Cytotoxic and antibacterial triterpenoids derivatives from Clematis ganpiniana

Ethnopharmacological relevance

The roots and rhizomes of Clematis are commonly used as an analgesic, abirritative, antibacterial, antiphlogistic, anticancer and diuretic agent. The Naxi people traditionally used Clematis ganpiniana's (Lévl. Et Vant.) as a diuretic agent, an anti-inflammatory and anticancer remedy.

Aim of study

To investigate the cytotoxic and antibacterial components from Clematis ganpiniana.

Materials and methods

The aboveground part of Clematis ganpiniana was isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods and comparison with published data. Their cytotoxic, apoptosis and antibacterial activities of purified components were also performed.

Results

By bioassay-guided fractionation techniques and chemical characterization, four triterpene glycosides were isolated and their cytotoxicity against cancer cells and antibacterial activity were tested. They showed significant inhibitory activities against MCF-7, MDA-MB-231 with IC50 value of 0.7–16.5 μg/ml, and significant apoptosis for MCF-7 and MDA-MB-231. Moreover, compound 4 showed weak wide-spectrum antibacterial activity.

Conclusion

These results provide promising baseline information for the potential use of Clematis ganpiniana as well as some of the isolated compounds in the treatment of cancer and infectious disease.     

The effect of Salvia divinorum and Mitragyna speciosa extracts,fraction and major constituents on place aversion and place preference in rats

Ethnopharmacological relevance

Consumer use of botanicals has increased despite, in many instances, the paucity of research demonstrating efficacy or identifying liabilities. This research employed the place preference/aversion paradigm to characterize the psychoactive properties of Salvia divinorum extract (10, 30, 100 mg/kg), salvinorin A (0.1, 0.3, 1.0 mg/kg), Mitragyna speciosa MeOH extract (50, 100, 300 mg/kg), Mitragyna speciosa alkaloid-enriched fraction (12.5, 25, 75 mg/kg) and mitragynine (5, 10, 30 mg/kg) in rats.

Material and methods

Following apparatus habituation and baseline preference scores, male Sprague-Dawley rats were given eight counter-balanced drug versus vehicle conditioning trials followed by a preference test conducted under drug-free states. S(+)-amphetamine (1 mg/kg) served as the positive control (in Exp. 2) and haloperidol (0.8, 1.0 mg/kg) served as the negative control in both studies.

Results

Rats displayed place aversion to both Salvia divinorum and salvinorin A that exceeded that of haloperidol. Rats showed place preference to mitragynine that was similar to that of S(+)-amphetamine. This CPP effect was much less pronounced with the Mitragyna speciosa extract and its fraction.

Conclusions

These findings suggest that both botanicals possess liabilities, albeit somewhat different, that warrant caution in their use.     

Antihypertensive activity of Salvia elegans Vahl. (Lamiaceae): ACE inhibition and angiotensin II antagonism

Ethnopharmacological relevance

Salvia elegans Vahl. (Lamiaceae), recognized with the popular name of “mirto” is widely used in Mexico for healing purposes, and also them as antihypertensive treatment.

Aim of the study

The high prevalence of this illness and the side effects of antihypertensive drugs conducted us to the evaluation of the Salvia elegans extract on angiotensin II action.

Materials and methods

The acute response of blood pressure to angiotensin II administration was measured in mice. We also tested in vitro the inhibitory effect on angiotensin convertase enzyme. Additionally, characterization of the pharmacological effect of the extract fraction was obtained.

Results

We obtained dose–response curve for the administration of complete extract and extract fractions. Due to the hydroalcoholic extract (SeHA) treatment blood pressure decreased significantly from systolic dose of 0.75 mg kg⁻¹ (p < 0.05) and even had an antihypertensive effect that was greater than that treatment with losartan. SeHA extract decreased the E_max of the AG II hypertensive effect by about 20% in both systolic and diastolic pressures, treatment with losartan also decreased the same parameter between 6% and 8% for systolic and diastolic pressures, respectively. Fractions SeF8 and SeF8-8 showed similar levels of AG II ED₅₀ for both pressures compared with losartan, these fractions showed major compounds with maximum absorbance peaks at 221, 289 and 330 nm typical of flavonoids. In the inhibition assay the activity of angiotensin converting enzyme (ACE), the extract SeHA showed percentage inhibition (%IACE) of 50.27 ± 5.09% (n = 5). SeBuOH fraction is found to have greater inhibitory capacity of achieving a IACE 78.40 ± 2.24% (n = 5), which was similar to the values obtained in the presence of the SeF8-22 fraction (82.61 ± 1.74%) and lisinopril (87.18 ± 1.16%). The changes in the value of K_M suggest that components of the extracts and fractions were recognized by the enzyme's active site. The main compounds of the fractions SeBuOH, SeF8-22 were by flavonoid and phenyl propanoid types, according to UV absorption spectra of the fractions.

