WIN-34B,a new herbal medicine,inhibits the inflammatory response by inactivating IκB-α phosphorylation and mitogen activated protein kinase pathways in fibroblast-like synoviocytes

Ethnopharmacological relevance

The dried flowers of Lonicera japonica Thunb and dried roots of Anemarrhena asphodeloides BUNGE have been used for the treatment of a variety of inflammatory diseases in traditional Korean medicine.

Objective

The aim of the study is to evaluate the anti-inflammatory effects of WIN-34B, a new herbal medicine, in fibroblast-like synoviocytes (FLS) obtained from patients with osteoarthritis (OA).

Materials and methods

WIN-34B is isolated from the n-butanol fraction of dried flowers of L. japonica and dried roots of A. asphodeloides. The anti-inflammatory effects of WIN-34B on cell viability, the production and release of inflammatory mediators, matrix metalloproteinases (MMPs), aggrecanases, tissue inhibitor of matrix proteinases (TIMP) is compared with celecoxib in IL-1β-stimulated human OA FLS. Furthermore, the effect of WIN-34B on inhibitory kappa B-α (IκB-α) phosphorylation and mitogen-activated protein kinases (MAPK) in the IL-1β-stimulated OA FLS was also evaluated.

Results

WIN-34B significantly inhibited the IL-1β-induced cell viability in human OA FLS without cytotoxicity. Compared to celecoxib, WIN-34B exhibited similar or better anti-inflammatory effects through significant suppression of inflammatory mediators (IL-1β, TNF-α, PGE2 and NO), MMPs (MMP-1, MMP-3 and MMP-13) and aggrecanases (ADAMTS-4 and ADAMTS-5), and enhancement of TIMPs (TIMP-1 and TIMP-3). Moreover, WIN-34B reduced the phosphorylation of IκB-α, ERK1/2, p38 and JNK1/2 in IL-1β-stimulated OA FLS.

Conclusions

WIN-34B exhibited similar or better anti-inflammatory properties in IL-1β-stimulated OA FLS compared to celecoxib. The anti-inflammatory effects of WIN-34B are due to inhibition of inflammatory mediators (IL-1β, TNF-α, PGE2 and NO) and regulation of MMPs, ADAMTSs and TIMPs via the inhibition of IκB-α and MAPK phosphorylation in IL-1β-stimulated OA FLS.     

Gastroprotective and safety effects of WIN-34B, a novel treatment for osteoarthritis, compared to NSAIDs

Ethnopharmacological relevance

The dried flowers of Lonicera japonica, also known as Japanese honeysuckle, and the dried root of Anemarrhena asphodeloides, the component herbs of WIN-34B, are traditionally used in Eastern medicine to treat various inflammatory conditions including arthritis.

Objective

To study the acute and chronic toxicities of WIN-34B and to compare its effects on gastric mucosa with those of diclofenac, a widely used NSAID, and celecoxib, a selective COX-2 inhibitor.

Materials and methods

To investigate acute toxicity, we orally administered a single dose of 5000 mg/kg WIN-34B to rats. To investigate chronic toxicity, we orally administered 500, 1000 or 2000 mg/kg WIN-34B to rats daily for 13 weeks. To assess its effects on gastric mucosa, rats received either a single dose or repeated doses of WIN-34B (400, 1000, or 2000 mg/kg), diclofenac (10, 40, or 80 mg/kg), celecoxib (100 or 1000 mg/kg), or vehicle, after which samples of gastric mucosa were assessed grossly and histologically. We also measured tissue activity of myeloperoxidase and synthesis of eicosanoids, including prostaglandin E₂ (PGE₂) and leukotriene B₄ (LTB₄). To further assess its effects, we administered WIN-34B to rats either intraperitoneally or orally, measured gastric injury scores using a rat model of diclofenac-induced gastric injury, and measured eicosanoid synthesis.

