Evaluation of antipyretic activity of Calotropis gigantea (Asclepiadaceae) in experimental animals

The roots of Calotropis gigantea have been used in leprosy, eczema, syphilis, elephantiasis, ulceration and cough in the Indian system of traditional medicine. The present communication evaluated its antipyretic activity by using yeast-induced and TAB (Typhoid) vaccine-induced pyrexia in rats and rabbits. In both yeast-induced and TAB vaccine-induced fever, the fever was significantly reduced and the body temperature was normalized by administration of 200 and 400 mg/kg dose intraperitoneally. Based on the results of the present study it can be concluded that the extract of C. gigantea has potential antipyretic activity against both yeast-induced and TAB vaccine-induced fever, indicating the possibility of developing C. gigantea as a cheaper and potent antipyretic agent.     

19-Nor- and 18,20-epoxy-cardenolides from the leaves of Calotropis gigantea

Two new cardenolides (1 and 2) along with 12 known compounds were isolated from the dichloromethane extract of the leaves of Calotropis gigantea. The structural elucidation was accomplished by spectroscopic methods. Some of the isolates were evaluated for cytotoxic activity against KB, BC, and NCI-H187 cancer cell lines, and all cardenolides tested were found to possess strong inhibitory effects. The presence of a deoxysugar at C-3, a formyl group at C-10, and an alpha,beta-unsaturated gamma-lactone was crucial for cytotoxic activity.     

Anti-diarrhoeal activity of the latex of Calotropis procera

The dry latex (DL) of Calotropis procera (Asclepiadaceae), a potent anti-inflammatory agent has been evaluated for anti-diarrhoeal activity. Like atropine and phenylbutazone (PBZ), a single oral dose of DL (500 mg/kg) produced a significant decrease in frequency of defecation, severity of diarrhoea and afforded protection from diarrhoea in 80% rats treated with castor oil. To understand the mechanism of its anti-diarrhoeal activity, we further evaluated its effect on intestinal transit, castor oil induced intestinal fluid accumulation (enteropooling) and electrolyte concentration in the intestinal fluid. DL produced a decrease in intestinal transit (27-37%) as compared to both normal and castor oil treated animals. Unlike atropine, DL significantly inhibited castor oil induced enteropooling. However, it did not alter the electrolyte concentration in the intestinal fluid as compared to castor oil treated rats.     

Antinociceptive activity of Calotropis procera latex in mice

This work evaluated the antinociceptive effect of proteins from the Calotropis procera (Asclepiadaceae) latex using three different experimental models of nociception in mice. The latex protein fraction administered intraperitoneally in male mice at the doses of 12.5, 25 and 50 mg/kg showed the antinociceptive effect in a dose dependent manner compared to the respective controls in all assays. Inhibitions of the acetic acid-induced abdominal constrictions were observed at the doses of 12.5 (67.9%), 25 (85%) and 50 (99.5%) mg/kg compared to controls. Latex protein at the doses of 25 (39.8%; 42%) and 50 mg/kg (66.6%; 99.3%) reduced the nociception produced by formalin in the 1st and 2nd phases, respectively, and this effect was not reversed by pretreatment with naloxone (1 mg/kg). In the hot plate test, an increase of the reaction time was observed only at 60 min after the treatment with latex at the doses of 25 (79.5%) and 50 (76.9%) mg/kg, compared to controls and naloxone was ineffective to reverse the effect. It was concluded that the protein fraction derived from the whole latex of Calotropis procera possesses antinociceptive activity, which is independent of the opioid system.     

Evaluation of in vitro schizontocidal activity of plant parts of Calotropis procera--an ethnobotanical approach

Calotropis procera (Ait.) R.Br. commonly known, as 'Arka' is a popular medicinal plant found throughout the tropics of Asia and Africa and is used in many traditional systems of medicine. Important factors of the various parts of this plant have been widely reported. Good record keeping of subjective and objectively recorded cures by practitioners of traditional medicinal system will help in the establishment of the use of C. procera as an antimalarial plant. It has been attempted to see the effect of crude fractions of its flower, bud and roof against a chloroquine sensitive strain, MRC 20 and a chloroquine resistant strain, MRC 76 of Plasmodium falciparum using the Desjardins method and the effectiveness of its fractions compare better with the CQ sensitive strain than the CQ resistant strain in vitro.     

