Evaluation of the wound healing property of Boesenbergia longiflora rhizomes

Ethnopharmacological relevance

The rhizomes of Boesenbergia longiflora (Wall.) Kuntze (Zingiberaceae) have been traditionally used for treatment of inflammatory bowel disease, ulcerative colitis, aphthous ulcer and abscess by decoction with alcohol.

Aim of the study

The rhizomes of Boesenbergia longiflora were carried out to investigate for anti-inflammatory and wound healing activities in order to support the traditional use.

Material and methods

The ethanolic extract of Boesenbergia longiflora and its fractions were tested using relevant in vitro anti-inflammatory and wound healing assays. For the in vitro studies, murine macrophage RAW264.7 cells and mouse fibroblast L929 cells were assessed for anti-inflammatory and fibroblast stimulatory activities, respectively. In vivo anti-inflammatory activity was determined by carrageenan-induced rat paw edema model as well as acute toxicity estimated by the up-and-down method in mice.

Results

The present study has demonstrated that the ethanolic extract of Boesenbergia longiflora rhizomes possesses a potent anti-inflammatory and wound healing activities. Among the isolated fractions, the CHCl₃ fraction showed potent anti-inflammatory effect through nitric oxide inhibitory activity (IC₅₀=5.5 μg/ml) and reduction of carrageenan-induced rat paw edema (ED₅₀=222.7 mg/kg), whereas this fraction exhibited wound healing property via fibroblast migration on both day 1 (77.3%) and day 2 (100%) as well as enhanced collagen production (187.5 μg/ml) at concentration of 3 μg/ml, compared to that of the controls, 39.4% for fibroblast and 60.8 μg/ml for collagen, respectively. The anti-inflammatory mechanism of the CHCl₃ fraction is found to suppress the iNOS and COX-2 mRNA expression.

Conclusion

The scientific investigation of wound healing activity of Boesenbergia longiflora rhizomes support the Thai traditional uses for treatment of inflammatory bowel disease, ulcerative colitis, aphthous ulcer and abscess. The EtOH extract and CHCl₃ fraction exert potential wound healing property through NO inhibition, anti-oxidant effect and stimulation of fibroblast migration and collagen production. The phytochemical screening revealed that the CHCl₃ fraction of Boesenbergia longiflora rhizomes contains diarylheptanoids, flavonoids and terpenes. The isolation of the compounds responsible for the wound healing effect is now in progress.     

NMR metabolomics for identification of adenosine A1 receptor binding compounds from Boesenbergia rotunda rhizomes extract

Ethnopharmacological relevance

Boesenbergia rotunda Linn. (Zingiberaceae) is traditionally used in many Asian countries as medicine for stomach pain and discomfort, viral and bacterial infection, inflammation, and as diuretic agent.

Aim of the study

The study aimed to identify adenosine A1 receptor binding compounds from Boesenbergia rotunda rhizome extract by using comprehensive extraction coupled to the NMR metabolomics method.

Materials and methods

Dried and powdered Boesenbergia rotunda rhizomes were extracted with the comprehensive extraction method to obtain several fractions with different polarity. Each fraction was divided into two: for NMR analysis and for adenosine A1 receptor binding test. Orthogonal projection to the least square analysis (OPLS) was used to study the correlation between metabolites profile and adenosine A1 receptor binding activity of the plant extracts. Based on Y-related coefficient and variable of important (VIP) value, signals in active area of OPLS loading plot were studied and the respective compounds were then elucidated

Results and discussions

Based on OPLS Y-related coefficient plot and variable of importance value plot, several characteristic signals were found to positively correlate to the binding activity. By using 1D and 2D NMR spectra of one of the most active fraction, pinocembrine and hydroxy-panduratin were identified as the possible active compounds. Two signals from ring C of pinocembrine flavanone skeleton with negative coefficient correlations possibly overlapped with those of non-active methoxylated flavanones which were also presence in the extract. NMR based metabolomics applied in this study was able to quickly identify bioactive compounds from plant extract without necessity to purify them. Further confirmation by isolating pinocembrine and hydroxy-panduratin and testing their adenosine A1 receptor binding activity to chemically validate the method are required.

