Antimicrobial activity of Acacia mellifera extracts and lupane triterpenes

Ethnopharmacological relevance

Acacia mellifera (Vahl) Benth (Leguminosae) is a subtropical medicinal plant that is widely used in traditional African medicines against various diseases such as pneumonia and malaria.

Aim of the study

The present study was performed to evaluate the antimicrobial effects of extracts from the stem bark of Acacia mellifera.

Materials and methods

The extracts were examined for antibacterial and antifungal activity using the disc-diffusion method against bacterial strains: Streptococcus pneumoniae (ATCC 25923), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 35218), Escherichia coli (ATCC 25922) and Staphylococcus aureus (ATCC 25923) and fungal strains Candida albicans (ATCC 90028), Candida krusei (ATCC 6255), Cryptococcus neoformans (ATCC 6603) and clinical isolates of Microsporum gypseum and Trichophyton mentagrophytes.

Results

Some of these extracts were found to be active against some bacterial and fungal strains and were further fractionated to give 12 pure compounds. The methanolic and methanol:dichloromethane (1:1) extracts exhibited antibacterial and antifungal activity. The two were active against Staphylococcus aureus (ATCC 25923), Microsporum gypseum, and Trichophyton mentagrophytes. Activity guided fractionation led to isolation of two active compounds: 3-(Z)-cis coumaroylbetulin and 30-hydroxylup-20 (29)-en-3β-ol which were against Staphylococcus aureus (ATCC 25923), Microsporum gypseum, Trichophyton mentagrophytes and Pseudomonas aeruginosa (ATCC 27853).

Conclusions

These results may partly explain and support the use of Acacia mellifera stem barks for the treatment of infectious diseases in traditional Kenya medicine.     

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 biological activities of niloticane,a new bioactive cassane diterpene from the bark of Acacia nilotica subsp. kraussiana

Ethnopharmacological relevance

Acacia nilotica subsp. kraussiana was reported in African traditional medicine for the treatment of various ailments. Isolation of an active compound in this study from the bark extract may lead to the validation of its efficiency as a traditional crude drug.

Aims of the study

This study aimed to isolate active compound(s) from an ethyl acetate bark extract of Acacia nilotica subsp. kraussiana and to investigate some of its biological activity.

Materials and methods

The isolation process was carried out using bioassay-guided fractionation. The isolated compound was tested for antibacterial activity using the micro-dilution assay; anti-inflammatory activity using the COX-1 and COX-2 assays and investigated for inhibitory effect against acetylcholinesterase using the microplate assay.

Results

A new bioactive compound was isolated and identified as a cassane diterpene, niloticane. Niloticane showed antibacterial activity against Gram-positive bacteria Bacillus subtilis and Staphylococcus aureus with MIC values of 4 and 8 μg/mL, respectively. With Gram-negative bacteria, niloticane showed weak activity. MIC values obtained were 16 and 33 μg/mL against Klebsiella pneumonia and Escherichia coli, respectively. In the cyclooxygenase test, niloticane possessed activity with IC₅₀ values of 28 and 210 μM against COX-1 and COX-2, respectively. IC₅₀ values observed with indomethacin (positive control) were 3.6 μM for COX-1 and 189 μM for COX-2. In the acetylcholinesterase test, niloticane showed anti-cholinesterase activity with an IC₅₀ value of 4 μM. IC₅₀ values obtained by the galanthamine (positive control) was 2.0 μM.

Conclusion

The results obtained support the traditional uses of the bark of Acacia nilotica subsp. kraussiana in African traditional medicine for the treatment of some ailments that relate to microbial diseases, inflammation and central nervous system disorders.     

儿茶化学成分研究

目的:研究儿茶Acacia catechu的化学成分。方法:应用正相硅胶、Sephadex LH-20、ODS等柱色谱技术及重结晶等方法分离纯化,通过理化性质和波谱学方法鉴定化合物的结构。结果:从儿茶乙酸乙酯部位中分离出12个化合物,分别鉴定为对-羟基苯甲酸(4-hydroxybenzoic acid,1)、山柰酚(kaempferol,2)、槲皮素(quercetin,3)、3,4′,7-三羟基-3′,5-二甲氧基黄酮(3,4′,7-trihydroxyl-3′,5-dimethoxyflavone,4)、儿茶素(catechin,5)、表儿茶素(epicatechin,6)、阿福豆素(afz-elechin,7)、表阿福豆素(epiafzelechin,8)、mesquitol(9)、ophioglonin(10),香橙素(aromadendrin,11)和苯酚(phenol,12)。结论:化合物7,12为从该植物首次分离得到,化合物4,9~11为从该属植物首次分离得到。     

