Anti-inflammatory,antipyretic and antinociceptive activities of Tabernaemontana pandacaqui Poir

Studies on carrageenin-induced rat paw edema, yeast-induced hyperthermia in rat and writhing response induced by acetic acid in mice showed that the alcoholic extract of stems of Tabernaemontana pandacaqui (T. pandacaqui) has significant anti-inflammatory, antipyretic and antinociceptive activities. These activities are due to alkaloidal components since they were also observed when the crude alkaloidal (CA) fraction separated from alcoholic extract was tested in the same models.     

Cardiovascular effects of Tabernaemontana pandacaqui

Intravenous injection of ethanolic extracts of the stem, leaf and flower of Tabernaemontana pandacaqui caused hypotension in pentobarbital anesthetized rats. At high doses (100-300 mg/kg), the flower extract showed a transient hypertensive effect preceeding hypotensive activity. The effects of the extracts on the heart rate of anesthetized rats correlated well with the negative chronotropic and inotropic activity observed with isolated atrium. The hypotensive activity was not inhibited by antihistaminic and antimuscarinic agents. The extracts had no effect on the pressor effects induced by norepinephrine or dual carotid occlusion. These results suggest that the hypotensive action of the extracts is not mediated through histaminic and muscarinic receptors stimulation, alpha-adrenoceptor blockade or interference of sympathetic transmission.     

Interference of linoleic acid fraction in some receptor binding assays.

An extract of a suspension culture of Tabernaemontana pandacaqui Poir. was fractionated by centrifugal partition chromatography. Aliquots were tested in an adenosine A1 receptor binding assay. This led to the isolation and identification of linoleic acid, which proved to be a noncompetitive inhibitor. This "false positive"effect also extended to some other binding assays.     

Screening for acetylcholinesterase inhibitory activity in plants used in Thai traditional rejuvenating and neurotonic remedies

Acetylcholinesterase (AChE) inhibitor has been used as a drug for the symptomatic treatment of Alzheimer's disease. In order to search for new AChE inhibitors, 32 plants used in Thai traditional rejuvenating and neurotonic remedies were collected. The plant methanolic extracts were tested for AChE inhibitory activity using Ellman's colorimetric method in 96-welled microplates. The results showed that the methanolic extracts from roots of Stephania suberosa Forman. and Tabernaemontana divaricata (L.) R.Br. ex Roem. & Schult. at concentration of 0.1 mg/ml inhibited more than 90% of AChE activity. At the same concentration, four extracts, i.e. stems of Piper interruptum Opiz., seeds of Piper nigrum L., rootbarks of Butea superba Roxb. and roots of Cassia fistula L. extracts showed 50-65% inhibitory activity on AChE. The rest of the extracts showed the AChE inhibitory activity below 50%.     

马蹄花提取物对大鼠的抗生育作用(英文)

AIM:To evaluate the anti-fertility effect of methanolic(MeTD) and aqueous(AqTD) flower extracts of Tabernaemon-tana divaricata in rats.METHODS:The anti-fertility activity of the extracts was evaluated using two experimental animal models:1) Estrogenic activity was carried out in immature female rats using ethinyl estradiol as standard.The evaluation parameters includes changes in uterine weight and histopathology of uterus.2) Anti-implantation and early abortifacient activity was performed in female Wistar rats.The number of implants and resorbtions were compared to vehicle control.RESULTS:Phytochemical analysis of MeTD and AqTD revealed the presence of carbohydrates,amino acids,steroids,glycosides,flavonoids,alkaloids and tannins.In estrogenic activity,the MeTD and AqTD were offered significant estrogen-like activity at 500 mg?kg-1,p.o.by increasing the uterine weight com-pared to vehicle control group.In Anti-implantation and early abortifacient activity study,MeTD(500 mg?kg-1,p.o.) showed significant effect and it was evident by decrease in the number of implants and increase in the number of resorbtions compared to vehicle control group.CONCLUSION:The MeTD at 500 mg?kg-1,p.o.possess significant estrogenic,anti-implantation and early abortifacient activ-ity,while the AqTD at 500 mg?kg-1,p.o.was found to possess significant estrogenic activity and the results are in consistent with the literature reports related to anti-fertility effect of flower extracts of Tabernaemontana divaricata.     