Ethnopharmacology of Calotropis procera flowers

An ethanolic extract of the flowers of Calotropis procera was investigated for anti-inflammatory, antipyretic, analgesic and antimicrobial activities. The plant extract reduced the paw swelling induced by carrageenan by 37%, fever in rats by 40% and showed some weak effect in rats on the writhing induced by acetic acid. The growth of both gram-positive and gram-negative bacteria was significantly inhibited. A dose-dependent effect on prostaglandin release was also observed.     

Anthelmintic activity of Calotropis procera (Ait.) Ait. F. flowers in sheep

The anthelmintic activity of Calotropis (C.) procera flowers in comparison with levamisole was evaluated through in vitro and in vivo studies. In vitro studies revealed anthelmintic effects (P<0.05) of crude aqueous (CAE) and crude methanolic extracts (CME) of Calotropis procera flowers on live Haemonchus (H.) contortus as evident from their mortality or temporary paralysis. For in vivo studies, Calotropis procera flowers were administered as crude powder (CP), CAE and CME to sheep naturally infected with mixed species of gastrointestinal nematodes. Egg count percent reduction (ECR) was recorded as 88.4 and 77.8% in sheep treated with CAE and CP at 3gkg(-1) body weight on day 7 and 10 post-treatment (PT), respectively. CME was least effective resulting in 20.9% reduction in ECR on day 7 PT. It was found that Calotropis procera flowers possess good anthelmintic activity against nematodes, yet it was lower than that exhibited by levamisole (97.8-100%). It is suggested that further research on large scale be carried out involving a large number of animals, doses higher than those used in the current study, identification of active principles, and standardization of dose and toxicity studies for drug development.     

Putrescine bisamides from Aglaia gigantea

Phytochemical analysis of the leaves of Aglaia gigantea collected in Vietnam yielded three cinnamoyl putrescine bisamide derivatives, which included the known compound dasyclamide ( 1), as well as two new natural products, gigantamide A ( 2) and grandiamide D ( 3). In this study, the structure of dasyclamide ( 1) was confirmed by X-ray crystallography. The structures of the two new alkaloids, gigantamide A ( 2) and grandiamide D ( 3), were elucidated through extensive 1D and 2D NMR spectroscopy and analysis of their mass spectrometric (ESIMS, HRQTOFMS) data. The absolute configuration of grandiamide D ( 3) was determined via Mosher ester derivatization.     

Antinociceptive and antiarthritic activity of Cissampelos pareira roots

In the present study, 50% aqueous ethanolic extract of Cissampelos pareira (Menispermaceae) roots (C. pareira) at the dose levels of 100-400 mg/kg, once daily for 3 days exhibited significant (P < 0.001) resistance against mechanical pain after 30 min in analgesymeter induced pain in mice. In acetic acid (0.6%; i.p.) inducing writhing, Cissampelos pareira significantly (P < 0.05) decreased the writhing episodes; the degree of percent protection at 200 and 400 mg/kg was 22.73 and 51.63. The hot plate reaction time was increased by 2.07 (P < 0.05) and 2.70 (P < 0.001) folds. respectively. Further Cissampelos pareira showed the dose dependent significant protective effect against complete Freund's adjuvant induced arthritis. The percentage protection on the 18th day was 40.54 (P < 0.01) and 71.52 (P < 0.001) at 200 and 400 mg/kg respectively. Lysosomal enzymes (acid phosphatase and N-acetyl glucosaminidase) were decreased by 50% (P < 0.01) and 26.26% (P < 0.05) by using Cissampelos pareira, dextramethasone decreased them 56.56% (P < 0.01) and 31.82% (P < 0.01) and the glycoprotein contents (total hexose and sialic acid) were increased by 1.55-folds (P < 0.01) and 1.51-folds (P < 0.05) by using Cissampelos pareira while dextramethasone increases them by 1.51-folds (P < 0.001) and 1.60-folds (P < 0.01) respectively in stomach homogenate with respect to arthritic group. The increased pain threshold and protective effect against CFE by Cissampelos pareira vindicated its medicinal value in treatment of pain and arthritis.     

Antidiarrhoeal activity of the aqueous extract of Terminalia avicennoides roots

The antidiarrhoeal effects of the aqueous root extract of Terminalia avicennoides were evaluated in rodents. Studies were carried out on the isolated rabbit jejunum, gastrointestinal motility in vivo and on castor oil-induced diarrhoea in mice. The results revealed that the extract exhibited a concentration-dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum and attenuated acetylcholine induced contractions. The extract (100, 200 and 400 mg/kg) also caused a dose-dependent decrease of gastrointestinal transit and markedly protected mice against castor oil-induced diarrhoea. The intraperitoneal LD(50) of the extract was found to be 871.4-917.4 mg/kg in mice (95% confidence). A preliminary phytochemical screening of the aqueous extract of T. avicennoides roots revealed the presence of tannins, saponins and flavonoids. The results obtained showed that the water extract of T. avicennoides roots may contain some biologically active principles that may be active against diarrhoea and this may be the basis for its use traditionally for gastrointestinal disorders.     