Anti-nociceptive activity of Pereskia bleo Kunth. (Cactaceae) leaves extracts

Ethnopharmacological relevance

Local communities in Malaysia consume Pereskia bleo Kunth. (Cactaceae) leaves as raw vegetables or as a concoction and drink as a tea to treat diabetes, hypertension, rheumatism, cancer-related diseases, inflammation, gastric pain, ulcers, and for revitalizing the body.

Aim of the study

To evaluate anti-nociceptive activity of the extracts and vitexin, isolated for the first time in this species, in two analgesic models; formalin-induced licking and acetic acid-induced abdominal writhing.

Materials and methods

Three and a half kilos of P. bleo leaves were extracted using Soxhlet apparatus with ethanol for 72 h. The crude ethanol extract was treated with activated charcoal overnight and subjected to a liquid–liquid partition yielding hexane, dichloromethane, ethyl acetate and butanol extracts. All extracts, including the crude ethanol and vitexin isolated from the ethyl acetate partition were tested for peripheral anti-nociceptive activity using formalin test and acetic acid-induced abdominal writhing, besides having their acute toxicity assays performed.

Results

The phytochemical analyses resulted in the isolation of vitexin (1), β-sitosterol glucoside (2) and β-sitosterol (3) isolated from the ethyl acetate, dichloromethane and hexane extracts, respectively. This is the first time vitexin and β-sitosterol glucoside are isolated from this species. The anti-nociceptive activities for all extracts were only moderate. Vitexin, which was isolated from the ethyl acetate extract did not show any activity in all models tested when used alone at the same concentration as it appears in the extract.

Conclusion

This study showed that all the extracts possess moderate anti-nociceptive activity. Vitexin is not the compound responsible for the anti-nociceptive effect in the ethyl acetate extract. Further investigations are needed to identify the compound(s) that might be responsible for the anti-nociceptive activity in this plant.     

山香圆叶中黄酮苷类成分及其抗炎活性研究

应用大孔树脂、聚酰胺、Sephadex LH-20,HPLC等各种色谱技术对山香圆叶95％乙醇提取物经乙酸乙酯萃取后的水部位进行分离纯化,分离得到8个黄酮苷类化合物,采用NMR等谱学方法分别鉴定为:野漆树苷(1),女贞苷(2),刺槐素-7-O-[β-D-吡喃葡萄糖基-(1→6)-α-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(3),刺槐素-7-O-[α-L-吡喃鼠李糖基(1→6)-o-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(密蒙花新苷,4),木犀草素-7-O-α-L-吡喃鼠李糖基-(1→2)-β-D-吡喃葡萄糖苷(5),金圣草素-7-O-α-L-吡喃鼠李糖基-(1→2)β-D-吡喃葡萄糖苷(6),刺槐素-7-O-α-L-吡喃鼠李糖基-(1→2)β-D-吡喃葡萄糖苷(蒙花苷,7),芹菜素6,8-二-C-β-D-吡喃葡萄糖苷(8).其中化合物3～8为首次从该植物中分离获得.采用脂多糖(LPS)刺激RAM264.7巨噬细胞炎症模型对分离得到的化合物进行抗炎活性评价,结果表明化合物2,3在1x10-5 mol.L-1浓度下,对LPS刺激RAW264.7细胞NO生成的抑制率分别为33.7％和23.8％,提示化合物2,3具有较弱的抗炎活性.     

Analgesic and anti-inflammatory effects of Cassia siamea Lam. stem bark extracts

Aim of the study

The present study was carried out to investigate analgesic and anti-inflammatory activities of Cassia siamea Lam stem bark extracts. We have also determined the cytotoxicity of each extract.

Materials and methods

C. siamea, a widespread medicinal plant traditionally used in sub-Saharan Africa, was collected in Congo Brazzaville. Stem bark was extracted with petroleum ether (CSE1), chloroform (CSE2), ethanol (CSE3) and water (CSE4). Analgesic, anti-inflammatory and antipyretic activities of these extracts were assessed in rats with hot plate test, paw pressure and carrageenan induced paw oedema. Cytotoxicity was assessed against KB and Vero cells.