Results

WIN-34B showed no signs of acute or chronic toxicity in terms of general behavior, gross appearance of the internal organs, blood chemistry, or mortality. WIN-34B did not cause significant gastric mucosal damage after single or repeated doses. In contrast, diclofenac and celecoxib both caused gastric damage. In terms of eicosanoid synthesis, WIN-34B significantly suppressed LTB₄ synthesis while both diclofenac and celecoxib increased LTB₄ synthesis. WIN-34B slightly reduced PGE₂ production, while both diclofenac and celecoxib significantly reduced PGE₂ production. In a rat model of diclofenac-induced gastric injury, WIN-34B significantly suppressed LTB₄ synthesis and restored PGE₂ release.

Conclusions

These results demonstrate that WIN-34B did not cause acute or chronic toxicity in male or female rats. In addition, WIN-34B did not cause significant gastric mucosal damage, instead appearing to protect the mucosa from diclofenac-induced gastric damage through the regulation of PGE₂ and LTB₄.     

金银花气味与化学成分的相关性分析

该文通过测定金银花的气味及其化学成分绿原酸、木犀草苷和多酚类的含量,将气味综合指标值与化学成分指标值相联系,探索气味与化学成分之间的相关性。实验中利用数字化气味指纹分析仪(电子鼻)测量金银花的气味;采用高效液相色谱法测定金银花样品中绿原酸、木犀草苷的含量,用紫外-可见分光光度法测多酚类的含量;最后采用SPSS 17.0软件分析金银花气味与化学成分之间的相关性。结果显示金银花气味综合指标值与绿原酸、多酚类含量有显著性相关关系(正相关),并且建立了回归方程;与木犀草苷之间不存在显著相关关系。进而证明金银花的气味与其内在的化学成分密切相关,能为初步判断或预测金银花中化学成分的含量提供一种新思路、新方法。     

金银花类药用植物IspE和IspH基因克隆和生物信息学分析

目的:克隆金银花类药用植物4-二磷酸胞苷-2-C-甲基赤藓糖激酶(4-diphosphocytidyl-2-C-methyl-D-erythritol kinase,IspE)和4-羟基-3-甲基-2-邻苯基二磷酸还原酶(4-hydroxy-3-methylbut-2-enyl diphosphate reductase,IspH)基因,并对其基因序列、蛋白特性和转录活性进行分析、比较.方法:从忍冬Lonicera japonica转录组测序结果中分析获得了IspE,IspH基因.分别以忍冬、红白忍冬L.japonica var.chinensis、红腺忍冬L.hypoglauca和水忍冬L.dasystyla新鲜花蕾为材料,利用RT-PCR技术克隆获得了4种金银花类药用植物IspE和IspH基因的全长cDNA.运用生物信息学分析软件,预测编码蛋白的结构和功能,并通过RT-PCR检测IspE和IspH在忍冬、红白忍冬、红腺忍冬、水忍冬花蕾中的转录情况.结果:金银花类药用植物IspE基因含有1个完整的开放阅读框,长度为1 221 bp,编码406个氨基酸;IspH含有一个完整的开放阅读框,长度为1 380 bp,编码459个氨基酸.IspE和IspH均为非分泌蛋白,均定位于叶绿体中.RT-PCR分析结果表明在忍冬、红腺忍冬和水忍冬的花蕾中IspE,IspH基因的转录水平没有显著差异,但红白忍冬花蕾中IspE,IspH基因的转录水平均显著高于忍冬.结论:克隆获得忍冬、红白忍冬、红腺忍冬和水忍冬中IspE,IspH基因,并证实了其在不同金银花类药用植物中的表达,为进一步研究IspE,IspH基因对萜类化合物生物合成和花香气以及颜色的影响奠定了基础.     