Conclusions

The experimental results demonstrated the antihypertensive effect of Salvia elegans and it was due to the AG II antagonism and inhibition of angiotensin converting enzyme.     

Appraisal of scopolamine-induced antiamnesic effect in mice and in vitro antiacetylcholinesterase and antioxidant activities of some traditionally used Lamiaceae plants

Ethnopharmacological relevance

Salvia species and Melissa officinalis are used for their memory-enhancing effects in European folk medicine. Teucrium polium was reported to be used in Anatolia for memory-enhancement in a very old book written by an Ottoman herbalist–physician.

Aim of the study

Alzheimer's disease (AD) is a progressive neurological disorder mostly affecting the elder population. Currently, there is no cure for the treatment of severe type of AD. Therefore, in this study, the hydroalcoholic extracts of three traditionally used Lamiaceae species for memory-enhancement; Salvia triloba L., Melissa officinalis L., and Teucrium polium L., were assessed for their in vivo antiamnesic activity along with in vitro anticholinesterase and antioxidant activities.

Materials and methods

Scopolamine-induced antiamnesic activity was determined in mice by passive avoidance test, while anticholinesterase effect was measured by spectrophotometric Ellman method at 0.25, 0.50, 1.0, and 2.0 mg ml⁻¹ and antioxidant activity was assessed by scavenging effect against 2,2-diphenylpicrylhydrazyl (DPPH). Total phenol contents of the extracts were determined by Folin-Ciocalteau method.

Results

Salvia triloba was the most effective in antiamnesic experiment at 100, 200, and 400 mg kg⁻¹ doses having 22.7, 57.1, and 71.4% of relative effects, respectively. Teucrium polium was also active dose-dependently, whereas Melissa officinalis was completely inactive. In the anticholinesterase assay, the extracts showed similar inhibitions against acetylcholinesterase and Teucrium polium had the highest inhibition (65.8% at 1.0 mg ml⁻¹). Concerning the antioxidant effect, all the extracts exerted the highest activity among all having IC₅₀ values between 0.227 and 0.428 mg/ml.

Conclusion

Our data suggest that Teucrium polium among the screened plants deserves to be examined further as a herbal alternative for AD treatment.     

Antibacterial activity and chemical composition of essential oil of Pamburus missionis

Aim of the study

The aerial parts of Pamburus missionis (Wight) Swingle (Rutaceae) are traditionally used in the treatment of swelling, chronic rheumatism, paralysis, and puerperal diseases.The aim of this work was to investigate the chemical composition and antibacterial activity of essential oil of Pamburus missionis against different bacterial strains.

Materials and methods

The essential oil was obtained from fresh leaves by hydro distillation method and its chemical composition was analyzed by GC and GC–MS. The antibacterial activity was determined by disc diffusion and micro broth dilution assay.

Results

GC–MS analysis of the essential oil revealed the presence of 1-tridecanol (38.4%), n-hexadecanoic acid (16.1%), oxygenated monoterpenes (14.4%), monoterpene hydrocarbons (3.1%) and eugenol (1.9%) as the major components. The oil exhibited antibacterial activity at 100 and 450 μg against the test organisms with inhibition zones of 7–25 mm and minimal inhibitory concentrations values in the range of 10–100 and >100 mg/ml.

Conclusion

The present study reveals the antibacterial potency of essential oil of Pamburus missionis. The use of Pamburus missionis in the treatment of various ailments and puerperal diseases can be attributed to its antibacterial property.     

In vitro antigonococcal activity of Coscinium fenestratum stem extract

Ethnopharmacological relevance

Gonorrhea is a sexually transmitted disease (STD), which originates from bacteria, Neisseria gonorrhoeae. It is still one of the major health problems worldwide in both men and women. Many medicinal plants have been recorded in Thai folk medicine for relieving STD but there is no scientific report of these plants for antigonococcal activity.

