm-2) and cephalexin (0.005 mg mm-2). Extract solution at 0.005 mg mm-2 inhibited Staphylococcus aureus, with 0.6cm halo mean diameter. The inhibition halo for Pseudomonas aeruginosa was on average 1.2 cm. Tetracycline, cephalexin and negative control (ethanol 70 percent v/v) did not show antimicrobial action, whereas ceftriaxone sodium resulted in 2.2 and 1.0cm mean inhibition halo diameters for P. aeruginosa and Staphylococcus aureus, respectively.

Isolamento, identificação e avaliação da atividade antileucêmica de alcaloides indólicos monoterpênicos de Tabernaemontana salzmannii (A. DC.), Apocynaceae / Isolation, identification and antileukemic activity of the monoterpene indole alkaloids from Tabernaemontana salzmannii (A. DC.), Apocynaceae

O presente trabalho descreve o isolamento e a identificação de nove alcaloides indólicos monoterpênicos das cascas das raízes e folhas de Tabernaemontana salzmannii (Apocynaceae). As estruturas dos alcaloides foram identificadas através de métodos espectroscópicos uni (RMN ¹H, 13C, APT) e bidimensionais (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC e HMBC) e espectrometria de massas (EM), além da comparação com dados de literatura. Um screening in vitro da atividade antileucêmica foi feito com os alcaloides majoritários isolados. Dentre os nove alcaloides isolados, a isovoacangina e voacangina mostraram-se capazes de induzir morte celular por apoptose em células leucêmicas humanas THP-1.

This work describes the isolation and structural determination of nine monoterpenic indole alkaloids from the roots bark and leaves of Tabernaemontana salzmannii. The alkaloids were identified by spectroscopic methods uni (NMR ¹H, 13C, APT) and two-dimensional (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC and HMBC) and mass spectra besides comparison with literature data. An in vitro screening was done with the isolated major alkaloids. Among the nine alkaloids isolated, isovoacangine and voacangine alkaloids were able to induce apoptosis cell death in human leukemic cells line THP-1.

Isolamento, identificação e avaliação da atividade antileucêmica de alcaloides indólicos monoterpênicos de Tabernaemontana salzmannii A. DC., Apocynaceae / Isolation, identification and antileukemic activity of the monoterpene indole alkaloids from Tabernaemontana salzmannii A. DC., Apocynaceae

O presente trabalho descreve o isolamento e a identificação de nove alcaloides indólicos monoterpênicos das cascas das raízes e folhas de Tabernaemontana salzmannii (Apocynaceae). As estruturas dos alcaloides foram identificadas através de métodos espectroscópicos uni (RMN ¹H, 13C, APT) e bidimensionais (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC e HMBC) e espectrometria de massas (EM), além da comparação com dados de literatura. Um screening in vitro da atividade antileucêmica foi feito com os alcaloides majoritários isolados. Dentre os nove alcaloides isolados, a isovoacangina e voacangina mostraram-se capazes de induzir morte celular por apoptose em células leucêmicas humanas THP-1.

This work describes the isolation and structural determination of nine monoterpenic indole alkaloids from the root barks and leaves of Tabernaemontana salzmannii. The alkaloids were identified by spectroscopic methods uni (NMR ¹H, 13C, APT) and two-dimensional (¹H-¹H-COSY, ¹H-¹H-NOESY, HMQC and HMBC) and mass spectra besides comparison with literature data. An in vitro screening was done with the isolated major alkaloids. Among the nine alkaloids isolated, isovoacangine and voacangine alkaloids were able to induce apoptosis cell death in human leukemic cells line THP-1.

Study on chemical constituents of Tabernaemontana divaricata (II) / 第二军医大学学报

Objective: To extract and identify the chemical constituents in the roots and stems of Tabernaemontana divaricata. Methods: The solvent extraction and silica column chromatography were used to separate the chemical constituents, and their structures were identified by physicochemical properties and spectra analysis. Results: Six compounds were isolated and their structures were identified as his (2, 3-dihydroxypropyl) octacosanedioate (1), tetratriacontanol (2), palmitic acid (3), glycerol monopalmitatel (4), β-sitosterol (5), and β-daucosterol (6). Conclusion: Compound 1 is a new glyceroesters: compounds 2,3 and 4 are isolated from Tabernaemontana genus for the first time.

Isolamento e avaliação da atividade biológica dos alcalóides majoritários de Tabernaemontana angulata Mart. ex Müll. Arg., Apocynaceae / Isolation and evaluation of the biological activity related to the major alkaloids in Tabernaemontana angulata Mart. ex Müll. Arg., Apocynaceae

A necessidade da introdução de novos agentes quimioterápicos é uma realidade no controle de doenças infecciosas. O Brasil é o país mais rico em biodiversidade, e o Laboratório de Extração da Universidade Paulista tem coletado plantas na Amazônia e Mata Atlântica com a finalidade de identificar extratos vegetais antibacterianos e antitumorais. Estudos prévios demonstraram que a fração etanólica obtida do extrato bruto orgânico do caule de Tabernaemontana angulata Mart. ex Müll. Arg. apresentou atividade antimicrobiana significante contra Staphylococcus aureus ATCC6538, no ensaio de diluição em caldo. Verificou-se por cromatografia em camada delgada que os compostos majoritários presentes na fração ativa eram alcalóides. No presente trabalho, foi obtida a fração de alcalóides totais a partir do extrato bruto, da qual os compostos majoritários foram isolados por sucessivas cromatografias e, posteriormente, identificados por CG-EM e ¹H-RMN como os alcalóides indólicos coronaridina e voacangina. As frações obtidas do isolamento foram testadas no ensaio biológico, porém não demonstraram atividade antimicrobiana.

Introducing new chemotherapeutic agents is a great demand in the control of infectious diseases. Brazil is one of the richest countries in biodiversity and the Laboratório de Extração at UNIP has been collecting plants from the Amazon and Atlantic Rain Forests with the aim of screening for new antibacterial and antitumor plant extracts. Previous studies demonstrated that the ethanol fraction obtained from the crude extract of Tabernaemontana angulata stems showed an antibacterial activity against Staphylococcus aureus (ATCC 6538) in the microdilution broth assay. Two alkaloids were the major compounds in the active fraction, verified by thin layer chromatography analysis. In the present study, the total alkaloids were obtained from the crude extract and were fractionated by preparative thin layer chromatography for the isolation of the main components. The isolated compounds were identified by GC/MS and ¹H-NMR as coronaridine and voacangine. The alkaloid fractions obtained from the isolation procedure were tested for antibacterial activity, but no activity was detected.