Repeated-dose toxicological studies of Tithonia diversifolia (Hemsl.) A. gray and identification of the toxic compounds

Ethnopharmacological relevance

Tithonia diversifolia (Hemsl.) A. Gray has been commonly used in folk medicine to treat abscesses, microbiological infections, snake bites, malaria and diabetes. Both anti-inflammatory and anti-malarial properties have been identified using appropriate assays, but the effective doses have demonstrated toxic effects for the experimental animals. Most of the pharmacological activities have been attributed to sesquiterpene lactones (STLs) and some chlorogenic acid derivatives (CAs) in the leaves of this species. This work aimed to evaluate the repeated-dose toxicity of an aqueous extract (AE) from Tithonia diversifolia leaves and to compare the results with an extract rich in STLs (LRE) and a polar extract (PE) without STLs but rich in CAs. The purpose of this work was to provide insights into the identity of the compounds responsible for the toxic effects of Tithonia diversifolia.

Materials and methods

The major classes of compounds were confirmed in each extract by IR spectra and HPLC-UV-DAD profiling using previously isolated or standard compounds. The toxicity of each extract was evaluated in a repeated-dose toxicity study in Wistar rats for 90 days.

Results

The AE is composed of both STLs and CAs, the LRE is rich in STLs, and the PE is rich in CAs. The AE caused alterations in haematological parameters but few alterations in biochemical parameters and was relatively safe at doses lower than 100 mg/kg. However, the PE and LRE demonstrated several adverse effects by damaging the liver and kidneys, respectively.

Conclusion

STLs and CAs can be toxic in prolonged use at higher doses in extracts prepared from Tithonia diversifolia by affecting the kidneys and liver.     

Antimalarial compounds from the aerial parts of Flacourtia indica (Flacourtiaceae)

Aim of the study

In the Comoros Islands, the aerial parts of Flacourtia indica are used in traditional medicine to treat malaria. Because of the important use of this plant, the phytochemistry of the aerial parts was investigated.

Materials and methods

Three compounds were isolated from the decoction of this plant material, Pyrocatechol, Homaloside D and Poliothrysoside. The in vitro antiplasmodial activity on the chloroquine-resistant strain (W2) of Plasmodium falciparum and the cytotoxicity on two complementary human cell lines (THP1, HepG2), of AcOEt extract obtained after liquid/liquid extraction of the decoction and pure compounds, were evaluated.

Results

The Poliothrysoside isolated from the AcOEt extract presented a strong antiplasmodial activity (IC₅₀ = 7.4 μM) and a good selectivity index (>28) similar to chloroquine.

Conclusion

This study reports for the first time antiplasmodial activity for Flacourtia indica, for its AcOEt extract and the three major constituents and confirms its traditional use.     

Screening of plants used in Danish folk medicine to treat depression and anxiety for affinity to the serotonin transporter and inhibition of MAO-A

Ethnopharmacological relevance

A number of plant species are used in Danish folk medicine for treatment of depression and anxiety.

Materials and methods

Aqueous and ethanolic extracts of 17 plant species were tested for affinity to the serotonin transporter and for inhibition of MAO-A—both targets for antidepressive treatment.

Results

An ethanolic extract of aerial parts of Borago officinalis had affinity to the serotonin transporter. Ten extracts, from eight plants, had IC₅₀ values below 25 μg/ml extract in the MAO-A assay. The most active extracts in the MAO-A assay were the ethanol extract of seeds of Trigonella foenum-graecum (IC₅₀ 4 μg/ml); ethanol extract of leaves of Apium graveolens (IC₅₀ 5 μg/ml) and the water extract of aerial parts of Calluna vulgaris (IC₅₀ 8 μg/ml).

Conclusions

Besides Borago officinalis, which toxicity profile excludes it from further development as an herbal drug, none of the plants had potential as serotonin reuptake inhibitors. Several plants had MAO-A inhibitory activity.     