Aim of the study

This study was conducted to evaluate antigonococcal activity of 22 Thai medicinal plants selected from the plants popularly used in Thai folk medicine for treatment of gonorrhea.

Materials and methods

This study was performed by disc diffusion and agar dilution methods against Neisseria gonorrhoeae. Active compound was investigated by bioautographic assay.

Results

Among the selected plants, Coscinium fenestratum (Gaertn.) Colebr. extract showed the most effective activity against Neisseria gonorrhoeae ATCC 49226 with MIC value of 47.39 μg/ml. Bioautographic assay revealed that berberine was the active compound of Coscinium fenestratum against Neisseria gonorrhoeae. The average MIC values of purified berberine against Neisseria gonorrhoeae ATCC 49226 and 11 clinical isolates were 13.51 and 17.66 μg/ml, respectively while average MIC value of the crude extract of Coscinium fenestratum against all clinical isolates was about 56.39 μg/ml. There was no acute toxicity detected at the dose of 5 g of Coscinium fenestratum crude extract per kilogram.

Conclusions

These results provide theoretical support for ethnopharmacological relevance of antigonococcal activity of Coscinium fenestratum and its active compound.     

Screening of the topical anti-inflammatory activity of the bark of Acacia cornigera Willdenow, Byrsonima crassifolia Kunth, Sweetia panamensis Yakovlev and the leaves of Sphagneticola trilobata Hitchcock

Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID₅₀ (dose giving 50% oedema inhibition) values ranging from 112 μg/cm² (Byrsonima crassifolia) to 183 μg/cm² (Sphagneticola trilobata). As reference, ID₅₀ of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm².

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.     

Anthelmintic activity of Arisaema franchetianum and Arisaema lobatum essential oils against Haemonchus contortus

Ethnopharmacological relevance

Arisaema franchetianum and Arisaema lobatum are two perennial plants native to China. Arisaema franchetianum is universally used to promote the subsidence of induration and swelling, quicken blood and relieve pains, and kill intestinal parasites in humans and animals. Arisaema lobatum is used to treat malaria, intestinal parasites, and snake and insect bites in humans and animals. The aim of this study was to determine the composition of the essential oils from Arisaema franchetianum and Arisaema lobatum and evaluate the anthelmintic effect against Haemonchus contortus.

Materials and methods

Two oils were investigated by GC and GC–MS. The anthelmintic bioassay tests of Arisaema franchetianum and Arisaema lobatum essential oil, linalool and carvacrol were performed using egg hatch assay (EHA), larval development assay (LDA) and larval migration inhibition assay (LMIA).

Results

Fifty six components representing 96.88% of the Arisaema franchetianum oil and 64 components representing 96.88% of the Arisaema lobatum oil were identified. Carvacrol and linalool were found to be the major constituents of two oils. In the EHA, greater than 99% inhibition were observed with Arisaema franchetianum oil at 10 mg/mL (CE₅₀ 1.63 mg/mL) and Arisaema lobatum oil at 5 and 10 mg/mL (CE₅₀ 0.48 mg/mL). In the LDA, both oils induced complete inhibition at 10 mg/mL, with the CE₅₀ being 1.10 mg/mL for Arisaema franchetianum oil and 0.73 mg/mL for Arisaema lobatum oil. In the LMIA, the Arisaema franchetianum oil and Arisaema lobatum oil at best inhibited 74.1% and 95.6% of larval migration at 10 mg/mL, respectively. Carvacrol exhibited similar activity to Arisaema lobatum essential oil and linalool did not show high activity in every assay.

Conclusions

These data show for the first time that the essential oils obtained from Arisaema franchetianum or Arisaema lobatum had promising anthelmintic activity against Haemonchus contortus. Arisaema plant may offer an alternative source for the control of gastrointestinal nematodes of sheep and goats.     

Anthelmintic activity of Ziziphus nummularia (bark) and Acacia nilotica (fruit) against Trichostrongylid nematodes of sheep

Ethnopharmacological relevance

Ziziphus nummularia (Rhamnaceae) and Acacia nilotica (Fabaceae) are being used as anthelmintics in ethnoveterinary medicinal system of Pakistan.

Aim of the study

Present study was conducted to determine the anthelmintic activity of Ziziphus nummularia (bark) and Acacia nilotica (fruit) in order to justify their traditional use in veterinary medicine.

