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At least 19 recordsLinked to original sources

PubMed2002

Effect of Alstonia scholaris bark extract on testicular function of Wistar rats.

AIM: To evaluate the antifertility effect of Alstonia scholaris bark extract in male rats. METHODS: In male Wistar rats Alstonia scholaris bark extract was given by oral route at a dose of 200 mg/day for 60 days. The fertility and testicular function were assessed by mating tests, sperm motility, sperm concentration, biochemical indices and testicular cell population dynamics. RESULTS: Oral feeding with the extract at a dose of 200 mg/day for the period of 60 days did not cause body weight loss, while the weights of testes, epididymides, seminal vesicle and ventral prostate were significantly reduced. The production of step-19 spermatids was reduced by 79.6% in treated rats. The population of preleptotene and pachytene spermatocytes were decreased by 61.9% and 60.1%, respectively. Spermatogonia and Sertoli cell population were also affected. The seminiferous tubule and Leydig cell nuclear area were reduced significantly (P<0.01) when compared to the controls. Reduced sperm count and motility resulted in a total suppression of fertility. A significant fall in the protein and sialic acid content of the testes, epididymides, seminal vesicle and ventral prostate as well as glycogen content of testes were also noticed. The fructose content in the seminal vesicle was lowered whereas the testicular cholesterol was elevated as compared with the controls. The following compounds were obtained from the extract with chromatographic separation over Si-gel column: agr-amyrin, bgr-amyrin, lupiol acetate, venenative, rhazine and yohimbine. CONCLUSION: At the dose level employed, Alstonia scholaris bark extract has a significant antifertility effect in male rats; the primary site of action may be post meiotic germ cells (Step 19 spermatids).

Administration, Oral↗

PubMed1993

Alstonia species: are they effective in malaria treatment?

A review of the literature on Alstonia species indicates that evidence in support of their effectiveness in the treatment of malaria is controversial. The antiprotozoal activity of the major alkaloid present in Alstonia species, echitamine, was assessed in vitro against Plasmodium falciparum and Giardia intestinalis. Echitamine displayed little antiplasmodial activity, but two quinoline alkaloids from A. coriacea (corialstonine and corialstonidine) were found to have some activity against P. falciparum although this was approximately 10 times less than that of quinine. None of the three Alstonia alkaloids was active against G. intestinalis. These results are discussed in the context of previously published data.

Alkaloids↗

PubMed2005

The effect of seasonal variation on the antineoplastic activity of Alstonia scholaris R. Br. in HeLa cells.

In order to evaluate the seasonal variation as well as cytotoxicity of different fractions of Alstonia scholaris R. Br. (ASE), the HeLa cells were treated with different doses of various fractions of ASE collected in monsoon, winter and summer. The exposure of HeLa cells to different extracts prepared from the stem bark collected in monsoon, winter and summer seasons resulted in a dose dependent increase in the cell killing effect of ASE and the highest cell killing effect was observed for the extract prepared from the summer collections. Similarly, treatment of HeLa cells with different doses of various fractions of the Alstonia scholaris extract viz. residue (ASERS), steroidal (ASEST), chloroform (ASECH), petroleum ether (ASEPE), diethyl ether (ASEDE), ethyl acetate (ASEEA), n-butanol (ASENB), aqueous (ASEAQ) and echitamine chloride (ECL) also resulted in a dose dependent decline in the cell viability, where the greatest cytotoxic effect was observed for residue (ASERS), followed by the whole extract (ASE) and chloroform (ASECH) fraction, while the least activity was observed for the steroidal (ASEST) fraction. The cytotoxicity declined ASERS > ASE > ASECH >ECL > ASEEA > ASEDE > ASEPE > ASENB > ASEAQ > ASEST in order. Our study demonstrates that the extract prepared from the summer collection, and the fractions containing the alkaloids were highly effective in cell killing. The extract of ASE was more powerful than the active principle echitamine present in ASE.

Alstonia↗

PubMed2005

Evaluation of Alstonia scholaris leaves for broncho-vasodilatory activity.