Antiplasmodial and cytotoxic activities of Rwandan medicinal plants used in the treatment of malaria

Aim of the study

In our study, methanol, dichloromethane and aqueous extracts of 13 Rwandan medicinal plants used in the treatment of malaria were tested for in vitro antiplasmodial activity.

Materials and methods

The growth inhibition of chloroquine-sensitive Plasmodium falciparum strain (3D7) was evaluated using the measurement of lactate dehydrogenase activity. The active extracts were also tested against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity assay using human normal foetal lung fibroblasts (WI-38).

Results

The majority of the plants tested showed an antiplasmodial activity and the best results were observed with dichloromethane leaf and flower extracts of Tithonia diversifolia, leaf extract of Microglossa pyrifolia and root extract of Rumex abyssinicus, methanol leaf extract of Fuerstia africana, root bark extracts of Zanthoxylum chalybeum and methanol bark extract of Terminalia mollis. Those extracts were active (IC₅₀ < 15 μg/ml) on both chloroquine-sensitive and resistant strains of Plasmodium falciparum. Zanthoxylum chalybeum, Solanecio mannii and Terminalia mollis presented the best selectivity index.

Conclusions

The traditional use of most of the plant evaluated was confirmed by the antiplasmodial test. This study revealed for the first time the antiplasmodial activity of two plants: Terminalia mollis and Rumex abyssinicus.     

Hepatoprotective and toxicological assessment of an ethnomedicinal plant Euphorbia fusiformis Buch.-Ham.ex D.Don

Aim of the study

The tubers of Euphorbia fusiformis Buch.-Ham.ex D.Don (Euphorbiaceae) are traditionally used in India by the Malayali tribes of Chitteri hills, Eastern Ghats, Tamil Nadu to treat liver disorders. The objective of the present study was to assess the hepatoprotective potential and biosafety of Euphorbia fusiformis tuber upon administration thereby justifying the traditional claims.

Materials and methods

The hepatoprotective potential of the ethanol extract of Euphorbia fusiformis tuber against rifampicin induced hepatic damage was investigated in Wistar albino rats. The acute and subchronic toxicity were assessed in mice and rats, respectively.

Results

The ethanol extract of tubers (250 mg/kg p.o.) showed remarkable hepatoprotective effect against rifampicin induced hepatic damage in Wistar albino rats. The degree of protection was measured using the biochemical parameters serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), gamma glutamyl transpeptidase (GGTP), alkaline phosphatase (ALP), total bilirubin and total protein. Treatment with ethanolic extract prior to the administration of rifampicin significantly (P < 0.05 to P < 0.001) restored the elevated levels of the said parameters on a par with the control group. The single dose LD₅₀ was found to be 10,000 mg/kg bw when administered orally in mice. Subchronic toxicity studies in rats with oral doses of 125, 250 and 500 mg/kg exhibited no significant changes in body weight gain, general behavior, hematological and biochemical parameters. The histological profile of liver and kidney also indicated the non-toxic nature of this drug.

Conclusion

The ethanol extract of Euphorbia fusiformis tubers may have potential therapeutic value in the treatment of liver disorders and is safer to use even at higher doses when taken orally.     

In vivo antimalarial activities of Enantia polycarpa stem bark against Plasmodium berghei berghei in mice

Ethnopharmacological relevance

Enantia polycarpa (PC) Engl. Et Diels (Annonaceae) is used in traditional medicine as an antimalarial remedy in Southern Nigeria.

Aim of the study

The antimalarial activities of ethanolic stem bark extracts of Enantia polycarpa was studied in vivo, in mice infected with Plasmodium berghei berghei.

Materials and methods

The ethanolic stem bark extract of Enantia polycarpa was administered at doses ranging from 200 to 600 mg/kg/day to Plasmodium berghei infected mice in both early and established models of antiplasmodial studies.