Antimycobacterial evaluation and preliminary phytochemical investigation of selected medicinal plants traditionally used in Mozambique

Ethnopharmacological relevance

Several medicinal plants are traditionally used in Mozambique to treat tuberculosis and related symptoms.

Aims of the study

It was aimed to assess the in vitro antimycobacterial activity of crude extracts from fifteen medicinal plants and to reveal main classes of compounds which may account for the activity of extracts.

Methods and materials

The plant materials were sequentially extracted by n-hexane, dichloromethane, ethyl acetate, and 70% ethanol. Decoction of each plant material was also prepared according to traditional use. Broth microdilution method was employed to screen extracts against two mycobacterial species: Mycobacterium smegmatis ATCC 607 and Mycobacterium tuberculosis H37Rv. The extracts with minimum inhibitory concentration(s) (MIC) below 125 μg/mL were considered active and further tested against different mycobacterial species and strains, namely Mycobacterium tuberculosis H37Ra, Mycobacterium bovis BCG ATCC 35734, Mycobacterium smegmatis mc² 155, Mycobacterium avium DSM 44156 and DSM 44157. Cytotoxic effect was evaluated against human macrophages from the monocytic THP-1 cells. Main classes of compounds in these active extracts were proposed from their ¹H NMR spectroscopic characterizations.

Results

n-Hexane extracts of Maerua edulis and Securidaca longepedunculata, ethyl acetate extract of Tabernaemontana elegans and dichloromethane extract of Zanthoxylum capense were found to possess considerable activity against Mycobacterium bovis BCG and Mycobacterium tuberculosis H37Ra with MIC 15.6-62.5 μg/mL. Tabernaemontana elegans ethyl acetate extract displayed strong activity against Mycobacterium tuberculosis H37Rv (MIC 15.6 μg/mL). Except for Tabernaemontana elegans ethyl acetate extract which presented potent cytotoxic effects in THP-1 cells (IC₅₀ < 4 μg/mL), the other three plant extracts showed moderate to none toxicity. Based on ¹H NMR spectroscopic analysis, major components in both Maerua edulis and Securidaca longepedunculata n-hexane extracts were linear chain unsaturated fatty acids. Zanthoxylum capense dichloromethane extract contained more complex constituents (mostly phenolic compounds). In the most potent extract, Tabernaemontana elegans ethyl acetate extract, the prominent compounds were identified as indole alkaloids.

Conclusions

The pronounced antimycobacterial activity of the medicinal plants Maerua edulis, Securidaca longepedunculata, Zanthoxylum capense, and Tabernaemontana elegans suggested that they might provide compounds which could be potential anti-TB drug leads.     

Tabernaemontana divaricata extract inhibits neuronal acetylcholinesterase activity in rats

The current pharmacotherapy for Alzheimer's disease (AD) is the use of acetylcholinesterase inhibitors (AChE-Is). A previous in vitro study showed that Tabernaemontana divaricata extract (TDE) can inhibit AChE activity. However, neither the AChE inhibitory effects nor the effect on neuronal activity of TDE has been investigated in vivo. To determine those effects of TDE in animal models, the Ellman's colorimetric method was implemented to investigate the cortical and circulating cholinesterase (ChE) activity, and Fos expression was used to determine the neuronal activity in the cerebral cortex, following acute administration of TDE with various doses (250, 500 and 1000 mg/kg) and at different time points. All doses of TDE 2 h after a single administration significantly inhibited cortical AChE activity and enhanced neuronal activity in the cerebral cortex. The enhancement of Fos expression and AChE inhibitory effects in the cerebral cortex among the three TDE-treated groups was not significantly different. A 2 h interval following all doses of TDE administration had no effect on circulating ChE activity. However, TDE significantly inhibited circulating AChE 10, 30 and 60 min after administration. Our findings suggest that TDE is a reversible AChE-I and could be beneficial as a novel therapeutic agent for AD.     

A neutrophil multitarget functional bioassay to detect anti-inflammatory natural products.