Evaluation of antiasthmatic activity of Clitoria ternatea L. roots

Aim of study

Clitoria ternatea L. (Family: Fabaceae) is being used in traditional medicine for the treatment of severe bronchitis and asthma. So the aim of study was to evaluate antiasthmatic activity of ethanol extract of Clitoria ternatea roots.

Materials and methods

In the present study ethanol extract of Clitoria ternatea root (ECTR) was evaluated for preliminary phytochemical screening, acute toxicity studies and antiasthmatic activity using milk induced leucocytosis and eosinophilia in mice, egg albumin induced mast cell degranulations in rats and passive cutaneous anaphylaxis in rats at doses (100-150 mg/kg ip).

Results

The results of present investigation showed that the LD₅₀ of ECTR is more than 1300 mg/kg. ECTR significantly decreases milk induced leucocytosis and eosinophilia, protects egg albumin induced degranulations of mast cells in mice and inhibits area of blue dye leakage in passive cutaneous anaphylaxis in rats at (100-150 mg/kg, i.p.). Phytochemical studies observed the presence of steroids, saponin, flavonoids, and glycosides.

Conclusion

The present investigation concludes that the antiasthmatic activity of ECTR may be due to the presence of flavonoids or saponins.     

Anti-inflammatory activity of Jatropha curcas roots in mice and rats

Anti-inflammatory activity of topical application of Jatropha curcas L. root powder in paste form in TPA-induced ear inflammation was confirmed in albino mice and the successive solvent extraction of these roots was carried out by ether and methanol. The methanol extract exhibited systemic and significant anti-inflammatory activity in acute carrageenan-induced rat paw edema. It also showed activity against formalin-induced rat paw edema, as well as, turpentine-induced exudative changes and cotton pellet-induced granular tissue formation after oral treatment for 7 days in albino rats. Thus, resultant anti-inflammatory activity might be due to effects on several mediators and arachidonic acid metabolism involving cyclo-oxygenase pathway resulting in prostaglandin formation, anti-proliferative activity leading to reduction in granular tissue formation and leukocyte migration from the vessels.     

Anti-inflammatory activity of flavonoids from Cayaponia tayuya roots

Ethnopharmacological relevance

Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia.

The aim of the study

We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators.

Material and methods

The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis.

Results

The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5 mg/ear) inhibited the oedema by 66% (4.2 ± 0.6 mg vs. 12.3 ± 1.4 mg, P < 0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5 mg/ear × 7 applications (7.5 ± 0.6 mg vs. 11.9 ± 1.3 mg, P < 0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 μg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 μg/mL, the flavonoid-enriched fraction had no effect on TNF-α production. In addition, at 22.30 μg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.

Conclusion

These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.     

Antioxidant activity of Tinospora cordifolia roots in experimental diabetes.

We made an attempt to study the antioxidant properties of Tinospora cordifolia roots, an indigenous plant used in Ayurvedic medicine in India in alloxan diabetic rats. Oral administration of an aqueous T. cordifolia root extract (TCREt) (2.5 and 5.0 g/kg) for 6 weeks resulted in a decrease in the levels of plasma thiobarbituric acid reactive substances, ceruloplasmin and alpha-tocopherol in alloxan diabetic rats. The root extract also causes an increase in the levels of glutathione and vitamin C in alloxan diabetes. The root extract at a dose of 5.0 g/kg showed the highest effect. The effect of TCREt was more effective than glibenclamide. Insulin restored all the parameters to near normal levels.     