Results

At the doses used (100, 200, and 400 mg/kg) ethanol and water extracts showed significant and dose-dependent analgesic and anti-inflammatory effects. None of the extracts had cytotoxic activity on KB and Vero cell lines and the most active extracts (CSE3 and CSE4) had no acute toxicity.

Conclusions

The study highlighted the analgesic and anti-inflammatory of C. siamea stem bark. Four major families of compounds present in the plant may explain these activities: triterpenes (lupeol, oleanolic acid, ursolic acid, friedelin, betulin), flavonoids (apigenin, kaempferol, luteolin), anthraquinones (emodin), phytosterols (stigmasterol, beta-sitosterol).     

Topical anti-inflammatory activity of body fat from the lizard Tupinambis merianae

Aim of the study

Tupinambis merianae is one of the most frequently used animals in traditional medicine in Brazil as its body fat has many different therapeutic indications as a folk remedy. The present study evaluated the topical anti-inflammatory activity of Tupinambis merianae fat in treating ear edema in an animal model.

Materials and methods

Oil (OTM) was extracted from body fat located in the ventral region of Tupinambis merianae using hexane as a solvent. Ear edema provoked by the application of croton oil (single and multiple application), arachidonic acid, phenol and capsaicin to Swiss mice was used to evaluate the potential anti-inflammatory value of the topical use of OTM. Topical applications of these irritants were made to the right ears of animals that were pre-treated with a acetone (control), dexamethasone, or OTM.

Results

Our results indicate that Tupinambis merianae fat demonstrates significant topical anti-inflammatory activity that reduces inflammation related to ear edema caused by croton oil (single and multiple application), arachidonic acid, phenol. While the inflammation caused by capsaicin, OTM did not significantly reduce the edema.

Conclusion

This represents the first evidence of anti-inflammatory activity of Tupinambis merianae fat in in vivo models, confirming its usefulness in traditional medicine as a remedy for skin diseases (dermatitis). The fatty acids present in OTM most likely inhibit the response pathway of arachidonic acid and its metabolites, thus reducing the production of pro-inflammatory mediators.     

Antinociceptive activity of fractions from Couroupita guianensis Aubl. leaves

Ethnopharmacological relevance

Couroupitaguianensis Aubl. (Lecythidaceae) is popularly known in Brazil as “abricó-de-macaco”. Infusions or teas obtained from its leaves, flowers, and barks are used in South America for the treatment of several disorders such as pain and inflammatory processes.

Aim of the study

Evaluate antinociceptive effects of crude ethanol extract (CEE) and its fractions in three analgesic models (acetic acid-induced contortions, tail flick, and hot plate) and study the possible mechanism of their action.

Materials and methods

CEE, hexane, dichloromethane, ethyl acetate, and butanol fractions (10, 30, and 100 mg/kg, p.o.) and the reference drug morphine (5 mg/kg, s.c.) were evaluated. To elucidate the mechanism of action from the fractions, animals were pre-treated (30 min) with atropine (muscarinic receptor antagonist, 1 mg/kg, s.c.), mecamylamine (nicotinic receptor antagonist, 2 mg/kg, s.c.), naloxone (opioid receptor antagonist, 1 mg/kg, s.c.) or l-nitro arginine methyl ester (l-NAME, nitric oxide synthase inhibitor, 3 mg/kg, s.c.).

Results

CEE and fractions significantly inhibited the number of contortions induced by acetic acid. All fractions showed antinociceptive activity in the tail flick model, being the hexane and ethyl acetate the most potent and long acting fractions. In the hot plate method the highest effect observed was at the dose of 100 mg/kg from all fractions. Administration of naloxone inhibited the antinociceptive effect of fractions. Pre-treatment of mice with atropine reduced the antinociceptive activity of CEE and its fractions, the exception being the dichloromethane fraction. Mecamylamine did not inhibited the effect of dichloromethane fraction. l-NAME reduced the anti-hyperalgesic effect of all fractions, but the most prominent effect was observed in the antinociceptive activity caused by CEE and butanol fraction.