A multitarget functional bioassay was optimized as a method for detecting substances interacting with the inflammatory process of activated neutrophil granulocytes, mainly to release elastase detected by p-nitroanilide (pNA) formation. Using this bioassay, 100 fractionated extracts of 96 plants were screened, with results presented in a manner that links recorded biological activity to phylogenetic information. The plants were selected to represent a major part of the angiosperms, with emphasis on medicinal plants, Swedish anti-inflammatory plants, and plants known to contain peptides. Of the tested extracts, 41% inhibited pNA formation more than 60%, and 3% stimulated formation. The extract of Digitalis purpurea enhanced pNA formation, and digitoxin, the active compound, was isolated and identified. Plant extracts that exhibited potent nonselective inhibition (>80% inhibition) were evaluated further for direct inhibition of isolated elastase and trypsin enzyme. The inhibitory effect of most tested extracts on the isolated enzyme elastase was similar to that of PAF- and fMLP-induced pNA formation. Compared to trypsin, inhibition of elastase by extracts of Rubus idaeus and Tabernaemontana dichotoma was significantly higher (80% and 99%, respectively). Inhibition of trypsin by the extract of Reseda luteola was high (97%). Orders such as Lamiales and Brassicales were shown to include a comparably high proportion of plants with inhibitory extracts.     

Effect of an alkaloidal fraction of Tabernaemontana elegans (Stapf.) on selected micro-organisms

Ethnopharmacological relevance

Bacterial infections remain a significant threat to human health. Due to the emergence of widespread antibiotic resistance, development of novel antibiotics is required in order to ensure that effective treatment remains available. There are several reports on the ethnomedical use of Tabernaemontana elegans pertaining to antibacterial activity.

Aim of the study

The aim of this study was to isolate and identify the fraction responsible for the antimicrobial activity in Tabernaemontana elegans (Stapf.) root extracts.

Materials and methods

The active fraction was characterized by thin layer chromatography (TLC) and gas chromatography–mass spectrometry (GC–MS). Antibacterial activity was determined using the broth micro-dilution assay and antimycobacterial activity using the BACTEC radiometric assay. Cytotoxicity of the crude extract and fractions was assessed against primary cell cultures; lymphocytes and fibroblasts; as well as a hepatocarcinoma (HepG2) and macrophage (THP-1) cell line using the Neutral Red uptake and MTT assays.

Results

The crude root extracts were found to contain a high concentration of alkaloids (1.2%, w/w). GC–MS analysis identified the indole alkaloids, voacangine and dregamine, as major components. Antibacterial activity was limited to the Gram-positive bacteria and Mycobacterium species, with MIC values in the range of 64–256 μg/ml. When combined with antibiotics, additive antibacterial effects were observed. Marked cytotoxicity to all cell lines tested was evident in the MTT and Neutral Red uptake assays, with IC₅₀ values <9.81 μg/ml.

Conclusions

This study confirms the antibacterial activity of Tabernaemontana elegans and supports its potential for being investigated further for the development of a novel antibacterial compound.     

白子菜提取物对SHR大鼠靶器官损伤的保护作用研究

目的 评价白子菜水提物对高血压诱导的组织器官损伤的保护作用.方法 根据基础血压将40只SHR大鼠分成5组:空白对照组(蒸馏水)、阳性对照组(卡托普利,25 mg/kg)、白子菜水提物高、中、低剂量组(2 g生药/kg、1g生药/kg、0.5 g生药/kg),每天灌胃给药,持续7周,每周称重并记录心率1次,第7周末,通过肉眼和显微观察各鼠心、脑、肾和脾脏的外观或病理变化并予以分级评分.结果 经过7周实验,与空白组比较,白子菜高、中剂量组均能明显抑制心肌细胞肥大和肾小球(管)萎缩或代偿性肥大(P＜0.01).高剂量组能显著改善脾脏中央动脉硬化变性现象(P＜0.05),降低左室壁厚/右室壁厚,增加肾皮质厚/肾髓质厚(P＜0.05).而低剂量仅对肾脏病理改变有显著保护作用(P＜0.05).结论 白子菜提取物对高血压引起的主要器官损伤具有明显的保护作用.     