Conclusion

Two flavonoid derivatives, pinocembrine and hydroxy-panduratin, have been elucidated as possible active compounds bind to adenosine A1 receptor. Flavonoid was reported to be one of natural antagonist ligand for adenosine A1 receptor while antagonistic activity to the receptor is known to associate with diuretic activity. Thus, the result of this research supports the traditional use of Boesenbergia rotunda rhizome extract as diuretic agent.     

Anti-inflammatory activity of the extracts and fractions from Erigeron multiradiatus through bioassay-guided procedures

Ethnopharmacological relevance

Erigeron multiradiatus (Lindl.) Benth., an herb that grows in the alpine and subalpine meadow of Qinghai-Tibet plateau, has been widely used as a folk remedy by the native people for treatment of various inflammatory ailments.

Aim of the study

In order to isolate and identify the active components of Erigeron multiradiatus for anti-inflammatory activity, a preliminary phytochemical study and a bioassay-guided fractionation and purification process was performed.

Material and Methods

The dry whole plant Erigeron multiradiatus was extracted with 50% ethanol and then separated into CHCl₃, n-BuOH, and aqueous fractions. The anti-inflammatory activities of each fraction were investigated using two in vivo inflammation models.

Results

These results exhibited varying degrees of anti-inflammatory activities and the n-BuOH fraction showed the strongest anti-inflammatory activities. The n-BuOH fraction was then subjected to separation and purification using macroporous resins column chromatography and Sephadex LH-20 leading to two flavonoids glucuronides identified as scutellarein-7-O-β-glucuronide and apigenin-7-O-β-glucuronide. Furthermore, LC–MS/MS identification and quantification of isolated compounds were also performed.

Conclusion

Scutellarein-7-O-β-glucuronide and apigenin-7-O-β-glucuronide were considered as major components and principally responsible for the anti-inflammatory activity of Erigeron multiradiatus. Thus the results of our study provide a scientific basis for the utilization of Erigeron multiradiatus in traditional Tibetan medicine.     

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.     

Anti-inflammatory activity of flavonoids from Eupatorium arnottianum

Three anti-inflammatory compounds: nepetin, jaceosidin and hispidulin have been isolated and identified from Eupatorium arnottianum Griseb. dichloromethane extract. Nepetin reduced the TPA mouse ear edema by 46.9% and jaceosidin by 23.2% (1mg/ear). Both compounds inhibited the NF kappaB induction by 91 and 77%, respectively. Furthermore phytochemical analysis of the ethanol extract has led to the identification of eriodictyol, hyperoside, rutin, caffeic and chlorogenic acids. All these compounds are reported for the first time in this species. The finding of topical antiinflammatory activity exerted by Eupatorium arnottianum extract and the identification of active principles could support the use of this plant for the treatment of inflammatory affections.     

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.     

Anti-inflammatory and analgesic activity of aqueous extract of Flos populi

Ethnopharmacological relevance

Flos populi is an important traditional Chinese medicine prepared from the male inflorescence of Populus tomentosa Carr. or Populus canadensis Moench (Salicaceae family). Flos populi is mainly used for the treatment of various inflammatory diseases and anti diarrhea in East Asian countries. The objective of this study was to investigate the anti-inflammatory and analgesic properties of the aqueous extract of Flos populi (FPAE).

Materials and methods

Cotton pellets-induced granuloma, carrageenan-induced paw oedema, arachidonic acid-induced right ear oedema and xylene-induced ear oedema were used to assess anti-inflammatory activity of FPAE and analgesic activity was evaluated by hot plate test, acetic acid-induced abdominal writhing test and formalin test.