Materials and methods

In vitro anthelmintic activity of crude methanolic extract (CME) of both the plants was determined against Haemonchus contortus by the adult motility assay, the egg hatch test and the larval development assay. In vivo anthelmintic activity was evaluated in sheep naturally infected with gastrointestinal nematodes by administering increasing doses of crude powder (CP) and CME (1.0–3.0 g/kg).

Results

Both the plants exhibited dose- and time-dependent anthelmintic effects by causing mortality of worms, and inhibiting egg hatching and larval development. Acacia nilotica (LC₅₀ = 512.86 and 194.98 μg/ml) was found to be more potent than Ziziphus nummularia (LC₅₀ = 676.08 and 398.11 μg/ml) in egg hatch test and larval development assay, respectively. In vivo, maximum fecal egg count reduction (84.7%) was recorded on day 13 post-treatment in sheep treated with Ziziphus nummularia CME (3.0 g/kg) followed by 78.5% on same day with Acacia nilotica CME (3.0 g/kg).

Conclusions

These data show that both Ziziphus nummularia and Acacia nilotica possess anthelmintic activity in vitro and in vivo, justifying their use in traditional veterinary medicine in Pakistan.     

In vitro activity of Tridax procumbens against promastigotes of Leishmania mexicana

Ethnopharmacological relevance

Tridax procumbens is an active herb against leishmaniasis.

Aim of the study

Leishmaniasis is a group of diseases caused by Leishmania protozoa. We investigated the antileishmanial activity of Tridax procumbens extracts and a pure compound against promastigotes of Leishmania mexicana, the causative agent of cutaneous leishmaniasis in the New World.

Materials and methods

Extracts and (3S)-16,17-didehydrofalcarinol (1) were obtained by chromatographic methods from Tridax procumbens, and the latter identified by spectroscopic analysis. The effect of these extracts and 1 on the growth inhibition of promastigotes of Leishmania mexicana was evaluated. In order to test the safety of extracts and 1, mammalian cells were treated with them, and cell viability was assessed using trypan blue and MTT.

Results

We demonstrated that extracts of Tridax procumbens and 1 showed a pronounced activity against Leishmania mexicana. The methanol extract inhibited promastigotes growth of Leishmania mexicana with a 50% inhibitory concentration (IC₅₀) of 3 μg/ml, while oxylipin 1 exhibited the highest inhibition at IC₅₀ = 0.478 μg/ml.

Conclusions

In this study we report the biological activity of extracts and (3S)-16,17-didehydrofalcarinol (1), obtained from Tridax procumbens, on the promastigote form of Leishmania mexicana, with no effect upon mammalian cells.     

Antibacterial activity of Helleborus bocconei Ten. subsp. siculus root extracts

Aim of the study

Roots of Helleborus bocconei Ten. subsp. siculus (Schiffner) Merxm. & Podl. are widely used in veterinary folk medicine in Sicily (Italy) to diagnose and cure lower respiratory tract infections in cattle. This study intended to evaluate the in vitro antibacterial activity of the methanolic root extract of Helleborus bocconei Ten. subsp. siculus, and of the bufadienolide and ecdysteroid fractions extracted from its roots, against strains belonging to species commonly associated with respiratory tract infections.

Materials and methods

The phytochemical screening of the previously prepared plant extracts was carried out by chemical, thin-layer chromatography and spectroscopic methods. The in vitro antibacterial activity of the extracts against seven different standard bacterial strains was evaluated by broth microdilution.

Results

According to the present study, Helleborus bocconei Ten. subsp. siculus roots contain bufadienolides and ecdysteroids, and the extracts containing these compounds, as well as the crude methanolic root extract, show antibacterial activity against microorganisms responsible for respiratory infections. In particular, the bufadienolide extract has the highest inhibitory activity against all the tested organisms, and, as the other extracts, shows the lowest MIC values (100 μg/ml) against Moraxella catarrhalis and Streptococcus pneumoniae.

Conclusions

Since the roots of Helleborus bocconei Ten. subsp. siculus contain substances with antibacterial activity, the traditional use of this plant may also derive from its antibacterial properties.     

Anti-inflammatory,anti-angiogenic and anti-nociceptive activities of an ethanol extract of Salvia plebeia R. Brown

Ethnopharmacological relevance

Salvia plebeia R. Brown has been used for the treatment of a variety of inflammatory diseases, cold and tumors in many countries, including Korea and China.