The present study demonstrates that the ethanol extract of Alstonia scholaris (Apocynaceae) leaves induced pronounced bronchodilatory activity in anaesthetized rats with the probable involvement of prostaglandins. However, in vitro preparations of guinea-pig trachea did not confirm this property, indicating that bronchodilation is not due to the direct tracheal smooth muscle relaxation. The vasodilatory activity of the extract was independent of adrenergic or muscarinic receptors or prostaglandins but was mainly via endothelial-derived relaxing factor, nitric oxide. The extract inhibited the spontaneous movements of rabbit jejunum and contractile effects of acetylcholine and histamine on guinea-pig ileum. Additionally, the extract caused marked reduction of barium chloride-, potassium chloride- and calcium chloride-induced contraction on guinea-pig ileum and pulmonary artery, implying a direct interference of plant extract with the influx of calcium ions into cells. However, the extract has no detectable effect on mobilization of intracellular calcium. These results coupled with the in vivo effects of ethanol extract reveal that the Alstonia scholaris leaves possess broncho-vasodilatory activity mediated presumably by prostaglandins, calcium antagonism and endothelium-derived relaxing factor(s).

Alstonia↗

PubMed2003

Induction of developmental toxicity in mice treated with Alstonia scholaris (Sapthaparna) In utero.

BACKGROUND: The teratogenic effect of hydroalcoholic extract of Alstonia scholaris (ASE) was studied in the pregnant Swiss albino mice administered with 0, 60, 120, 240, 360, and 480 mg/kg ASE on Day 11 of gestation. METHODS: Females were allowed to complete the term and parturiate. The litters were monitored regularly for mortality, growth retardation, congenital malformations, and appearance of physiological markers up to 7 weeks post-parturition (p.p.). RESULTS: The administration of 60, 120, 180, and 240 mg/kg ASE to the pregnant mice on Day 11 did not induce mortality, congenital malformations, or alter the normal growth patterns. A further increase in the herbal extract dose up to 360 or 480 mg/kg resulted in a dose dependent increase in the mortality, growth retardation, and congenital malformations, characterized mainly by bent tails and syndactyly. The administration of higher doses (360 or 480 mg) of ASE also caused a significant delay in the morphological parameters such as fur development, eye opening, pinna detachment, and vaginal opening. The incisor eruption and testes decent were found to be delayed in litters born to the mothers treated with 240-480 mg/kg ASE. CONCLUSIONS: Our study indicates clearly that ASE treatment caused teratogenic effect only at doses above 240 mg/kg (>20% of LD(50)). Lower doses had no developmental toxicity.

Abnormalities, Drug-Induced↗

PubMed2006

Evaluation of anticancer activity of the alkaloid fraction of Alstonia scholaris (Sapthaparna) in vitro and in vivo.

The anticancer effect of various doses of an alkaloid fraction of Sapthaparna, Alstonia scholaris (ASERS), was studied in vitro in cultured human neoplastic cell lines (HeLa, HepG(2), HL60, KB and MCF-7) and in Ehrlich ascites carcinoma bearing mice. Treatment of HeLa cells with 25 microg/mL ASERS resulted in a time dependent increase in the antineoplastic activity and the greatest activity was observed when the cells were exposed to ASERS for 24 h. However, exposure of cells to ASERS for 4 h resulted in 25% viable cells and hence this time interval was considered to be the optimum time for treatment and further studies were carried out using this time. Treatment of various cells with ASERS resulted in a concentration dependent decline in the viable cells and a nadir was reached at 200 microg/mL in all the cell lines studied. The IC50 was found to be 5.53, 25, 11.16, 10 and 29.76 microg/mL for HeLa, HePG2, HL60, KB and MCF-7 cells, respectively. Similarly, administration of ASERS, once daily for 9 consecutive days to the tumor bearing mice caused a dose dependent remission of the tumor up to 240 mg/kg body weight, where the greatest antitumor effect was observed. Since 240 mg/kg ASERS showed toxic manifestations, the next lower dose of 210 mg/kg was considered as the best effective dose, in which 20% of the animals survived up to 120 days post-tumor-cell inoculation as against no survivors in the saline treated control group. The ASERS treatment resulted in a dose dependent elevation in the median survival time (MST) and the average survival time (AST) up to 240 mg/kg ASERS and declined thereafter. The surviving animals were healthy and disease free. The effect of ASERS was better than cyclophosphamide, which was used as a positive control, where all the animals succumbed to death by 40 days and the MST and AST were 19.5 and 18.3 days, respectively. The effective dose of 210 mg of ASERS was 3/10 of the LD50 dose, which increased the MST and AST up to 54 and 49.5 days, respectively.