Results

FPAE produced significant dose–response anti-inflammatory activity against cotton pellets-induced granuloma. FPAE at dosages of 50, 100 and 200 mg/kg b w. significantly reduced carrageenan-induced paw edema by 48.84% (P<0.05), 54.95% (P<0.05), and 62.05% (P<0.05) at 5 h after carrageenan injection, respectively. FPAE significantly (P<0.05) reduced the ear oedema induced by arachidonic acid and peaked at the dose of 200 mg/kg b w. (40.78%). A significant (P<0.05) dose dependent inhibition of xylene-induced oedema was produced by FPAE and peaked at the highest dose of 200 mg/kg b w. (23.95%). FPAE (50, 100 and 200 mg/kg b w.) produced significant dose–response analgesic activity in the hot-plate test. However, the low percentage inhibition (<50%) suggests that it is not a centrally acting analgesic. Extract at dosages of 50, 100 and 200 mg/kg b w., p.o. significantly reduced acetic acid-induced writhing by 39.6% (P<0.05), 45.4% (P<0.05), and 51.8% (P<0.05), respectively. The extract also caused marked dose-dependent inhibition of formalin-induced pain in the second phase (P<0.05).

Conclusion

The findings in this study suggest that the aqueous extract of Flos populi possesses anti-inflammatory and analgesic activities. These results may support the fact that this plant is used traditionally to cure inflammatory diseases.     

Anti-inflammatory activity of roots of Ecbolium viride (Forsk) Merrill

Ethnopharmacological relevance

Traditionally the aqueous extracts of dried roots of the plant Ecbolium viride are used for menorrhagia, rheumatism and jaundice.

Aim of the study

The aim was to evaluate the anti-inflammatory activity of Ecbolium viride extract in an in vivo model.

Materials and methods

The ethyl acetate fraction of Ecbolium viride root extract was prepared and administered orally to rats. The anti-inflammatory activity of Ecbolium viride was determined by carrageenan-induced paw edema and cotton pellet granuloma models.

Results

Oral administration of Ecbolium viride extract reduced inflammation significantly (P < 0.01) in both the carageenan paw edema and the cotton pellet granuloma models.

Conclusions

The results of the study supported the traditional use of Ecbolium viride in the treatment for inflammatory disease.     

Anti-inflammatory and anti-nociceptive properties of Prunus padus

Ethnopharmacological relevance

Prunus padus Linne has been widely used as a traditional medicine, with beneficial effects in numerous diseases, including stroke, neuralgia and hepatitis. In this study, we demonstrated anti-inflammatory and anti-nociceptive activities of the methylene chloride fraction of P. padus (MPP).

Materials and methods

In vitro studies, the anti-inflammatory effects of MPP were examined using IFN-γ/LPS-activated murine peritoneal macrophage model. To confirm the anti-inflammatory effects of MPP in vivo, trypsin-induced paw edema test was also conducted. The anti-nociceptive activities of MPP were measured using various experimental pain models including thermal nociception methods such as the tail immersion test and the hot plate test as well as chemical nociception methods like acetic acid-induced writhing test and formalin test. To determine whether analgesic activity of MPP is connected with the opioid receptor, we carried out combination test with naloxone, a nonselective opioid receptor antagonist.

Results

In the current study, MPP showed potent inhibitory effect on IFN-γ/LPS-induced NO production. MPP also suppressed not only iNOS enzyme activity but also iNOS expression. Moreover, MPP inhibited COX-2 expression dose dependently. IFN-γ/LPS stimulation induced the translocation of NF-κB to nucleus but it was attenuated in the presence of MPP. In vivo study revealed that MPP could reduce paw volume after subplantar injection of trypsin. In addition, MPP showed potent analgesic activities both thermal and chemical nociception compared to tramadol and indomethacin. Furthermore, pre-treatment of naloxone slightly suppress the analgesic activity of MPP indicating that MPP acts as a partial opioid receptor agonist.

Conclusions

In the present study, MPP showed potent anti-inflammatory properties through not only by suppressing various inflammatory mediators in vitro, but reducing the inflammatory edema in vivo. MPP also exhibited strong anti-nociceptive activities via both central and peripheral mechanism by acting as a partial opioid agonist. Based on these results we suggest that P. padus has the potential to provide a therapeutic approach to inflammation-mediated chronic diseases as an effective anti-inflammatory agent and painkiller.     