Aim of the study

This study aimed to assess anti-inflammatory and related activities of an ethanol extract (SPEE) prepared from the dried whole parts of Salvia plebeia.

Materials and methods

Anti-angiogenic and anti-nociceptive activities of SPEE were analyzed using the chick chorioallantoic membrane (CAM) assay and acetic acid-induced writhing response, respectively. Anti-inflammatory activity of SPEE was evaluated using acetic acid-induced vascular permeability, carrageenan-induced inflammation in the air pouch and analyses of nitrite content and induced nitric oxide synthase (iNOS) level in the macrophage cells.

Results

SPEE gave rise to a significant inhibition in chick chorioallantoic membrane angiogenesis. SPEE exhibited anti-inflammatory activities in vascular permeability and air-pouch models. In the air-pouch model, SPEE was able to diminish exudate volume, number of polymorphonulcear leukocytes and nitrite content. SPEE also displayed anti-nociceptive activity in the writhing response model in mice. SPEE significantly decreased nitrite content and induced nitric oxide synthase (iNOS) in the lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells, while it could not modulate cyclooxygenase-2 (COX-2) and matrix metalloproteinase-9 levels in the stimulated phages. SPEE decreased reactive oxygen species (ROS) level in the stimulated macrophages.

Conclusion

The ethanol extract (SPEE) of Salvia plebeia possesses anti-inflammatory and related anti-angiogenic, anti-nociceptive and antioxidant activities, which offers partial support to its folkloric use.     

Dual effects of lipophilic extract of Salvia miltiorrhiza (Danshen) on catecholamine secretion in cultured bovine adrenal medullary cells

Ethnopharmacological relevance

Salvia miltiorrhiza (Danshen) is a well known traditional Chinese herb, which has been used widely in China for the treatment of cardiovascular diseases in clinic.

Aim of this study

The aim of the present study is to clarify the effects of lipophilic extract of Salvia miltiorrhiza (LESM) on catecholamine (CA) secretion, a traditional Chinese medicine used widely for the treatment of cardiovascular diseases in China.

Materials and methods

LESM was evaluated for its effects on CA secretion using HPLC-ECD method. The effects of LESM on ²²Na⁺ influx and intracellular calcium ([Ca²⁺]_i) were also investigated.

Results

Our results showed that LEMS directly stimulated basal CA secretion in an extracellular Ca²⁺-dependent manner. And the stimulation was not affected by combination of hexamethonium (Hex), an inhibitor of nAChR. LESM also directly elevated [Ca²⁺]_i. In addition, using selective blockers of voltage-dependent Ca²⁺ channels, such as nitrendipine (for L-type), ω-agatoxin-IVA (for P-type) and ω-conotoxin-GVIA (for N-type), it was found that nitrendipine suppressed the elevation of [Ca²⁺]_i induced by LESM, but not ω-agatoxin-IVA or ω-conotoxin-GVIA. Compared with acetylcholine (ACh) only, however, combination of LESM with ACh inhibited the raise of CA secretion, ²²Na⁺ influx and [Ca²⁺]_i in a concentration-dependent manner. Furthermore, LESM also inhibited CA secretion induced by veratridine (Ver), and 56 mM K⁺ at concentrations similar to those for [Ca²⁺]_i rise. One of the lipophilic active compounds, cryptotanshione (Cryp), also had the same effects on CA secretion with LESM.

Conclusions

All these findings suggest that LESM exerts dual effects on CA secretion in cultured bovine adrenal medullary cells. LESM exerts antagonistic effects on nAChR, voltage-dependent Na⁺ and Ca²⁺ channels, whereas it is an agonist of L-type Ca²⁺ channel when it used alone.     

In vitro antibacterial effects of Cinnamomum extracts on common bacteria found in wound infections with emphasis on methicillin-resistant Staphylococcus aureus

Ethnopharmacological relevance

Cinnamomum species have been widely used in many traditional systems of medicine around the world. In the Malaysian traditional system of medicine, the leaves, stem bark and stem wood of Cinnamomum iners, Cinnamomum porrectum, Cinnamomum altissimum and Cinnamomum impressicostatum have been used to treat wound infections. To study the antibacterial effects of Cinnamomum iners, Cinnamomum porrectum, Cinnamomum altissimum and Cinnamomum impressicostatum against common bacteria found in wound infections with primary focus on methicillin-resistant Staphylococcus aureus (MRSA).