Results

The extract of Enantia polycarpa exhibited promising antimalarial activity against both early and established infections. At a dose of 600 mg/kg the extract achieved a 75.8% and 72% chemosuppression of parasitaemia in the study of acute and established infections, respectively. The extract also prolonged mean survival time of Plasmodium berghei infected mice during the study of established infection. The mean survival time of mice administered Enantia polycarpa extract at 600 mg/kg/day (27 days) was significantly longer than infected/untreated control (12 days). For the acute toxicity study the extract had an intraperitoneal LD₅₀ of 186 mg/kg but caused no mortality when administered orally at doses as high as 2,000 and 4,000 mg/kg.

Conclusions

Collectively, the results indicate that Enantia polycarpa is safe when administered orally and possesses promising antimalarial activity, thus supporting its use in traditional medicine for the treatment of malaria.     

Fertility inducing effect of aerial parts of Coccinia cordifolia L. in female rats

Ethnopharmacological relevance

The aerial parts of Coccinia cordifolia L. are used to treat female infertility in West Bengal state of India.

Aim of the study

The present study was undertaken to evaluate the fertility inducing effect of aerial parts of Coccinia cordifolia L. in female rats.

Materials and methods

The effect of aqueous extract of Coccinia cordifolia L. on hyperprolactinemia induced infertility, endometriosis induced infertility and androgen-induced infertility was studied. The effect on serum estrogen level, serum progesterone level and reproductive tract was also evaluated in normal healthy female rats. The extract was administered orally at two different doses of 500 mg/kg and 1000 mg/kg.

Results

In hyperprolactinemia induced infertility model, the numbers of uterine implants were almost 10 times more in the extract treated groups as compared to control. The high dose of extract also produced a significant increase in serum estrogen levels (p < 0.01) and number of corpus luteum (p < 0.05) in healthy female rats. The extract at both doses was effective in reducing the weight of endometrial implants by 70–80%, but failed to induce fertility in rats with endometriosis. The extract was ineffective in inducing fertility in androgen-induced infertility model.

Conclusions

The aqueous extract of Coccinia cordifolia L. induces fertility in hyperprolactinemia induced infertility model in female rats.     

Substantiation of the ethnopharmacological use of Conyza sumatrensis (Retz.) E.H.Walker in the treatment of malaria through in-vivo evaluation in Plasmodium berghei infected mice

Ethnopharmacological relevance

Scientific validation of ethnopharmacologically used plants and their utilization for therapeutic interventions can be a source of affordable treatment especially for neglected diseases in endemic areas. Conyza sumatrensis is a plant which finds its use in treating malaria like fevers but lacks proper scientific validation. Our study has tried to address this gap by authenticating its traditional use for the treatment of malaria.

Aim of the study

Evaluate the antimalarial activity of extracts derived from Conyza sumatrensis for its ethnopharmacological validation.

Materials and methods

Shade dried leaves were extracted with varying concentrations of ethanol and concentrated for bio-evaluation. Swiss albino mice infected with 1×10⁶ parasitized red blood cells, were orally administered with test extracts for 7 days in two sets of experiments. The first set was used to evaluate alcoholic, hydroalcoholic and aqueous extracts while the second set was used to evaluate the dose response of alcoholic extract ranging from 500–1600 mg/kg. Mean survival time, parasitaemia and haemoglobin levels were considered to interpret the antimalarial potential. Phytochemical analysis for the presence of flavonoids, alkaloids tannins, total phenolics, riboflavin and thiamine was also carried out.

Results

Among the three extracts administered at 1000 mg/kg, chemo suppression was significantly (p<0.001) observed in the alcoholic extract (62.59±12.52%) followed by hydroalcoholic (41.81±19.04%, p<0.01) and aqueous (32.04±19.04%, P<0.05) indicating that the active constituents leach out in ethanol. The dose response study involving the ethanol extract concluded the optimum dose to be 1000 mg/kg, as also evidenced by the haemoglobin levels.

Conclusion

The plant exhibits moderate antimalarial activity which can be further prospected for active fractions or pure molecules for adjunctive therapy.     

Pharmacological and toxicological effects of Paronychia argentea in experimental calcium oxalate nephrolithiasis in rats

Aim of the study

Renal protection and antiurolithiasic effects of two extracts of Paronychia argentea (PA), a traditional Algerian plant commonly known as Algerian tea, were evaluated. This study was carried out to determine whether the aqueous extract (APA) or the butanolic extract (BPA) of aerial parts could prevent or reduce calculi aggregation in experimental calcium oxalate (Ox) nephrolithiasis in Wistar rats.