Alkaloids↗

PubMed2005

A potent sperm motility-inhibiting activity of bioflavonoids from an ethnomedicine of Onge, Alstonia macrophylla Wall ex A. DC, leaf extract.

The methanol extract (ME) and the n-butanol fractions of methanolic extract of Alstonia macrophylla Wall ex A. DC leaves were investigated on the forward motility (FM) of mammalian (goat and human) spermatozoa. The ME at 600 microg mL-1 as well as fraction B at 100 microg mL-1 concentrations showed marked inhibition of sperm FM in both goat and human species when tested by microscopic and spectrophotometric methods. Approximately 60-80% of the goat spermatozoa lost their FM when treated with 600 microg mL-1 of ME and 100 microg mL-1 of fraction B. At 100 microg mL-1 concentration, fraction B showed 90% loss of FM in human spermatozoa, while fraction B at 400 microg mL-1 concentration showed complete inhibition of sperm FM at 0 min. The inhibitory activity of fraction B increases with increasing concentration in a dose-dependent manner. Phytochemical study of the extract revealed that the leaf contains tannins, flavonoids, sterols, triterpenes, alkaloids and reducing sugars. Further fractionation and purification of the bioactive n-butanol part of ME showed the presence of ursolic acid (fraction B), beta-sitosterol (fraction A), beta-sitosterol glucoside and a mixture of minor compounds (fraction C, detected on thin-layer chromatography). The results reveal that fraction B (ursolic acid), a pentacyclic triterpene, has the potential of sperm motility inhibition and can serve as a topical vaginal contraceptive.

Alstonia↗

PubMed2004

CNS activity of Alstonia macrophylla leaf extracts: an ethnomedicine of Onge of Bay Islands.

Methanol extract at 100-200 mg/kg p.o. and major nonpolar fraction B at 50 mg/kg of Alstonia macrophylla leaves caused a significant reduction in spontaneous activity, remarkable decrease in exploratory behavioural pattern, a reduction in muscle relaxant activity and also significantly potentiated phenobarbitone sodium-induced sleeping time. The phytochemical study of crude leaf extract revealed the presence of tannin, triterpenoid, flavonoid, sterol, alkaloid and reducing sugars. Further fractionation and purification of the n-butanol part of methanol extract yielded fraction A, fraction B and fraction C along with some minor fatty acids as the major compounds.

Alstonia↗

PubMed2004

Alkaloids from Alstonia angustifolia.

Six new alkaloids, viz., alstolactone, affinisine oxindole, lagumicine, N(4)-demethylalstonerine, N(4)-demethylalstonerinal, and 10-methoxycathafoline N(4)-oxide, in addition to 36 other known alkaloids, were obtained from the leaf extract of Alstonia angustifolia var. latifolia. The structures of the new alkaloids were determined using NMR and MS analysis.

Alkaloids↗

PubMed2005

Indole alkaloids from the leaves of Philippine Alstonia scholaris.

The first seco-uleine alkaloids, manilamine (1) (18-hydroxy-19,20-dehydro-7,21-seco-uleine) and N4-methyl angustilobine B (2), were isolated from the (pH 5) alkaloid extract of Philippine Alstonia scholaris leaves together with the known indole alkaloids 19,20-(E)-vallesamine (3), angustilobine B N4-oxide (4), 20(S)-tubotaiwine (5), and 6,7-seco-angustilobine B (6). The structure of the alkaloids was established from MS and NMR experiments.

Alstonia↗

PubMed2004

The evaluation of the acute toxicity and long term safety of hydroalcoholic extract of Sapthaparna (Alstonia scholaris) in mice and rats.