金银花花中活性成分含量及其相关酶活性的动态变化规律研究

目的: 研究不同花期金银花中活性成分含量及其相关次生代谢过程中关键酶活性的动态变化规律,为确定金银花最佳采收期,调控金银花质量和相关管理规范提供指导. 方法: 测定金银花不同花期苯丙氨酸解氨酶(PAL)、多酚氧化酶(PPO)、过氧化物酶(POD)的活性,以及总酚、总黄酮、绿原酸、花色苷等活性成分的含量. 结果: 从三青期到金花期,金银花中总酚、总黄酮和花色苷的含量呈下降趋势,三青期达到最高值,分别为4.04,6.71,0.26 mg·g^-1,绿原酸在三青期达到最高值,为0.968 mg·g^-1,大白期达到最低值,后又小幅升高.PAL,PPO,POD的活性从三青期逐渐下降,到银花期达到最低值,同三青期相比,三者的下降幅度分别为43%,62%,56%,后到金花期略有上升. 结论: 在金花期之前,金银花中的PPO,POD活性与酚类物质程正相关.在金银花成熟期,由于呼吸作用的加强,诱导POD活性上升,使POD成为金银花成熟阶段催化酚类物质氧化为醌的关键酶,即POD是控制金银花成熟阶段活性成分含量的关键酶.     

忍冬5个农家品种花粉形态比较观察

目的:比较山东主产区忍冬5个农家品种花粉形态特征,为品种划分及良种选育提供依据.方法:扫描电镜观察花粉粒形态及表面纹饰,数据采用SAS 9.1统计软件分析.结果:忍冬不同农家品种花粉粒大小、萌发孔及表面刺突的长短、疏密等均有一定差异.其中,大鸡爪的花粉粒及其萌发孔长度最大,分别为61.97μm×61.79μm,18.03μm,红梗子的花粉粒及其萌发孔长度最小,分别为57.46μm×57.29μm,16.55μm.结论:花粉粒形态特征可作为忍冬不同农家品种划分的参考.     

Jiawei-Yupingfeng-Tang,a Chinese herbal formula,inhibits respiratory viral infections in vitro and in vivo

Ethnopharmacological relevance

Jiawei-Yupingfeng-Tang (JYT) is a Chinese herbal formula that is widely used to treat respiratory tract illness. However, the effect of JYT on respiratory viruses remains unknown. The influenza virus (IFV) and the human respiratory syncytial virus (HRSV) cause millions of cases of severe illness per year, and many of these illnesses develop into lethal pneumonia. The aim of this study is to evaluate whether JYT can be used to treat these infections.

Materials and methods

The effect of JYT against IFV and HRSV was tested using a plaque reduction assay in the lower respiratory tract cell line A549. The expression of ICAM-1 was determined by real-time RT-PCR and western blotting. A mouse model infected with lethal influenza developing into interstitial pneumonia was used to evaluate the effect of JYT in vivo.

Results

JYT extract inhibited both IFV and HRSV in a dose-dependent manner when given before, during and after a viral infection. JYT was effective in blocking the entry of the virus. Furthermore, pre-treatment with JYT reduced the susceptibility of cells to the invasion of HRSV by inhibiting the expression of ICAM-1. Importantly, JYT extract increased the survival rate of lethal influenza-infected mice, prolonged the survival time and alleviated the virus-induced lung lesions, which is comparable with the effects of ribavirin treatment.

Conclusions

These data support JYT as an alternative modality to be used in the treatment of respiratory viral infection induced by HRSV and IFV.     

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.     

In vivo antimalarial activity of Keetia leucantha twigs extracts and in vitro antiplasmodial effect of their constituents

Ethnopharmacological relevance

The West African tree Keetia leucantha (Rubiaceae) is used in traditional medicine in Benin to treat malaria. The twigs dichloromethane extract was previously shown to inhibit in vitro Plasmodium falciparum growth with no cytotoxicity (>100 µg/ml on human normal fibroblasts).

Materials and methods

The dichloromethane and aqueous extracts of twigs of K. leucantha were evaluated in vivo against Plasmodium berghei NK 173 by the 4-day suppressive test and in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity. Bioguided fractionations were realized and compounds were structurally elucidated using extensive spectroscopic analysis.