Materials and methods

The two extracts (APA and BPA) were administrated orally and daily, during 28 days to nephrolithiasic treated rats at the dose of 250, 500 mg/kg b.w. and 10, 20 mg/kg b.w. respectively.Body weight, renal index, liver index, serum level of creatinine, uric acid, urea, K⁺, Ca²⁺, Mg²⁺, Na⁺ and transaminase (alanine aminotransferase, ALT; aspartate aminotransferase, AST), phosphatase alkaline activity (PAL) were evaluated following the 28 days treatment in rats. In addition histopathological changes in kidney and liver were stained in hematoxylin eosin (HE).

Results

The effect of the extracts could be advantageous in preventing urinary stone retention by reducing renal necrosis and thus inhibit crystal retention. In contradiction with APA, the two doses of BPA attenuated elevation in the serum creatinine (p < 0.01) and blood urea levels (p < 0.01) (nephroprotective effect). However, the increase in ALT (27%) and PAL (31–51%) serum levels and in the relative liver weights (p < 0.01) in the groups treated with doses of APA may indicate that this extract has not a hepatoprotective effect against oxalate toxicity.

Conclusions

The presented data indicate that administration of the butanolic extract of aerial parts to rats with NaOx induced lithiasis, and reduced and prevented the growth of urinary stones in experimental calcium oxalate nephrolithiasis in Wistar rats.     

Inhibitory effects of Solidago chilensis Meyen hydroalcoholic extract on acute inflammation

Aim of the study

Alcoholic or hydroalcoholic preparations of the plant Solidago chilensis Meyen (Asteraceae) are employed in popular medicines to treat inflammation.The anti-inflammatory effects of the hydroalcoholic extract of aerial parts of the plant (93% ethanol) were investigated and the main components of the extract were identified.

Materials and methods

Ear oedema was induced in male Wistar rats by topical application of the chloroform fraction of latex-extract from Euphorbia milii. Leukocyte mobilisation was quantified after air-pouch inflammation evoked by oyster glycogen. Leukocyte–endothelial interactions and mast cell degranulation were quantified by intravital microscopy. The extract itself was characterised via HPLC–DAD–MS and HPLC–MS/MS.

Results

Topical (12.5–50 mg/kg) or intraperitoneal (25 or 50 mg/kg) administrations of the extract reduced ear oedema formation (>25% reduction). Intraperitoneal applications of 25 mg/kg of extract inhibited the migration of polymorphonuclear cells into the inflamed cavity (about 50%). In addition, the rolling behaviour and adherence of circulating leukocytes to postcapillary venules of the mesentery network was diminished (50%), but the mast cell degranulation in the perivascular area was not affected. The major components of the extract were identified as caffeoylquinic acid derivatives and the flavonoid rutin.

Conclusions

The data presented herein show local and systemic anti-inflammatory effects of the hydroalcoholic extract of aerial parts of Solidago chilensis, and implicate the inhibition of leukocyte–endothelial interactions as an important mechanism of the extract's action.     

Sesquiterpene lactones with antinociceptive and antipyretic activity from two Centaurea species

Ethnopharmacological relevance

Several Centaurea species are used to alleviate pain and inflammatory symptoms in rheumatoid arthritis, high fever, and head ache in Turkish folk medicine.

Aim of the study

The effectiveness of extracts, fractions and subfractions from dried Centaurea solstitialis L. subsp. solstitialis (CSS) (Asteraceae) roots and aerial parts were studied on mice.

Materials and methods

The antinociceptive and antipyretic effects of Centaurea solstitialis L. subsp. solstitialis have been investigated by using p-benzoquinone-induced writhing reflex for antinociceptive activity and Freund's Complete Adjuvant-induced pyrexia model for antipyretic activity assessment in mice.