Conclusions

Results obtained demonstrated that Couroupita guianensis CEE and its fractions have antinociceptive activity that is mediated, at least in part, by opioid and cholinergic systems and nitric oxide pathway.     

Anti-inflammatory activity of ethanol extract and fractions from Couroupita guianensis Aublet leaves

Ethnopharmacological relevance

Couroupita guianensis Aublet, ‘macacarecuia’, ‘abricó-de-macaco’, ‘castanha-de-macaco’ and ‘amêndoa-dos-andes’, is found in tropical regions and is widely used in the treatment of tumors, pain, and inflammatory processes.

Aim of the study

Ethanol extract and hexane and ethyl acetate fractions were evaluated in models of inflammatory pain (formalin-induced licking) and acute inflammation (carrageenan-induced peritonitis).

Materials and methods

Ethanol extract, hexane and ethyl acetate fractions (10, 30 or 100 mg/kg, p.o.) and the reference drugs dexamethasone (5 mg/kg), morphine (5 mg/kg, s.c.), and acetylsalicylic acid (100 mg/kg, p.o.) were tested in formalin-induced licking response and carrageenan-induced peritonitis.

Results

All three doses from Couroupita guianensis fractions significantly reduced the time that the animal spent licking the formalin-injected paw in first and second phases. However, only higher doses (30 and 100 mg/kg) were able to inhibit the leukocyte migration into the peritoneal cavity after carrageenan injection. In this model, the 100 mg/kg dose almost abolished the cell migration. It was also observed that protein concentration resulted from extravasation to the peritoneum and nitric oxide (NO) productions were significantly reduced. Cytokines production was differently affected by the treatment. TNF-α production was reduced after ethanol extract and ethyl acetate fraction pre-treatment whereas hexane fraction had effect only with 100 mg/kg dose. IL-1β production was inhibited only after hexane fraction pre-treatment. The inhibitory effect observed was not due to a direct cytotoxic effect on cells nor to a NO-scavenger activity. The effect was due to a direct inhibition on NO production by the cells.

Conclusions

The results show that Couroupita guianensis fractions have anti-inflammatory effect, partly due to a reduction on cell migration and a inhibition on cytokines and inflammatory mediators production.     

Antinociceptive and anti-inflammatory activities of Bowdichia virgilioides (sucupira)

Ethnopharmacological relevance

Bowdichia virgilioides Kunth (Leguminosae Papilonoideae) is a plant with anti-inflammatory activity used in folk medicine. The importance of this plant promoted its inclusion in Brazilian Pharmacopoeia.

Aim of the study

In order to evaluate the actions of this plant, studies were performed on antinociceptive and anti-inflammatory activities.

Materials and methods

The aqueous extracts (AE) of Bowdichia virgilioides inner bark and leaves were used at 100, 200, and 400 mg/kg. Antinociceptive activity of plant extract was evaluated by writhing, hot-plate and formalin tests. Anti-inflammatory activity was evaluated using paw oedema and peritonitis methods.

Results

Oral treatment with the AE of inner bark or leaves elicited inhibitory activity (P < 0.01) on acetic acid effect at 200 and 400 mg/kg, and reduced the formalin effect at the second-phase (200 and 400 mg/kg, P < 0.01), however it did not elicit any inhibitory effect on hot-plate test. The indomethacin inhibited the acetic acid-induced writhing and the formalin effect at the second-phase (P < 0.001), and the morphine reduced the both phases of formalin test (P < 0.001). Carrageenan-induced oedema formation and neutrophil migration into the peritoneal cavity were reduced with the AE of inner bark or leaves at 100, 200, and 400 mg/kg (P < 0.05), and by the reference compounds aspirin (P < 0.001) and dexamethasone (P < 0.001), respectively.

Conclusions

The AE of Bowdichia virgilioides shows antinociceptive and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases.     

Antioxidant and anti-inflammatory activities of aqueous extract of Centipeda minima

Ethnopharmacological relevance

Centipeda minima (L.) is traditionally used in Chinese folk medicine for the treatments of rhinitis, sinusitis, relieving pain, reducing swelling, and treating cancer for a long history in Taiwan. However, there is no scientific evidence which supports the use in the literature.

Aim of the study

The aim of this study was to evaluate the antioxidant and anti-inflammatory activities of the aqueous extract of Centipeda minima (ACM).