Results

The in vivo antimalarial activity of K. leucantha dichloromethane and aqueous twigs extracts were assessed in mice at the dose of 200 mg/kg/day. Both extracts exhibited significant effect in inhibiting parasite growth by 56.8% and 53.0% (p<0.0001) on day 7-postinfection. An LC–MS analysis and bioguided fractionations on the twigs dichloromethane extract led to the isolation and structural determination of scopoletin (1), stigmasterol (2), three phenolic compounds: vanillin (3), hydroxybenzaldehyde (4) and ferulaldehyde (5), eight triterpenic esters (6–13), oleanolic acid and ursolic acid. The antiplasmodial activity of the mixture of the eight triterpenic esters showed an antiplasmodial activity of 1.66±0.54 µg/ml on the 3D7 strain, and the same range of activity was observed for isolated isomers mixtures.

Conclusions

This is the first report on the in vivo activity of K. leucantha extracts, the isolation of thirteen compounds and analysis of their antiplasmodial activity. The results obtained may partially justify the traditional use of K. leucantha to treat malaria in Benin.     

From popular use to pharmacological validation: A study of the anti-inflammatory,anti-nociceptive and healing effects of Chenopodium ambrosioides extract

Ethno-pharmacological relevance

Chenopodium ambrosioides (Amarantaceae) is an annual or perennial plant popularly known as ‘erva de Santa Maria’, ‘mastruço’ and ‘erva-do-formigueiro’. This herb is used in folk medicine in the form of teas, poultices and infusions for inflammatory problems, contusions and lung infections, and as an anthelmintic and anti-fungal.

Aim of the study

The aim of the present study was to further the understanding of the anti-nociceptive, anti-inflammatory and wound healing effects of ethanol extract (EE) obtained from the leaves and stems of Chenopodium ambrosioides in animal models of acute pain, inflammation and wound healing, thus supporting its medicinal use for the treatment of pain and inflammatory conditions

Materials and methods

The anti-nociceptive activity of EE (150–500 mg/kg) was evaluated using the nociception induced by formalin (2.5%), prostaglandin-E₂ (PGE2; 3 nmol/paw), capsaicin (CAP, 1.6 μg/paw) and bradykinin (BK, 10 nmol/paw). The anti-inflammatory activity of EE (150–500 mg/kg) was evaluated in carrageenan- (Cg, 300 μg/paw), PGE₂- (3 nmol/paw), substance P- (SP, 20 nmol/paw) and BK- (3 nmol/paw) induced paw oedema. The topical anti-inflammatory activity of EE (1%, 3% and 5%) was evaluated in arachidonic acid- (AA, 2 mg/ear), oil croton- (1 μg/ear) and CAP- (250 μg/ear) induced ear oedema. The effect of this extract in the inhibition of the influx of neutrophil, myeloperoxidase (MPO) and adenosine-deaminase (ADA) activities and nitric oxide (NO) and TNF-á levels was also determined using the mouse of pleurisy induced by Cg. The excision wound model in rats was used to evaluate the wound healing efficacy of EE (1%, 3% and 5%). To exclude the possible non-specific muscle relaxant or sedative effects of EE, mice motor performance was also evaluated with the rota-rod test.

Results

EE (5% per ear) was effective in reducing ear oedema induced by croton oil by 78.09%, CAP by 70.85% and AA by 77.02%. EE (500 mg/kg; p.o.) also significantly inhibited paw oedema induced by Cg by 40%, PGE₂ by 51%, SP by 56% and BK by 57%. EE (500 mg/kg; p.o.) inhibited the cell influx of leucocytes by 78% and neutrophils by 53%, MPO activity by 62.22% and ADA activity by 23.07%, as well as NO by 77.77% and TNF-á levels by 50% in the fluid leakage due to the carrageenan-induced pleurisy. EE also inhibited the formalin-induced nociceptive in both phases of pain (neurogenic and inflammatory) at a dose of 500 mg/kg, resulting in inhibitions of 77.39% and 95.60%, respectively. EE (500 mg/kg; p.o.) was also effective in inhibiting the nociception induced by PGE₂ (68%), CAP (53%) and BK (32%). Topical application of EE (5%) on excision wounds caused a significant reduction in wound area when compared with the untreated controls. Finally, treatment with EE (150–500 mg/kg) did not show any significant alterations in motor performance or body temperature compared with the control group.