Results

The ethanolic extract from the aerial parts of the plant was shown to possess significant antinociceptive (p < 0.01) and antipyretic activities (p < 0.01). The extract was then submitted to subsequent solvent extractions and chromatographic processes. Through bioassay-guided fractionation and isolation procedures two sesquiterpene lactones, solstitialin A and acetyl solstitialin, were isolated and defined as the active components of CSS. On the other hand, a comparative study was conducted on another species, Centaurea depressa Bieb., which has no similar folkloric utilization. Following the same fractionation chart same compounds were defined as the active ingredients.

Conclusion

Results of the present study proved that aerial part of CSS possesses antinociceptive and antipyretic activities supporting the folkloric assertion in Turkish folk medicine. However, these effects seem not limited to CSS, some other Centaurea species, in fact, having no folkloric use might be equally active.     

Anti-hyperglycemic effect,inhibition of inflammatory cytokines expression,and histopathology profile in streptozotocin-induced diabetic rats treated with Arracacia tolucensis aerial-parts extracts

Ethopharmacological relevance

Arracacia tolucensis is a medicinal plant used in northeast of Mexico as a remedy to treat people with Diabetes mellitus (DM); however, there are no scientific studies that support this information. Thus, we evaluated the anti-hyperglycemic effect of the hexane, ethyl acetate and ethanol extracts from aerial parts in streptozotocin-induced diabetic rats.

Materials and methods

DM was induced in Wistar male rats by single intraperitoneal injection of streptozotocin (STZ 50 mg/kg). After STZ-induction, hyperglycemic rats were treated with all three extracts orally at a single dose (250 mg/kg) each 48 h for 21 days. Glibenclamide (1 mg/kg) was used as a reference drug. The fasting blood glucose levels, the hematic biometry and biochemical profiles, and the inhibition of inflammatory cytokines expression were estimated. Histopathology analysis of pancreas, liver, spleen, and kidney tissue was carried out.

Results

Ours results showed that ethyl acetate extract decreased blood glucose levels significantly (75%, p< 0.05) when compared to diabetic rats and controlled the body weight loss; the lipids level did not change, but the enzyme levels of aspartate aminotransferase and alanine aminotransferase decreased significantly (60.83% and 66.16%, respectively, p< 0.05) and inhibited the expression of inflammatory cytokines,with respect to diabetic rats. Histopathology injury was not observed; by contrast repair of islet of Langerhans was exhibited.

Conclusion

These results validate the use of Arracacia tolucensis as a treatment against DM and suggests it is suitable to continue studies for its safe therapeutic use.     

Gastroprotective activity of the ethanol extract from the inner bark of Caesalpinia pyramidalis in rats

Ethnopharmacological relevance

Caesalpinia pyramidalis Tul. (Fabaceae), known as “catingueira”, has been used in folk medicine in the treatment of various disorders such as gastritis, heartburn, indigestion, and stomach ache. However, the gastroprotective properties of this species have not yet been studied.

Materials and methods

The ethanol extract of Caesalpinia pyramidalis inner bark was used in rats via oral route, at the doses of 30, 100, and 300 mg/kg. The antiulcer assays were performed using the ethanol- and nonsteroidal anti-inflammatory drug-induced ulcer models. Gastric secretion parameters (volume, pH, and total acidity) were also evaluated by the pylorus ligated model, and the mucus in the gastric content was determined. The anti-Helicobacter pylori activity of the ethanol extract of Caesalpinia pyramidalis was performed using the agar-well diffusion and broth microdilution methods.

Results

The ethanol extract (30, 100, and 300 mg/kg) produced dose dependent inhibition (P<0.01) on the ulcer lesion index, the total lesion area, and the percentage of lesion area in the ethanol-induced ulcer model. The ethanol extract (30, 100, and 300 mg/kg) also reduced (P<0.001) the ulcer index in the indomethacin-induced ulcer model. In the model ligature pylorus, the treatment with Caesalpinia pyramidalis ethanol extract failed to significantly change the gastric secretion parameters. However, after treatment with the ethanol extract of Caesalpinia pyramidalis (30, 100, and 300 mg/kg), there was a significant increase (P<0.05) in mucus production. The ethanol extract showed anti-Helicobacter pylori activity, with inhibition halos of 12.0±1.7 mm at 10,000 μg/mL. The minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values of the ethanol extract were of 625 and 10,000 μg/mL, respectively.