The acute and sub-acute toxic effects of various doses of hydroalcoholic extract of Alstonia scholaris (ASE) was studied in mice and rats. The acute toxicity in mice depended on the season of collection of plant. The highest acute toxicity was observed in the ASE prepared from the summer collection followed by winter. The least toxicity was observed in the extract prepared from the bark of A. scholaris collected in the monsoon season. The administration of different doses of ASE showed a dose dependent increase in the toxicity in all species of mice. The Swiss albino mice were found to be the most sensitive followed by the DBA and C(57)BL. The crossbred mice were resistant when compared to the pure inbred strains. The oral administration of ASE was non-toxic up to a dose of 2000 mg/kg b. wt., while maximum number of animals succumbed to death after administration of 1100 mg/kg ASE by intraperitoneal route. The rats were more sensitive than the mice as the LD(50) dose of ASE was lesser for the former than the latter. The sub-acute toxicity in the rats was carried out with 120 and 240 mg/kg b. wt. ASE (1/10th and 1/5th of the LD(50) dose of ASE). The 240 mg was observed to be more toxic than 120 mg/kg ASE since it caused mortality and deformity in various organs of the recipient animals. The various biochemical parameters like AST, ALT, ACP, ALP, CK, LDH, creatinine, urea, ammonia, glucose and LPx were higher at 240 mg/kg ASE when compared with the 120 mg and the non-drug treated animals. In contrast, the total protein, albumin, DNA, RNA, cholesterol, glucose, glutathione, total thiols declined in the 240 mg/kg ASE treated animals when compared with non-drug treated controls. The hematological analysis showed a dose dependent decrease in the RBC, WBC, hemoglobin, neutrophils and monocytes, while a significant increase in the lymphocytes, eosinophils and basophils was observed. The observed toxic effect of ASE may be due to the presence of echitamine. Our studies shows that at high doses, A. scholaris exhibited marked damage to all the major organs of the body.

Administration, Oral↗

PubMed2003

Antibacterial activity of Alstonia scholaris and Leea tetramera.

The crude methanolic extracts of the leaves, stem and root barks of Alstonia scholaris and Leea tetramera on partitioning (petrol, dichloromethane, ethyl acetate, butanol) gave fractions exhibiting improved and broader spectrum of antibacterial activity. Especially the butanol fractions of A. scholaris and the root bark of L. tetramera. None of the fractions were active against the fungi tested.

Alstonia↗

PubMed2003

Effect of Sapthaparna (Alstonia scholaris Linn) in modulating the benzo(a)pyrene-induced forestomach carcinogenesis in mice.

The chemopreventive effect of various doses of hydroalcoholic extract of Alstonia scholaris (ASE) was studied on the benzo(a)pyrene (BaP) induced forestomach carcinoma in female mice. The treatment of mice with different doses, i.e. 1, 2 and 4 mg/ml ASE in drinking water before, during and after the treatment with carcinogen, exhibited chemopreventive activity. The highest activity was observed for 4 mg/ml ASE, where the tumor incidence (93.33%) was reduced by 6.67%. Similarly, the tumor multiplicity reduced (61.29%) significantly (P<0.02) at 4 mg/ml in the pre-post-ASE treated group. However, the pre or post-treatment of mice with 4 mg/ml ASE did not show chemopreventive activity. These findings are corroborated by micronucleus assay, where treatment of mice with ASE before, during and after carcinogen treatment reduced the frequency of micronuclei (MN) in the splenocytes in a dose dependent manner. The MN frequency reached a nadir at 4 mg/ml ASE, the highest drug dose which showed maximum chemopreventive action. The ASE treatment not only reduced the frequency of splenocytes bearing one MN but also cells bearing multiple MN indicating the efficacy of ASE in inhibiting mutagenic changes induced by BaP. The pre or post-treatment of mice with 4 mg/ml ASE also significantly reduced the frequency of BaP-induced MN in the splenocytes of treated animals.

Alstonia↗

PubMed2003

The enantiospecific, stereospecific total synthesis of the ring-A oxygenated sarpagine indole alkaloids (+)-majvinine, (+)-10-methoxyaffinisine, and (+)-N(a)-methylsarpagine, as well as the total synthesis of the alstonia bisindole alkaloid macralstonidine.