Anti-cancer activity of compounds from Bauhinia strychnifolia stem

Ethnopharmacological relevance

The stem and root of Bauhinia strychnifolia Craib (Fabaceae family) have been traditionally used in Thailand to treat fever, alcoholic toxication, allergy and cancer. An EtOH extract of Bauhinia strychnifolia showed good inhibitory activity against several cancer cell lines including HT-29, HeLa, MCF-7 and KB. As there has been no previous reports on chemical constituents of Bauhinia strychnifolia, this study is aimed to isolate the pure compounds with anti-cancer activity.

Materials and methods

Five pure compounds were isolated from EtOH extract of Bauhinia strychnifolia stem using silica gel, dianion HP-20 and sephadex LH-20 column chromatography and were tested for their cytotoxic effects against HT-29, HeLa, MCF-7 and KB cell lines using the Sulforhodamine B (SRB) assay.

Results

Among five compounds, 3,5,7,3′,5′-pentahydroxyflavanonol-3-O-α-l-rhamnopyranoside (2) possessed very potent activity against KB (IC₅₀=0.00054 μg/mL), HT-29 (IC₅₀=0.00217 μg/mL), MCF-7 (IC₅₀=0.0585 μg/mL) and HeLa cells (IC₅₀=0.0692 μg/mL). 3,5,7-Trihydroxychromone-3-O-α-l-rhamnopyranoside (3) also showed good activity against HT-29 (IC₅₀=0.02366 μg/mL), KB (IC₅₀=0.0412 μg/mL) and MCF-7 (IC₅₀=0.297 μg/mL), respectively. The activity of 2 (IC₅₀=0.00054 μg/mL) against KB cell was ten times higher than that of the positive control, Camptothecin (anti-cancer drug, IC₅₀=0.0057 μg/mL). All compounds did not show any cytotoxicity with normal cells at the concentration of 1 μg/mL.

Conclusion

This is the first report of compounds 2 and 3 on anti-cancer activity and based on the anti-cancer activity of extracts and pure compounds isolated from Bauhinia strychnifolia stem, it might be suggested that this plant could be useful for treatment of cancer.     

Anti-inflammatory activity of dried flower extracts of Aegle marmelos in Wistar rats

Ethnopharmacological relevance

Almost all part of the plant Aegle marmelos (Bael tree) has been used in the traditional medicine systems of Asian countries to treat various diseases over many centuries. The water extract of the dried flowers of Aegle marmelos is a commonly used beverage among Sri Lankan population in rural areas. Although extensive investigations done on many parts of the plant there are no experimental data available on the extracts of flowers. Anti-inflammatory effect of the water extract of dried flowers of Aegle marmelos (WEAM) was evaluated in the present study.

Materials and methods

The anti-inflammatory effect of the WEAM was evaluated by inhibition of the rat paw oedema, induced by carrageenan. The mechanism of the anti-inflammatory effect was assessed by the inhibition of production of nitric oxide (NO) by rat peritoneal cells, infiltration of rat peritoneal cells, anti-histamine effect, membrane stabilization activity, the antioxidant capacity and inhibition of lipid peroxidation by the WEAM.

Results

The maximum percentage inhibition of paw oedema was exhibited by the dose of 200 mg/kg at 2 h. The WEAM showed a significant increment of rat peritoneal cell infiltration, inhibition of NO production by rat peritoneal cells and inhibition of wheal formation on the skin of the rat after injection of histamine. The WEAM protected the erythrocyte membrane from heat-induced lysis in a dose-dependent manner and showed a significant anti-oxidant effect and lipid peroxidation inhibition activity.

Conclusion

The WEAM possesses significant anti-inflammatory effect by multiple mechanisms in Wistar rats.     