Conclusions

Collectively, the present results suggest that the ethanol extract of Caesalpinia pyramidalis displays gastroprotective actions, supporting the folkloric usage of the plant to treat various gastrointestinal disturbances.     

Studies on neuropharmacological profile of ethanol extract of Moringa oleifera leaves in mice

Ethnopharmacological relevance

Moringa oleifera (family Moringaceae), commonly called Horseradish or tree of life, is traditionally used for the treatment of epilepsy and neurologic conditions.

Aim of the study

The objective of this study is to investigate the neurobehavioural and anticonvulsant properties of the ethanol extract from the leaves of Moringa oleifera.

Materials and methods

Neurobehavioural properties were evaluated using the open field, hole board, Y-maze, elevated plus maze (EPM) and pentobarbitone-induced hypnosis. Pentylenetetrazole (leptazol), picrotoxin and strychnine induced convulsion tests were used to investigate the anti-convulsive actions of Moringa oleifera.

Results

The result showed that the extract (250–2000 mg/kg) caused a significant dose-dependent decrease in rearing, grooming, head dips and locomotion (P<0.001). It also enhanced learning and memory and increased anxiogenic effect. In addition, the extract (2000 mg/kg) protected mice against pentylenetetrazol induced convulsion, but has no effect on picrotoxin and strychnine induced convulsion. The effects of the extract in the various models were comparable to those of the standard drugs used except in Y-maze, EPM and picrotoxin and strychnine induced convulsion. The LD₅₀ obtained for the acute toxicity studied using oral route of administration was >6.4 g/kg.

Conclusion

The findings from this study suggest that the ethanol extract of Moringa oleifera leaves possesses CNS depressant and anticonvulsant activities possibly mediated through the enhancement of central inhibitory mechanism involving release γ-amino butyric acid (GABA). The results partially justified the traditional use of the extract for the treatment of epilepsy.     

Effects of ethanolic dried leaf extract of Lecaniodiscus cupanioides on antioxidant enzymes and biochemical parameters in rats

Ethnopharmacological relevance

Lecaniodiscus cupanioides is widely used in West African folk medicine for the treatment of inflammatory conditions, fevers and bacterial infections.

Aim of the study

To evaluate the potential toxic effects of the ethanolic dried leaf extract of Lecaniodiscus cupanioides (LC) on antioxidant enzymes in selected organs and biochemical parameters.

Materials and Methods

Crude ethanolic extract of Lecaniodiscus cupanioides dried leaves was prepared. A 90-day sub-chronic toxicity study was conducted using albino rats. Reconstituted Lecaniodiscus cupanioides was administered at a dosage of 400, 800 and 1600 mg/kg (high dose) with a control group receiving 10 ml/kg orally. Histopathological studies of major organs and blood chemistry analysis were performed on blood obtained via cardiac puncture after euthanization. Selected organs (liver, kidney and brain) were harvested for antioxidant and histopathological assessments.

Results

The extract produced significant (p<0.05) increases in the weights of liver, kidney and brain at 800 mg/kg and 1600 mg/kg compared to the control. Biochemical analysis showed significant increase in Alanine transferase (ALT) at 800 mg/kg and 1600 mg/kg. Assay for antioxidant enzymes showed a reversible decrease in the activity of Catalase (CAT), Superoxide dismutase (SOD) and Glutathione (GSH) with an increase in Malondialdehyde (MDA) at 800 mg/kg and 1600 mg/kg Lecaniodiscus cupanioides. Histopathological study showed reversible congestion in the brain, liver, and kidney at 800 mg/kg and 1600 mg/kg.