Materials and methods

The crude extracts from the leaves, stem-bark and stem-wood of Cinnamomum iners, Cinnamomum porrectum, Cinnamomum altissimum and Cinnamomum impressicostatum were obtained using sequential extraction with hexane, ethylacetate, methanol and water. The volatile oils were obtained by hydro-distillation. The antibacterial activities of extracts were investigated using disk diffusion assays and broth microdilution assays.

Results

The volatile oils obtained from the stem-bark of Cinnamomum altissimum, Cinnamomum porrectum and Cinnamomum impressicostatum have shown significant antibacterial activity against a wide range of Gram positive and Gram negative bacteria including MRSA. A few test extracts have shown better activity against MRSA as compared to methicillin sensitive Staphylococcus aureus (MSSA). Amongst all the test extracts, Cinnamomum impressicostatum stem-bark water extract produced the largest inhibition zone of 21.0 mm against MRSA while its inhibition zone against MSSA was only 8.5 mm. The minimum inhibitory concentration (MIC) of this extract against MRSA was 19.5 μg mL⁻¹ and the corresponding minimum bactericidal concentration (MBC) was 39.0 μg mL⁻¹.

Conclusions

This study has scientifically validated the traditional use of Cinnamomum species in treating wound infections. Of high scientific interest was the observation that the antibacterial effect of Cinnamomum impressicostatum stem-bark crude water extract against MRSA was significantly higher than its effect against MSSA, suggesting that the extract contains a compound(s) with higher specific neutralising activity against the drug resistance markers of MRSA.     

Antisecretory activity from the flowers of Chiranthodendron pentadactylon and its flavonoids on intestinal fluid accumulation induced by Vibrio cholerae toxin in rats

Ethnopharmacological relevance

The flowers of Chiranthodendron pentadactylon Larreat. (Sterculiaceae) has been traditionally used as folk medicine in Mexico for the treatment of gastrointestinal disorders such as diarrhea and dysentery.

Aim of the study

This study aimed to assess the antisecretory activity which supports the therapeutic use of Chiranthodendron pentadactylon and its flavonoids to treat diarrhea.

Materials and methods

The methanol extract of Chiranthodendron pentadactylon, subsequent fractions, and flavonoids were evaluated on cholera toxin-induced intestinal secretion in rat jejunal loops model.

Results

Three antisecretory flavonoids were isolated by bioassay-guided purification, namely, isoquercitrin 3, (+)-catechin 4 and (−)-epicatechin 5. Among them, epicatechin exhibited the most potent antisecretory activity with ID₅₀ of 8.3 μM/kg. Its potency was close that of to loperamide (ID₅₀ 6.1 μM/kg), drug used as control. Isoquercitrin (ID₅₀ 19.2 μM/kg) and catechin (ID₅₀ 51.7 μM/kg) showed moderate and weak activity, respectively.

Conclusion

The results of the present study lend some support to the anecdotal report for the traditional use of the flowers of Chiranthodendron pentadactylon in the control of dysentery.     

Characterization of the antinociceptive and anti-inflammatory activities from Cocos nucifera L. (Palmae)

Aim of the study

Cocos nucifera cultivated in Brazil is known as “coco-da-Bahia” or “coqueiro-da-Índia”. The tea from the husk fiber is widely used to several inflammatory disorders. Crude extract and fractions obtained from Cocos nucifera “common variety” were evaluated to test the anti-inflammatory and antinociceptive activities.

Materials and methods

Crude extract (CE, 50, 100, and 150 mg/kg), fraction 1 (F1, molecular weight lesser than 1 kDa, 1, 10, and 50 mg/kg), fraction 2 (F2, molecular weight higher than 1 kDa, 1, 10, and 50 mg/kg), and the references drugs morphine (5 mg/kg), acetilsalicilic acid (200 mg/kg), prometazine (30 mg/kg), and metisergide (5 mg/kg) were evaluated on models of analgesia and inflammation.

Results

CE, F1, and F2 significantly develop peripheral and central antinociceptive activity but with less effect on supra-spinal regions of the brain. Administration of the opioid antagonist, naloxone (5 mg/kg) inhibited the antinociceptive effect indicating that Cocos nucifera crude extract and fractions may be acting in opioid receptors. CE and F1 also inhibited rat paw edema induced by histamine, and serotonin.

Conclusions

results demonstrated that Cocos nucifera and its fractions have antinociceptive and anti-inflammatory activities which confirm the popular use of this plant in several inflammatory disorders.     