Materials and methods

The following activities were investigated: antioxidant activities [2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), DPPH (1,1-diphenyl-2-picrylhydrazyl)], and anti-inflammatory [lipopolysaccharide (LPS) induced nitric oxide (NO) production in RAW264.7 macrophages and paw-edema induced by λ-carrageenan (Carr)]. We also investigated the anti-inflammatory mechanism of ACM via studies of the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) and the levels of malondialdehyde (MDA) in the edema paw. Serum NO, tumor necrosis factor α (TNF-α), and interleukin-1β (IL-1β) were also measured in vivo. In HPLC analysis, the fingerprint chromatogram of ACM was established.

Results

ACM showed the highest TEAC and DPPH radical scavenging activities, respectively. ACM also had highest contents of polyphenol and flavonoid contents. We evaluated that ACM and the reference compound of protocatechualdehyde and caffeic acid decreased the LPS-induced NO production in RAW264.7 cells. Administration of ACM showed a concentration dependent inhibition on paw edema development after Carr treatment in mice. The anti-inflammatory effects of ACM could be via NO, TNF-α, and IL-1β suppressions and associated with the increase in the activities of antioxidant enzymes. Western blotting revealed that ACM decreased Carr-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions.

Conclusions

Anti-inflammatory mechanisms of ACM might be correlated to the decrease in the level of Malondialdehyde (MDA), iNOS, and COX-2 via increasing the activities of CAT, SOD, and GPx in the edema paw. Overall, the results showed that ACM demonstrated antioxidant and anti-inflammatory activity, which supports previous claims of the traditional use for inflammation and pain.     

番荔枝皮化学成分及其抗肿瘤活性的研究

目的:研究番荔枝Annona squamosa的化学成分,并对分离化合物进行活性筛选.方法:综合运用各种色谱方法分离纯化番荔枝中的化学成分;采用NMR等波谱方法鉴定其结构;运用SRB法测定化合物对肿瘤细胞体外增殖能力的抑制作用.结果:从番荔枝皮乙醇提取物中分离得到11个化合物,分别是annosquamosin C(1),15,16-epoxy-17-hydroxy-ent-kau-ran-19-oic acid(2),16,17-dihydroxy-ent-kauran-19-oic acid(3),annosquamosin A(4),ent-kaur-16-en-19-oic acid (5),19-nor-ent-kauran-4-ol-17-oic acid(6),16-hydroxy-ent-kau-ran-19-oic acid(7),ent-15β-hydroxy-kaur-16-en-19-oic acid (8),annosquamosin B (9),ent-16β,17-dihydroxykauran-19-al(10),16,17-dihydroxy-ent-kauran-19-oic acid methyl ester(11).抗肿瘤活性实验表明,化合物1,2,3,5,9对人肺癌95-D细胞的体外增殖能力均具有不同程度的抑制作用,化合物5的活性最强,IC50为7.78 μmol·L-1;化合物2,5,9对人卵巢癌A2780细胞有抑制作用,其中化合物2和9的抑制作用较强,IC50分别为0.89,3.10 μmol·L-1.结论:化合物2,8,11分别为首次从该科、该属和该种植物分离得到;化合物5对人肺癌95-D细胞的抑制作用较强;化合物2和9对人卵巢癌细胞A2780的抑制作用较强.     

Comparison of active constituents,acute toxicity,anti-nociceptive and anti-inflammatory activities of Porana sinensis Hemsl., Erycibe obtusifolia Benth. and Erycibe schmidtii Craib

Ethnopharmacological relevance

Erycibe obtusifolia and Erycibe schmidtii, which belong to the same genus as Erycibe, are widely used in traditional medicine for the treatment of joint pain and rheumatoid arthritis (RA). Porana sinensis has become a widely used substitute for Erycibe obtusifolia and Erycibe schmidtii as they have declined in the wild. In the present work, the content of the main active components, the acute toxicity, the anti-nociceptive and anti-inflammatory activities of Porana sinensis, Erycibe obtusifolia and Erycibe schmidtii were compared, and the mechanisms of anti-nociceptive and anti-inflammatory activities were discussed.