德国鸢尾化学成分研究

通过硅胶,Sephadex LH-20葡聚糖凝胶,ODS反相柱色谱等分离技术对鸢尾科Iridaceae植物德国鸢尾Iris germanica根茎的化学成分进行分离纯化,采用理化性质及波谱分析方法对分离得到的化合物进行结构鉴定。从该植物根茎中分离得到21个化合物,分别鉴定为商陆素（1）,5,3,3’-三羟基-7,4’-二甲氧基黄烷酮（2）,5,7,4’-三羟基双氢黄酮（3）,cirsiliol-4’-glucoside（4）,3β,4’-dihydroxy-7,3’-dimethoxy flavornone-5-O-β-D-glucopyranoside（5）,染料木素（6）,irilin D（7）,muningin（8）,5,7, 4’-三羟基-6,3’,5’-三甲氧基异黄酮（9）,鸢尾苷元（10）,野鸢尾苷元（11）,鸢尾苷（12）,野鸢尾苷（13）,芒果苷（14）,irisxanthone（15）,焦谷氨酸（16）,2,4’, 6-trihydroxy-4-methoxybenzophenone-2-O-β-D-glucoside（17）,茶叶花宁（18）,草夹竹桃苷（19）,β-谷甾醇（20）,胡萝卜苷（21）。其中化合物 1~9,16,17 为首次从德国鸢尾中分离得到,化合物 8,9 为首次从鸢尾属植物中分离得到,化合物 1,4,17 为首次从鸢尾科植物中获得。     

Evaluation of anti-inflammatory and mechanism of action of extract of Macrosiphonia longiflora (Desf.) Müll. Arg

Ethnopharmacological relevance

Macrosiphonia longiflora (Desf.) Müll. Arg (Apocynaceae), popularly known as ‘velame’ and ‘velame branco’, is a native subshrub that grows in the Brazilian Cerrado. This plant is widely used in traditional medicine in the form of decoction and infusion, particularly as anti-inflammatory, depurative, anti-rheumatic, antisyphilitic and antiulcer remedy. There is no available information in the literature that has addressed its pharmacological activity and phytochemical analysis.

Aim of the study

This study aimed to evaluate the anti-inflammatory pharmacological profile of the hydroethanolic extract of Macrosiphonia longiflora, using in vivo and in vitro acute inflammation experimental models, as well as investigate the roles of cytokines and nitric oxide in its mechanism of action, and including phytochemical analysis constitution of its hydroethanolic extract.

Materials and methods

Hydroethanolic (70%) extract of Macrosiphonia longiflora (HEMl) was prepared by maceration. The preliminary phytochemical analysis was performed according to procedures described in the literature. Selected secondary metabolites detected were quantified by spectrophotometry and high performance liquid chromatography (HPLC). Its cytotoxic potential in Chinese hamster ovary (CHO-k1) epithelial cell lines was evaluated using Alamar Blue. in vivo anti-inflammatory activity was evaluated with carrageenan- and dextran-induced paw edemas, carrageenan-induced pleurisy in rats and lipopolysaccharide (LPS)-induced peritonitis in mice. The in vitro anti-inflammatory activity was evaluated using RAW 264.7 cells stimulated with LPS and interferon (INF)-γ. Effects of HEMl on the inflammatory cytokines (IL-1β, IL-10, IL-17, INF-γ and TNF-α) concentrations in the peritoneal lavage were evaluated using commercial ELISA kits, while the Griess method was employed to determine nitric oxide (NO) concentrations in the peritoneal lavage, as well as in the supernatants of RAW 264.7 cells.