The first stereospecific, enantiospecific total synthesis of the ring-A oxygenated sarpagine indole alkaloids (+)-N(a)-methylsarpagine (8), (+)-majvinine (14), and (+)-10-methoxyaffinisine (49), as well as the first total synthesis of the Alstonia bisindole alkaloid macralstonidine (9), has been accomplished. This approach employed the Schöllkopf chiral auxiliary for the stereospecific construction of the desired d-(+)-tryptophan unit required for the asymmetric Pictet-Spengler reaction. In addition, the strategy was doubly convergent for the enolate-mediated Pd(0) coupling process and the asymmetric Pictet-Spengler reaction can be employed to synthesize both macroline (2) and N(a)-methylsarpagine (8), the coupling of which provides macralstonidine (9). This approach to ring-A substituted alkoxyindole alkaloids should find wide application for the synthesis of other alkaloids for it is stereospecific and either enantiomer can be prepared with ease.

Alstonia↗

PubMed2005

Actinophyllic acid, a potent indole alkaloid inhibitor of the coupled enzyme assay carboxypeptidase u/hippuricase from the leaves of Alstonia actinophylla (Apocynaceae).

Bioassay-guided fractionation of the aqueous extract of the leaves of Alstonia actinophylla with use of a coupled enzyme assay, CPU/hippuricase, to detect carboxypeptidase U inhibitors led to the isolation of a novel indole alkaloid, actinophyllic acid (1). The structure of 1 was determined from detailed 2D NMR studies. Actinophyllic acid was found to be a potent inhibitor of the coupled enzyme assay with an IC(50) of 0.84 microM. Actinophyllic acid possesses a unique 2,3,6,7,9,13c-hexahydro-1H-1,7,8-(methanetriyloxymethano)pyrrolo[1',2':1,2]azocino[4,3-b]indole-8(5H)-carboxylic acid skeleton.

Alstonia↗

PubMed2004

New indole alkaloids from Alstonia macrophylla.

Ten new indole alkaloids, alstomaline (1), 10,11-dimethoxynareline (2), alstohentine (3), alstomicine (4), 16-hydroxyalstonisine (5), 16-hydroxyalstonal (6), 16-hydroxy-N(4)-demethylalstophyllal oxindole (7), alstophyllal (8), 6-oxoalstophylline (9), and 6-oxoalstophyllal (10), in addition to 21 other known ones, were obtained from the leaf extract of the Malayan Alstonia macrophylla. The structures were determined using NMR and MS analysis.

Acetylation↗

PubMed2004

New indole alkaloids from the bark of Alstonia scholaris.

A new indole alkaloid, akuammiginone (1), and a new glycosidic indole alkaloid, echitamidine-N-oxide 19-O-beta-d-glucopyranoside (2), together with the five known alkaloids, echitaminic acid (3), echitamidine N-oxide (4), N(b)-demethylalstogustine N-oxide (5), akuammicine N-oxide (6), and N(b)-demethylalstogustine (7), were isolated from the trunk bark of Alstonia scholaris collected in Timor, Indonesia. The structures of all compounds were elucidated by spectroscopic methods. This is the first report of compounds 3-5and 7 in A. scholaris. Some NMR assignments of the known compounds were revised.

Alstonia↗

PubMed2002

Evaluation of anti-inflammatory activity of Alstonia macrophylla Wall ex A. DC. leaf extract.

Methanolic extract of dried leaves of Alstonia macrophylla Wall ex A. DC. and its fractions were investigated for its anti-inflammatory activity. The extract at a concentration of 200 mg kg(-1) and 400 mg kg(-1), p.o. and its fractions at 25 mg kg(-1) and 50 mg kg(-1), p.o. showed the significant dose dependent antiinflammatory activity in carrageenan and dextran-induced rats hind paw edema (acute models) as well as in cotton pellet-induced granuloma (chronic model) in rats. Anti-inflammatory activity of the tested extract and its fractions was comparable with that of the standard drug Indomethacin (10 mg kg(-1)).

Acute Disease↗