Materials and methods

A quantitative HPLC (high performance liquid chromatography) method was first developed to compare the content of the main active components (scopoletin, scopolin and chlorogenic acid). The anti-inflammatory and anti-nociceptive activities of 40% ethanolic extracts of the three plants were compared using the models of xylene-induced ear edema, formalin-induced inflammation, carrageenan-induced air pouch inflammation, acetic acid-induced writhing and formalin-induced nociception. The acute toxicity of the 40% ethanolic extracts of the three plants was studied.

Results

The assay suggested a large content of scopoletin, scopolin and chlorogenic acid in the three plants. The 40% ethanolic extracts of the three plants were almost non-toxic at the dose of 5 g/kg and all of them showed significant anti-inflammatory effects in the tests of xylene-induced ear edema and formalin-induced inflammation. In the carrageenan-induced air pouch inflammation test, the synthesis of PGE2 was significantly inhibited by all the extracts. They significantly inhibited the number of contortions induced by acetic acid and the second phase of the formalin-induced licking response. Naloxone was not able to reverse the analgesic effect of these extracts.

Conclusion

The study identifies the similarity of the three plants in their main active components as well as acute toxicity, anti-nociceptive and anti-inflammatory activities. It supports the use of Porana sinensis as a suitable substitute, but further studies are needed to confirm this.     

Anti-inflammatory activity of Trichosanthes cucumerina Linn. in rats

Aim of the study

Trichosanthes cucumerina Linn. (Family: Cucurbitaceae) is one of the medicinal plants that is often used in Sri Lankan traditional systems of medicine. One of its uses is the treatment of inflammatory conditions. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of Trichosanthes cucumerina hot water extract (HWE) and its fractions.

Materials and methods

The anti-inflammatory activity of Trichosanthes cucumerina was evaluated by use of the carrageenan-induced paw oedema model in Wistar rats. In addition, the mechanism/s by which Trichosanthes cucumerina is mediated the anti-inflammatory activity was assessed by determining its effects on (a) membrane stabilizing activity and (b) nitric oxide inhibitory activity.

Results

Apart from the lowest dose of the HWE, other tested doses (500, 750, 1000 mg/kg) produced a significant (P ≤ 0.05) inhibition of the inflammation, most pronounced at 5 h after the injection of carrageenan. The anti-inflammatory effect induced by 750 mg/kg, was comparable to that of the reference drug, indomethacin at 4 and 5 h. Inhibition of nitric oxide (NO) production and membrane stabilization activities are probable mechanisms by which Trichosanthes cucumerina mediates its anti-inflammatory actions. Among the tested fractions, methanol fraction (MEF) and aqueous fraction (AQF) at a dose of 75 mg/kg exhibited marked inhibition against carrageenan-induced hind paw oedema. The anti-inflammatory effect induced by MEF, was comparable to that of the reference drug, indomethacin and as well as to the 750 mg/kg of HWE at 4 and 5 h.

Conclusions

(a) These findings rationalize the traditional usage of this plant as an anti-inflammatory agent and (b) membrane stabilizing properties and NO inhibitory activity are possible mechanisms through which Trichosanthes cucumerina mediates its anti-inflammatory action.     

In vivo anti-nociceptive and anti-inflammatory activities of the aqueous extract of the leaves of Piper sarmentosum

Ethnopharmacological relevance

Piper sarmentosum (Piperaceae) is a medicinal plant traditionally used by the Malays to treat headaches, toothaches, coughs, asthma and fever.

Aim of the study

In order to establish the pharmacological properties of the leaf of this plant, studies were performed on anti-nociceptive and anti-inflammatory activities.

Materials and methods

The aqueous extract of Piper sarmentosum (AEPS) was prepared in the doses of 30, 100 and 300 mg/kg. Anti-nociceptive activity of AEPS was evaluated by abdominal constriction and hot-plate tests. AEPS was also pre-challenged with 5 mg/kg naloxone to determine the involvement of opioid receptors. Anti-inflammatory activity was evaluated using carrageenan-induced paw edema assay.

Results

Subcutaneous administration of AEPS exhibited anti-nociceptive activity (P < 0.05) in a dose-dependent manner in the abdominal constriction and hot-plate tests. Pre-treatment with naloxone completely (P < 0.05) diminished the extract anti-nociceptive activity in both tests. The AEPS, at all doses used, exerted significant (P < 0.05) anti-inflammatory activity in a dose-dependent manner.