Results

Preliminary phytochemical analysis, revealed the presence of phenolics compounds, terpenoids, alkaloids and flavonoids. Spectrophotometric analysis revealed the presence of relatively high content of phenolics and flavonoids in HEMl. HPLC analysis confirmed the presence of the quantified compounds and demonstrated the presence of ellagic acid in the detected matrix of compounds. HEMl appeared to be non-cytotoxic. It effectively inhibited (p<0.05) paw edema induced by carrageenan and dextran. Furthermore, HEMl also significantly reduced exudates volume and leukocyte migration in the carrageenan-induced pleurisy and LPS-induced peritonitis, neutrophils counts in LPS-induced peritonitis. HEMl also acts by effectively inhibiting the following inflammatory cytokines: IL-1β and IL-10 levels in the peritoneal lavage, but had no effect on IL-17 level in the peritonitis model. In addition, HEMl had no effect on the levels of tumor necrosis factor alpha (TNF-α) present in the peritoneal lavage and cells supernatants. The concentration of NO, as assessed by measurement of nitrite (NO₂⁻), showed that pretreatment with HEMl reduced NO significantly in the peritoneal lavage and in RAW 264.7 cells co-stimulated with LPS and INF-γ.

Conclusion

The results obtained in this study indicate that HEMl possesses very low cytotoxic potential. In addition, it demonstrated a potent anti-inflammatory activity in both the in vivo and in vitro models of acute inflammation. The anti-inflammatory effect is partly related to the inhibition of IL-1β, IL-10, and nitric oxide releases, but independent of TNF-α and IL-17 modulation. Phytochemical analysis revealed the predominant presence of the flavonoids (naringin, rutin, myricetin, morin, quercetin, (±)-naringenin, and luteolin) and phenols (ellagic acid), which are possibly involved in the anti-inflammatory effect of HEMl. The current study provided supportive evidence for the popular use of HEMl in the treatment of inflammatory conditions, and shed more light on the possible roles of the inflammatory cytokines in its mechanisms of action as anti-inflammatory agent.     

Anti-inflammatory activity of Chrysanthemum indicum extract in acute and chronic cutaneous inflammation

Aim of the study

Although Chrysanthemum indicum Linné (Compositae) has long been used in traditional Korean, Chinese, Japanese medicine to treat various immune-related diseases the underlying mechanism(s) by which these effects are induced remains to be defined in vivo model system. We investigated the effects of 70% ethanolic extract from Chrysanthemum indicum Linné (CIE) on skin inflammation in mice.

Materials and methods

Production of pro-inflammatory cytokines (TNF-α and IL-1β), activation of myeloperoxidase, and histological assessment were examined in acute and chronic skin inflammation using 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-induced mouse ear edema.

Results

CIE inhibited topical edema in the mouse ear, following administration at 200 mg/kg (i.p.), leading to substantial reductions in skin thickness and tissue weight, inflammatory cytokine production, neutrophil-mediated myeloperoxidase activity, and various histopathological indicators. Furthermore, CIE was effective at reducing inflammatory damage induced by chronic TPA exposure.

Conclusions

These results demonstrate that CIE is an effective anti-inflammatory agent in murine phorbol ester-induced dermatitis, and suggest that the extract may have therapeutic potential in a variety of immune-related cutaneous diseases.     

旋覆花中化学成分及其活性研究

综合运用硅胶柱色谱、凝胶柱色谱、制备HPLC色谱分离方法分离纯化旋覆花中的化学成分,采用NMR和质谱等有机波谱学方法鉴定各单体化合物的结构,进一步测试各化合物的抗炎活性。从旋覆花乙酸乙酯提取物中分离得到15个化合物,鉴定为二氢芥子醇（1）,（3S,5R,6S,7E）-5,6-epoxy-3-hydroxy-7-megastigmen-9-one（2）,（6R,7E）-9-hydroxy-4,7-megastigmadien-3-one（3）,阿里二醇（4）,蒲公英醇乙酸酯（5）,8,9,10-三羟基百里香酚（6）,花旗松素（7）,木犀草素（8）,泽兰黄酮（9）,泽兰黄醇素（10）,菠叶素（11）,槲皮素（12）,对羟基桂皮酸（13）,咖啡酸（14）,咖啡酸乙酯（15）。化合物 1,2,7,13,15 为首次从该属植物中分离得到,化合物 3,4,9~11,14 为首次从该种植物中分离得到。抗炎活性测定结果表明,化合物 3,6~12,14 具有明确的抑制c-Kit Ligand（KL） 诱导的肥大细胞白三烯C₄ （LTC₄） 生成和脱颗粒的作用,而且化合物 8和12 具有较强的抑制脂多糖（LPS）诱导的巨噬细胞RAW264.7细胞一氧化氮（NO） 释放作用。首次报道了黄酮类化合物 7,9~11 对LTC₄和肥大细胞脱颗粒具有较强的抑制作用。     