Davilla elliptica and Davilla nitida: Gastroprotective,anti-inflammatory immunomodulatory and anti-Helicobacter pylori action

Ethnopharmacological relevance

Davilla elliptica and Davilla nitida are species commonly found in the Brazilian Cerrado biome.

Aim of the study

Based on ethnopharmacological and phytochemical analyses, methanolic extracts from leaves of Davilla elliptica (EDE) and Davilla nitida (EDN) were evaluated for their anti-ulcer, anti-inflammatory, immunological and anti-Helicobacter pylori activities.

Materials and methods

The gastroprotective action of both extracts was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated anti-inflammatory (carrageenin-induced rat hind paw edema), immunomodulatory (murine peritoneal macrophages) and antibacterial action of both extracts against a standard strain of Helicobacter pylori.

Results

EDE and EDN (500 mg/kg) were able to protect gastric mucosa against HCl/ethanol solution (EDE 63%; EDN 59%), absolute ethanol (EDE 95%; EDN 88%), and also against injurious effect of NSAID (EDE 77%; EDN 67%). When EDE and EDN were challenged with sulfhydryl depleter compound, the gastroprotective action of both extracts was completely abolished. EDE had gastroprotective effect related to increase of glutathione bioavailability and stimulated higher levels of NO, H₂O₂ and TNF-α production. Otherwise EDN showed better anti-Helicobacter pylori action than EDE. Neither extracts presented anti-inflammatory activity by oral route.

Conclusion

The phytochemical investigation showed that both extracts possess phenolic acid derivatives, acylglycoflavonoids and condensed tannins with evident quantitative variations that probably influenced the pharmacological differences between extracts.     

Mast cell stabilizing effects of Sphaeranthus indicus

Aim of the study

We investigated the effects of Sphaeranthus indicus on mast cell stabilizing activity to provide scientific basis for the clinical use of S. indicus.

Materials and methods

The protective effect of different extracts of whole plant of S. indicus against compound 48/80 and sheep serum induced mast cell degranulation was evaluated.

Results

Ethanol extract of S. indicus at the doses of 150 mg/kg and 300 mg/kg and ethyl acetate extract at the dose of 100 mg/kg, 150 mg/kg and 300 mg/kg showed slightly better protection of mast cell degranulation (77–86%) than the standard drug ketotifen (75%) in the sheep serum model. These extracts also showed better mast cell stabilizing activity (77–88%) than the standard drug (69%) when peritoneal mast cells are treated with compound 48/80.

Conclusion

These results suggest that S. indicus has potent mast cell stabilizing effects thereby inhibiting mediator release from mast cells.     

In vitro antiplasmodial activity of plants used in Benin in traditional medicine to treat malaria

Aim of the study

The aim of the study was to evaluate the in vitro antiplasmodial activity of crude extracts of 12 plant species traditionally used in Benin for the treatment of malaria in order to validate their use.

Materials and methods

For each species, dichloromethane, methanol and total aqueous extracts were tested. The antiplasmodial activity of extracts was evaluated using the measurement of the plasmodial lactate dehydrogenase activity on chloroquine-sensitive (3D7) and resistant (W2) strains of Plasmodium falciparum. The selectivity of the different extracts was evaluated using the MTT test on J774 macrophage-like murine cells and WI38 human normal fibroblasts.

Results

The best growth inhibition of both strains of Plasmodium falciparum was observed with the dichloromethane extracts of Acanthospermum hispidum DC. (Asteraceae) (IC₅₀ = 7.5 μg/ml on 3D7 and 4.8 μg/ml on W2), Keetia leucantha (K. Krause) Bridson (syn. Plectronia leucantha Krause) (Rubiaceae) leaves and twigs (IC₅₀ = 13.8 and 11.3 μg/ml on 3D7 and IC₅₀ = 26.5 and 15.8 μg/ml on W2, respectively), Carpolobia lutea G.Don. (Polygalaceae) (IC₅₀ = 19.4 μg/ml on 3D7 and 8.1 μg/ml on W2) and Strychnos spinosa Lam. (Loganiaceae) leaves (IC₅₀ = 15.6 μg/ml on 3D7 and 8.9 μg/ml on W2). All these extracts had a low cytotoxicity.

Conclusion

Our study gives some justifications for the traditional uses of some investigated plants.