Conclusions

The AEPS exhibits opioid-mediated anti-nociceptive activity at the peripheral and central levels, as well as anti-inflammatory activity, which confirmed the traditional uses of the plant in the treatment of pain- and inflammatory-related ailments.     

Ultrastructural alterations of the tegument of Raillietina echinobothrida treated with the stem bark of Acacia oxyphylla (Leguminosae)

Ethnopharmacological relevance

The stem bark of Acacia oxyphylla Graham ex Bentham is used as an anthelmintic by the natives of Mizoram (North-East India).

Aim of the study

The present study was performed to evaluate whether or not the plant-derived components caused any ultrastructural changes in the tegumental interface of the parasite.

Materials and methods

The test parasite Raillietina echinobothrida, the cestode of domestic fowl, was exposed to the ethanolic crude extract and acetone fraction of stem bark of Acacia oxyphylla for varying concentrations and time duration and processed for transmission electron microscopy as soon as paralysis set in the treated parasites.

Results

Treatment with crude alcoholic extract and its acetone fraction revealed complete inactivation and flaccid paralysis of the cestode, which was soon followed by death. The treated parasites also exhibited intense vacuolization of the tegumental layers along with complete disorganization and/or erosion of microtriches.

Conclusions

Considerable structural alterations in the treated parasites are suggestive of an efficient vermicidal activity of the Acacia oxyphylla stem bark-derived botanicals against cestodes.     

Antinociceptive and anti-inflammatory effects of Thespesia populnea bark extract

The ethanolic extract of Thespesia populnea bark (TPE) was investigated for anti-inflammatory and analgesic activity at the doses (p.o.) of 100, 200 and 400mg/kg body weight. For evaluation of inflammation carrageenan-, histamine- and serotonin-induced paw edema served as acute models and formaldehyde-induced arthritis served as a chronic model in rats. The acetic acid-induced writhing response and formalin-induced paw licking time in the early and late phases of mice were used to assess analgesic activity. The higher doses of TPE (200 and 400mg/kg, p.o.) were inhibiting carrageenan, histamine and serotonin-induced paw edema as well as formaldehyde-induced arthritis successfully. In addition, TPE (200 and 400mg/kg, p.o.) significantly attenuated the writhing responses induced by an intraperitoneal injection of acetic acid and late phase of pain response induced by an subplantar injection of formalin in mice. Furthermore, our phytochemical studies indicated that the ethanolic extract of bark contains alkaloids, carbohydrates, protein, tannins, phenols, flavonoids, gums and mucilage, saponins and terpenes. From acute oral toxicity studies (OECD-423 guidelines), no mortality was observed even at highest dose of TPE (2000mg/kg, p.o.).     

Antioxidant and anti-inflammatory activities of the phenolic extracts of Sapium sebiferum (L.) Roxb. leaves

Ethnopharmacological relevance

The leaves of Sapium sebiferum have long been used in Traditional Chinese Medicine (TCM) for the treatment of eczema, shingles, edema, swelling, ascites, scabs, and snakebites, among other maladies.

Aim of this study

The present study aimed to investigate the antioxidant and anti-inflammatory effects of the phenolic extracts of Sapium sebiferum leaves using in vitro and in vivo models.

Materials and methods

The in vitro antioxidant activities of the extracts were measured using common chemical methods (total phenolic content; total flavonoid content; scavenging of DPPH·, ABTS+·, superoxide, and nitrite radicals; reducing power; β-carotene bleaching; and FTC assays). The in vivo topical anti-inflammatory activities were tested using the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced dermatitis animal model. The SOD and CAT activities and the GSH content of ear tissue were also determined using test kits.

Results

The extracts of Sapium sebiferum leaves exhibited strong in vitro antioxidant activities. They also showed significant (P<0.001) and dose-dependent anti-inflammatory activities in an acute dermatitis model at the doses of 0.03 mg/ear, 0.1 mg/ear, and 0.3 mg/ear. The application of Sapium sebiferum leaf extracts increased the SOD and CAT activities and the GSH content relative to those of the TPA treatment group. The anti-inflammatory effect of the Sapium sebiferum leaf extract was positively correlated with its antioxidant activity.

Conclusion

These results demonstrate that Sapium sebiferum leaf extract is an effective anti-inflammatory agent in the TPA-induced dermatitis model, and its anti-inflammatory effect is related, at least in part, to its antioxidant activity.