黑刺菝葜根茎中苯丙素和二苯乙烯类化学成分的研究

运用硅胶,Sephadex LH-20等各种色谱技术对黑刺菝葜Smilax scobinicaulis根茎的化学成分进行研究.通过波谱数据的分析鉴定化合物的结构分别为白藜芦醇3-O-β-D-葡萄糖基-(1→3)-β-D-葡萄糖苷(1),白藜芦醇(2),δ-葡萄素(3),咖啡酸乙酯(4),1-O-咖啡酰甘油酯(5),1-O-对香豆酰基甘油酯(6),1-O-阿魏酰甘油酯(7),大海米酰胺(8),桑辛素M(9).其中化合物1为新化合物,化合物3～5,8,9为首次从该植物中分离得到.     

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 effect of a methanolic extract of leaves of Dregea volubilis

Aim of study

The aim of this study was to establish the anti-inflammatory activity of the methanolic extract of Dregea volubilis leaves (MEDV) with its fractions and to delineate the possible mechanism of action for MEDV.

Materials and methods

The anti-inflammatory activities of MEDV along with its petroleum ether and chloroform fractions were evaluated in a carrageenan induced model of acute inflammation. The effect of MEDV on lipopolysaccharide induced production of nitric oxide (NO) in macrophages was also studied.

Results

MEDV (100, 200 and 400 mg/kg body weight) significantly reduced carrageenan induced paw edema; chloroform fraction was most potent (66%, p < 0.001). MEDV was non-toxic up to 125 μg/ml in mouse peritoneal macrophages wherein it (0-100 μg/ml) reduced lipopolysaccharide induced NO production.

Conclusion

MEDV possesses significant anti-inflammatory activity. Chloroform fraction of MEDV showed best anti-inflammatory activity.     

In vitro antimicrobial activity of extracts and compounds of some selected medicinal plants from Cameroon

Aim of the study

Seven extracts and eight compounds from four selected Cameroonian medicinal plants, Solanecio mannii Hook f. (Asteraceae), Monodora myristica Dunal (Annonaceae), Albizia gummifera (J.F. Gmel) C.A. Smith (Fabaceae/Mimosoideae) and Glyphaea brevis (Spreng) Monachino (Tiliaceae), traditionally used for the treatment of hepatitis, parasites and other infectious diseases, were tested in vitro for their antimicrobial activity against Gram-positive (5 species) and Gram-negative (4 species) bacteria species and pathogenic yeasts (2 Candida species), to establish whether or not they have antimicrobial activity and to validate scientifically their use in traditional medicine.

Materials and methods

The agar disc diffusion and the microbroth dilution methods were used to determine the zone of inhibition between the edge of the filter paper and the edge of the inhibition area (IZ) and the minimal inhibitory concentration (MIC) respectively.

Results

The most active extracts against Candida albicans and Candida krusei were respectively the cyclohexane extract from the fruits of Monodora myristica and the ethyl acetate extract from the stem bark of Albizia gummifera (MIC = 6.3 μg/ml for both extracts). The lowest MIC value (1.6 μg/ml) for purified compounds was obtained on Candida albicans with a mixture of linear aliphatic primary alcohols (n-C24H50O to n-C30H62O), with n-hexacosanol (1b) as major compound and mixture of fatty acid esters of diunsaturated linear 1,2-diols (6).

Conclusion

These results afford ground informations for the potential use of the crude extracts of these species as well as of some of the isolated compounds in bacterial and fungal infections.     

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.