Bioactivity studies on Cassia alata Linn. leaf extracts

The hexane, chloroform and ethyl acetate extracts of the leaves of Cussia alata Linn. were tested for their antimutagenic, antifungal, analgesic, antiinflammatory and hypoglycaemic activities. At a dosage of 5 mg/20 g mouse, the hexane extract was analgesic as it reduced the number of squirms induced by acetic acid by 59.5%. Both the hexane and EtOAc extracts exhibited antiinflammatory activity at a dosage of 5 mg/20 g mouse with a 65.5% and 68.2% decrease in carrageenan-induced inflammation, respectively. The chloroform extract was antimutagenic, at a dosage of 2 mg/20 g mouse, with a 65.8% inhibition in the mutagenicity of tetracycline. It was also the most active against Trichophyton mentagrophytes, at a concentration of 50 mg/mL but it had no activity against Candida albicans. The hexane and EtOAc extracts showed some activity against both organisms, with the EtOAc extract being more active against C. albicans. The EtOAc extract was hypoglycaemic. At a dosage of 5 mg/20 g mouse, it decreased the blood sugar level of mice by 58.3%. Pharmacological studies showed that all extracts caused an immediate decrease in motor activity, enophthalmus, hyperemia, micturition and diarrhoea. At a dosage of 150 mg/20 g mouse, the EtOAc extract caused paralysis, screen grip loss and enophthalmus accompanied by drooping and closure of the eyelids.     

Antiprotozoal activities of Colombian plants.

In our search for therapeutical alternatives for antiprotozoal chemotherapy, we collected a selection of 44 plants from western Colombia upon ethnopharmacological and chemotaxonomic considerations. Polar and apolar extracts of these species were examined for antimalarial activity using in vitro tests with two clones of Plasmodium falciparum. Leishmanicidal and trypanocidal activity were determined in vitro using promastigote and amastigote forms of several strains of Leishmania sp. and epimastigotes of Trypanosoma cruzi. Among the selected plants, the 15 following species showed good or very good antiprotozoal activity in vitro: Aspidosperma megalocarpon, Campnosperma panamense, Conobea scoparioides, Guarea polymera, Guarea guidonia, Guatteria amplifolia, Huberodendron patinoi, Hygrophila guianensis, Jacaranda caucana, Marila laxiflora, Otoba novogranatensis, Otoba parviflora, Protium amplium, Swinglea glutinosa and Tabernaemontana obliqua. Cytotoxicity was assessed in U-937 cells and the ratio of cytotoxicity to antiprotozoal activity was determined for the active extracts. Ten extracts from eight species showed selectivity indexes > or = 10. Among the extracts that showed leishmanicidal activity, the methylene chloride extract of leaves from C. scoparioides showed a selectivity index in the same range that the one of the Glucantime control. Several of the active leishmanicidal plants are traditionally used against leishmaniasis by the population of the concerned area.     

In vivo antitumoural activity and acute toxicity study of Larrea divaricata Cav. extract

In the present work, we analysed the effect of the extract of Larrea divaricata Cav. on a mammary carcinoma chemically induced with N-nitroso-N-methylurea in female rats. The extract was administered in a dose of 25 mg/kg, subcutaneously, beginning 20 days after tumour appearance. Of a total of 75 tumours treated with extract, a regression of 10 tumours (13%) was observed, a stabilization of 60 tumours (80%) and an increment of 5 tumours (6%). None of the 80 control tumours decreased (0%) and only 12 tumours remained static (15%). The survival time of the animals treated with the extract was significantly higher (p <0.05) than the survival time of the controls. The LD₅₀ in females was lower than in male mice. Data indicate that the aqueous extract of Larrea divaricata Cav. could be considered tumouristatic as the extract blocked progress of the tumour. © 1997 John Wiley & Sons, Ltd.     