Conclusion

Findings in this study reveal that the ethanolic dried leaf extract of Lecaniodiscus cupanioides has the potential for inhibiting in vivo antioxidant enzymes activity and causing hepatotoxicity after prolonged exposure.     

Citrus limetta leaves extract antagonizes the hypertensive effect of angiotensin II

Ethnopharmacological relevance

Citrus limetta Risso (Rutaceae) is widely used in Mexico for healing purposes, among them as antihypertensive treatment.

Aim of the study

To assess the antihypertensive effect of C. limetta leaves as one of its ethnomedical uses.

Materials and methods

The acute response of blood pressure to angiotensin II administration was measured in mice. Additionally, the acute oral toxicity profiles were determined.

Results

The findings of the current investigation showed that different concentrations of the aqueous extract prevented the raise of systolic blood pressure (p ≤ 0.001 vs. vehicle), diastolic blood pressure (p ≤ 0.0002 vs. vehicle) and mean blood pressure (p ≤ 0.0000 vs. vehicle); with a dose dependent effect for diastolic pressures at 125–500 mg/kg dosages. The 500 and 1000 mg/kg doses inhibited the action of Ang II in similar extent to telmisartan. Toxic signs or deaths were not observed in mice treated at 2000 mg/kg of C. limetta extract.

Conclusions

All doses of C. limetta aqueous extract, used in this assay, were safe and effective.     

Anti-inflammatory effects and acute toxicity of hydroethanolic extract of Jacaranda decurrens roots in adult male rats

Ethnopharmacological relevance

Jacaranda decurrens subsp. symmetrifoliolata Farias and Proença (Bignoniaceae) is a species traditionally used for the treatment of inflammatory diseases. However, until this moment, there is no scientific evidence of these effects.

Aim of study

To evaluate the anti-inflammatory effects of hydroethanolic root extract of Jacaranda decurrens in rats and to determine the safe of this plant after acute exposure.

Materials and methods

The acute toxicity of Jacaranda decurrens root extract (EJD) was evaluated by oral administration to male rats as single doses of 0; 500; 1000 or 2000 mg/kg body weight. General behavior and toxic symptoms were observed for 14 days. The anti-inflammatory activity was evaluated in carrageenan-induced inflammatory paw edema and myeloperoxidase activity in male rats.

Results

No signs of acute toxicity were observed, indicating that the LD₅₀ is greater than 2000 mg/kg. EJD (100 and 300 mg/kg) significantly reduced edema formation and at higher dose, the reduction was similar to dexamethasone. A significant decrease in myeloperoxidase activity was also observed.

Conclusions

The present study shows that Jacaranda decurrens extract has anti-inflammatory properties in rats without causing acute toxicity. These properties observed may be due to the presence of bioactive constituents such as ursolic acid.     

Antibacterial and anti-inflammatory activities of extract and fractions from Pyrrosia petiolosa (Christ et Bar.) Ching

Ethnopharmacological relevance

Pyrrosia petiolosa is commonly used as a traditional Chinese medicine for treatment of acute pyelonephritis, chronic bronchitis and bronchial asthma. This study aims to evaluate the antibacterial activity of the ethanol extract and its derived fractions of Pyrrosia petiolosa obtained with solvents of different polarities and to perform the anti-inflammatory screening.

Materials and methods

The powdered aerial parts of Pyrrosia petiolosa were used to extract various fractions with ethanol, petroleum ether, ethyl acetate, N-butanol and aqueous. Qualitative phytochemical screening was performed on the ethanol extract, petroleum ether fraction, ethyl acetate fraction, N-butanol fraction and aqueous fraction. The agar diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were employed to evaluate antibacterial activity of the ethanol extract and fractions. The in vitro cytotoxicity of ethanol extract and fractions was determined using MTT assay. The anti-inflammatory activity was analyzed using the mouse ear swelling induced by xylene.