巨柏茎叶的萜类成分（英文）

目的：对巨柏（Cupressus gigantea）茎叶的化学成分进行研究。方法：采用硅胶和 Sephadex LH-20 柱色谱的方法分离和纯化化合物, 通过 NMR, MS 及理化性质鉴定化合物结构。结果：从巨柏茎叶分离得到 15 个 labdane-type二萜, 其中一个为新化合物, 分别为：15-methoxy-18-hydroxylabda-8（17）,13-diene （1）, 13-epitoruolsol （2）, labd-8（17）,14-dien-13-ol （3）, 13-epi-cupressic acid （4）, cis-communic acid （5）, trans-communic acid （6）, labd-15-aceoxy-8（17）,13E-dien （7）, labd-8（17）,13E-dien-15-ol （8）, isocupressic acid （9）, acetylisocupressic acid （10）, isoabienol （11）, 13-oxo-14,15-dinor-labd-8（17）-en-19-oic acid （12）, pimarenic acid （13）, sandaracopimaric acid （14）, and pimarol （15） 此外还有两个已知倍半萜 ent-oplopanone （16） 和 （＋）-T-Cadinol （17）。结论：化合物（1）为新的倍半萜, 所有化合物均为首次从该植物中分得。     

Pharmacological studies on aerial parts of Calotropis procera.

The decoction of the aerial part of Calotropis procera is commonly used in Saudi Arabian traditional medicine for the treatment of variety of diseases including fever, joint pain, muscular spasm and constipation. The present investigation was undertaken to confirm its claimed activity in traditional medicine. The ethanol extract of the plant was tested on laboratory animals for its antipyretic, analgesic, anti-inflammatory, antibacterial, purgative and muscle relaxant activities. The results of this study showed a significant antipyretic, analgesic and neuromuscular blocking activity. On smooth muscle of guinea pig ileum, the extract produced contractions which was blocked by atropine supporting its use in constipation. The extract failed to produce significant anti-inflammatory and antibacterial activities. Our phytochemical studies on the aerial parts of C. procera showed the presence of alkaloids, cardiac glycosides, tannins, flavonoids, sterols and/or triterpenes. However, the chemical constituents responsible for the pharmacological activities remains to be investigated. The safety evaluation studies revealed that the use of extract in single high doses (up to 3 g/kg) does not produce any visible toxic symptoms or mortality. However, prolong treatment (90 days) causes significantly higher mortality as compared to control group.     

The antimicrobial activity of roots of Jatropha podagrica (Hook)

Hexane, chloroform and methanol extracts of the rootwood and rootbarks of Jatropha podagrica were studied for their antimicrobial activity against 18 organisms. All the extracts exhibited some broad spectrum antibacterial activity, at a concentration of 20 mg/mL. The hexane extracts were generally more active than the chloroform and methanol extracts. The hexane extract of the yellow rootbark was the most active of all the extracts and its activity was comparable to that of gentamycin but better with regard to the control of S. aureus and B. cereus. Three of the extracts, hexane extract of the yellow rootbark and hexane and methanol extracts of the rootwood showed moderate antifungal activity against the yeast fungus, Candida albicans.     

Polyhydroxylated sterols from the octocoral Dendronephthya gigantea

Two new polyhydroxylated sterols, dendronesterols A (1) and B (2), have been isolated from the octocoral Dendronephthya gigantea. The structures of 1 and 2 were proposed on the basis of extensive NMR experiments. Compound 2 was found to be weakly cytotoxic toward L1210 cells.     

Anxiolytic activity of Panax ginseng roots: an experimental study.

The putative anxiolytic activity of the white and red varieties of ginseng, the root of Panax ginseng, was investigated in rats and mice using a number of experimental paradigms of anxiety and compared with that of diazepam. Pilot studies indicated that single-dose administration of ginseng had little to no acute behavioural effects, hence the two varieties of ginseng were administered orally at two dose levels twice daily for 5 days, while diazepam (1 mg/kg, i.p.) was administered acutely. White and red varieties of ginseng (20 and 50 mg/kg) showed positive results when tested against several paradigms of experimental anxiety. Both were effective in the open-field and elevated plus-maze tests and reduced conflict behaviour in thirsty rats and footshock-induced fighting in paired mice. Ginseng also attenuated pentylenetetrazole-induced decrease in rat brain MAO activity, confirming its anxiolytic activity since this has been proposed to be an endogenous marker for anxiety. The effects induced by white and red ginseng (50 mg/kg x 5 days) were comparable to those induced by diazepam (1 mg/kg).     

Volatiles with antimicrobial activity from the roots of Greek Paeonia taxa

The traditional uses of the roots of Paeonia taxa are described. The volatile constituents, obtained by steam distillation of the roots of Paeonia clusii Stern subsp. clusii, Paeonia mascula L. subsp. hellenica and Paeonia parnassica, were studied by GC/MS. Salicylaldehyde, paeonol, methyl salicylate and benzoic acid were found to be the major components among the twelve constituents identified. The evaluation of the in vitro antimicrobial activity of the volatile compounds against six bacteria and three fungi is also reported.