The relaxation of isolated rabbit corpus cavernosum by the herbal medicine Catuama and its constituents

The effects of the Brazilian herbal medicine Catuama and each of its plant constituents (Paullinia cupana, Trichilia catigua, Zingiber officinalis and Ptychopetalum olacoides) were investigated on rabbit corpus cavernosum (RbCC) using a bioassay cascade. Catuama caused short-lived and dose-dependent relaxations (11% +/- 7%, 26% +/- 5% and 82% +/- 9%, at doses of 1, 3 and 10 mg, respectively). Neither the nitric oxide synthesis inhibitor N(omega)-nitro-L-arginine methyl ester (L-NAME; 10 microM) nor the soluble guanylate cyclase inhibitor ODQ (10 microM) significantly affected the Catuama-induced relaxations. Similarly, the selective ATP-dependent K(+) channel (K(ATP)) blocker glibenclamide (10 microM), the muscarinic receptor antagonist atropine (1 microM) and the voltage-dependent Na(+) channel blocker tetrodotoxin (1 microM) all failed to affect significantly the Catuama-induced relaxations. These results indicate that the relaxations induced by Catuama involve neither nitric oxide release nor K(ATP) channel activation. The extracts of P. cupana, Z. officinalis and P. olacoides caused short-lived and dose-dependent RbCC relaxations, whereas T. catigua evoked long-lasting relaxations which were occasionally preceded by a brief contractile effect. The extract of P. cupana was the most active in relaxing RbCC strips. The relaxations induced by all extracts were not significantly affected by L-NAME (10 microM). The infusion of ODQ (10 microM) had no significant effect on the P. cupana- and Z. officinalis-induced relaxations but reduced by >50% (p < 0.05) those evoked by P. olacoides and T. catigua. Incubations of RbCC with Catuama(10 mg/mL for 0.25 to 5 min) caused increases of cAMP levels (143% increase at 5 min of incubation). Incubations of RbCC with P. cupana extract (1 mg/mL) increased the cAMP levels by 200% whereas higher doses (10 and 100 mg/mL) caused smaller increases in the nucleotide levels (150% and 89%, respectively). The extracts of Z. officinalis and P. olacoides (same doses) caused smaller increases of the cAMP levels compared with the P. cupana extract, whereas T. catigua (1-100 mg) did not increase the levels of this nucleotide above the basal values. Our results show that of the four extracts assayed, P. cupana was the most effective, indicating that it is the main extract responsible for the relaxing effect of Catuama on rabbit cavernosal tissue.     

The antiinflammatory and liver protective effect of Tithonia diversifolia (Hemsl.) gray and Dicliptera chinensis Juss. Extracts in rats

The antiinflammatory and liver protective effect of water extracts of Tithonia diversifolia (Hemsl.) Gray (aerial part), T. diversifolia (stem) and Dicliptera chinensis Juss. (aerial part) against paw oedema induced by carrageenan and acute hepatic damage induced by CCI₄ were determined in rats. The results indicated that treatment with a water extract of the aerial part of T. diversifolia decreased the paw oedema induced by carrageenan (p < 0.001) and the GOT, GPT level elevation caused by CCI₄ were reduced (p < 0.01). The pathological changes of hepatic lesions caused by CCI₄ were improved by treatment with the drug extracts mentioned above.     

Ethnobotanical and antimicrobial investigation on some species of Terminalia and Combretum (Combretaceae) growing in Tanzania.

An ethnobotanical investigation on the medicinal uses of some species of Terminalia and Combretum (Combretaceae) was carried out in Mbeya, Tanzania during a 5-weeks field expedition. Of the sixteen species collected, Combretum fragrans F. Hoffm., Combretum molle G. Don., Combretum psidioides Welw., Combretum zeyheri Sond., Terminalia kaiserana F. Hoffm. and Terminalia sericea Burch ex. DC. have medical applications against various bacterial infections, such as gonorrhoea and syphilis, and against symptoms like diarrhoea, hypertension and even cancer. Antimicrobial screening of the crude extracts of the selected Combretum and Terminalia species was performed by the agar diffusion method. Among the most effective extracts were methanol extracts of the roots of Terminalia sambesiaca Engl. & Diels., T. kaiserana Guill. & Perrott., T. sericea Burch. ex DC., C. fragrans F. Hoffm. and Combretum padoides Engl. & Diels., all of which showed marked inhibition against Gram-positive bacteria, and were also good inhibitors of Enterobacter aerogenes. All four of the extracts of the roots of T. sericea tested, (methanol, ethanol, acetone and hot water) had good antimicrobial activity. A methanolic leaf extract of T. kaiserana was the only extract to have a bacteriocidic effect on Escherichia coli. Methanol root extracts of T. sambesiaca and methanol leaf extracts of T. sericea were the most effective against Candida albicans. The results of the antimicrobial screening support the ethnomedical uses of these plants.     