Results

The phytochemical screening revealed the presence of anthraquinones, flavonoids, terpenoids, steroids, saponins, phenols and reducing sugars in the extract and fractions. Antibacterial results showed that petroleum ether fraction and N-butanol fraction inhibited all the tested microorganisms with the maximum inhibition zone of 15.25±0.35 mm. Ethyl acetate fraction also exhibited good antibacterial activity except Pseudomonas aeruginosa ATCC 27853, while extract and aqueous fraction inhibited 8 out of 13 (61.5%) of the tested microorganisms. The MIC values of ethanol extract and fractions ranged from 1.25 to 10.00 mg/mL and most of the MBC values were equal or twice as high as the corresponding MIC values. The in vitro cytotoxicity showed the ethanol extract and fractions exhibited non-toxic or low toxic activity against lung cancer cell lines A549 and mouse spleen cells. In anti-inflammatory experiment, ethanol extract at 5.0 and 10.0 mg/kg exhibited significant anti-inflammatory activity against the mouse ear swelling induced by xylene and the maximum inhibition rate reached as high as 67%.

Conclusions

Pyrrosia petiolosa could be a potential candidate for future development of a novel antibacterial and anti-inflammatory agent.     

Leucas cephalotes regulates carbohydrate and lipid metabolism and improves antioxidant status in IDDM and NIDDM rats

Ethnopharmacological relevance

Leucas cephalotes (Roth.) Spreng. (Laminaceae) is an ayurvedic traditional medicinal plant used in India, Nepal and Pakistan to treat several ailments including diabetes.

Aim of the study

The aim of the present study is to investigate the antidiabetic, antihyperlipaemic and antioxidant activities of Leucas cephalotes for its purported use in diabetes.

Materials and methods

The ethanol extract of leaves of Leucas cephalotes was administered (150, 300 and 450 mg kg⁻¹ bw) to diabetes induced (IDDM and NIDDM) rats and carbohydrate, lipid, antioxidant, urea and creatinine profiles were assessed.

Results

All the three doses of extract decreased plasma glucose and lipid profiles and, improved the antioxidant status of both types of diabetic rats. The extract administration improved hepatic glycogen content and hexokinase activity, decreased glucose-6-phosphatase activity, blood urea, creatinine contents and decreased lipid peroxidation in diabetic rats. Of the three doses used, 450 mg kg⁻¹ bw dose was found to be more potent in its effects comparable to those of glibenclamide and metformin.

Conclusion

Leucas cephalotes regulates both carbohydrate and lipid metabolism and, improves body antioxidant defense systems in both types of diabetes.     

Qualea parviflora Mart.: An integrative study to validate the gastroprotective,antidiarrheal, antihemorragic and mutagenic action

Ethnopharmacological relevance

Qualea parviflora Mart. is a medicinal species commonly found in the Brazilian Cerrado biome.

Aim of the study

Based on ethnopharmacological data, methanolic extract from Qualea parviflora (QP) bark was evaluated for its antiulcer, analgesic, anti-hemorrhagic, mutagenic and anti-Helicobacter pylori activities.

Material and methods

The gastroprotective action of the extract was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated mutagenic effect (Ames assay), anti-Helicobacter pylori, anti-hemorrhagic action, analgesic and inflammatory effects (hot-plate test and carrageenin-induced hind paw edema) of methanolic extract from Qualea parviflora.

Results

QP (500 mg/kg, p.o.) was able to protect gastric mucosa against HCl/ethanol solution (77%), absolute ethanol (97%), and also against injurious effect of NSAID (36%). When QP was challenged with sulfhydryl depletor compound, the gastroprotective action of extract was abolished. QP treatment was able to maintain the GSH level and show a concentration-dependent inhibition effect on the lipid peroxidation. QP present anti-Helicobacter pylori effect (MIC = 75 μg/mL), anti-hemorrhagic and antidiarrheal action but not present analgesic or anti-inflammatory effect.

Conclusion

methanolic extract from Qualea parviflora had gastroprotective effect related to the increase of gastric mucosa defensive factors such PGE₂ levels and maintain the basal gastric glutathione levels. The methanolic extract also showed anti-Helicobacter pylori activity, anti-hemorrhagic effect and antioxidant action, but absence of analgesic, mutagenic and toxic effects, a profile that adds safety to its use.