In vitro antitrypanosomal activity of Moringa stenopetala leaves and roots.

The leaves and the root extracts of Moringa stenopetala were tested in vitro against trypomastigotes of Trypanosoma brucei, Trypanosoma cruzi and L. donovani amastigotes. The fresh root wood ethanol extract and the dried leaves acetone extract were found to be active against T. brucei with an ED(50) value of 9.2 microg/mL and 10.0 microg/mL respectively. All the other extracts were inactive against all the tested parasite forms.     

Terminalia arjuna,an ayurvedic cardiotonic,increases contractile force of rat isolated atria

The direct effects of aqueous, ethanolic, chloroform and petroleum ether extracts of Terminalia arjuna (family: Combretaceae) bark, an ayurvedic remedy for cardiovascular disorders, were studied on isolated atria of rats. The aqueous extract produced a substantial positive inotropic effect (EC₅₀ = 0.25 mg/mL) but no change in the rate. The ethanol, chloroform and petroleum ether extracts all decreased the rate of contraction. A slight increase in force was seen with ethanol and chloroform extracts. Higher concentrations of the chloroform extract had a negative inotropic effect. The ethanol extract decreased the maximum following frequency of the left atria. It is concluded that Terminalia arjuna has a significant positive inotropic property on rat atria in vitro which could contribute to its efficacy in treating cardiovascular disorders.     

Relative efficacy of three medicinal plant extracts in the alteration of thyroid hormone concentrations in male mice

Relative importance of Bacopa monnieri (200 mg/kg), Aegle marmelos (1.00 g/kg) and Aloe vera (125 mg/kg) leaf extracts in the regulation of thyroid hormone concentrations in male mice was investigated. While serum levels of both T(3) and T(4) were inhibited by A. vera, A. marmelos extract could decrease only T(3) concentration. On the other hand, T(4) concentration was increased by B. monnieri extract suggesting its thyroid-stimulating role. When the relative potency of each plant extract was calculated in terms of percent increase or decrease in thyroid hormones, as compared to the control value, the decrease in T(3) concentration by A. marmelos was about 62% indicating its possible use in the regulation of hyperthyroidism. B. monnieri could increase T(4) concentration by 41% without enhancing hepatic lipid peroxidation (LPO) suggesting that it can be used as a thyroid-stimulating drug. In fact, hepatic LPO was decreased and superoxide dismutase (SOD) and catalase (CAT) activities were increased by B. monnieri and A. marmelos leaf extracts showing their antiperoxidative role. It is thus suggested that A. marmelos and A. vera may be used in the regulation of hyperthyroidism, while B. monnieri in hypothyroidism.     

Screening South Indian medicinal plants for antifungal activity against cutaneous pathogens

In this study, twenty-eight South Indian medicinal plants were screened for their anti-fungal activity against six species of fungi (Trichophyton mentagrophytes, T. rubrum, T. soudanense, Candida albicans, Torulopsis glabrata, and C. krusei). Three plant species extracts, Celastrus paniculatus, Eriodendron anfractuosum and Ficus glomerata showed inhibitory activity. An aqueous extract of galls of Terminalia chebula showed inhibitory effects on three dermatophytes (Trichophyton spp.) and three yeasts (Candida spp.). Seeds extract of T. chebula inhibited only the growth of T. glabrata. An aqueous extract of T. chebula showed inhibitory effects higher than those measured in ethanol extracts. It is therefore suggested that tannins are plausible candidates for the anti-dermatophytic effects of T. chebula. Chebulinic acid, a known tannin of T. chebula was tested and found not inhibitory, thus a search for the active compound is needed.