Conclusions

The results, including the inhibition of mediators (BK, NO, SP, PGE₂ and TNF-á) and enzyme (MPO and ADA) activity, validate the use of the plant under study for therapeutic treatment of anti-inflammatory, painful and wound healing processes.     

Screening of analgesic and anti-inflammatory activities of Citrullus colocynthis from southern Tunisia

Ethnopharmacological relevance

Inflammations and immune-related diseases such as rheumatoid arthritis are growing global concerns. Most of the drugs from plants which have become important in modern medicine had a folklore origin and are traditional in systems of medicine. Citrullus colocynthis Schrad. (cucurbitaceae), endemic in Southern Tunisia, is used in folk medicine to treat many inflammation diseases.

Aim of study

To evaluate the acute toxicity of different parts of Citrullus colocynthis and then to screen the analgesic and anti-inflammatory activities of aqueous extracts from roots and stems of the plant and from fruits and seeds at different maturation stages.

Materials and methods

After identification and acute toxicity assay Citrullus colocynthis Schrad. aqueous extracts were screened for analgesic and anti-inflammatory activities using, respectively, the acetic acid writhing test in mice and the carrageenan-induced paw edema assay in rats.

Results

All extracts displayed analgesic and anti-inflammatory activities at different doses without inducing acute toxicity. Topic results were obtained with immature fruits followed by seeds. The stem and root extracts were shown to possess the less significant inhibitory activity against analgesic and anti-inflammatory models.

Conclusions

Based on this study, we confirmed that Citrullus colocynthis Schrad. is a potentially useful drug suitable for further evaluation for rheumatoid arthritis, and its folk medicinal use as an analgesic and anti-inflammatory agents is validated.     

Identification of Escherichia coli enterotoxin inhibitors from traditional medicinal herbs by in silico, in vitro, and in vivo analyses

Ethnopharmacological relevance

Glycyrrhiza uralensis has been used for the treatment of gastrointestinal disorders, such as diarrhea, in several ancient cultures. Glycyrrhizin is the principal component of liquorice and lots of pharmacological effects have been demonstrated.

Aim of the study

Heat-labile enterotoxin (LT), the virulence factor of enterotoxigenic Escherichia coli, induces diarrhea by initially binding to the G_M1 on the surfaces of intestinal epithelial cells and consequently leading to the massive loss of fluid and ions from cells. Therefore, we evaluated the inhibitory effects of traditional medicinal herbs (TMH) on the B subunit of LT (LTB) and G_M1 interaction.

Materials and methods

The inhibitory effects of TMH on LTB-G_M1 interaction were evaluated by G_M1-enzyme-linked immunosorbent assay (ELISA). The likely active phytochemicals of these TMH were then predicted by in silico model (docking) and analyzed by in vitro (G_M1-ELISA) and in vivo (patent mouse gut assay) models.

Results

We found that various TMH, which have been ethnomedically used for the treatment of diarrhea, inhibited the LTB-G_M1 interaction. Docking data showed that triterpenoids were the most active phytochemicals and the oleanane-type triterpenoids presented better LTB-binding abilities than other types of triterpenoids. Moreover, by in vitro and in vivo models, we demonstrated that glycyrrhizin was the most effective oleanane-type triterpenoid that significantly suppressed both the LTB-binding ability (IC₅₀ = 3.26 ± 0.17 mM) and the LT-induced fluid accumulation in mice.

Conclusions

We found an LT inhibitor, glycyrrhizin, from TMH by in silico, in vitro, and in vivo analyses.     

In vitro and in vivo anti-hepatitis B virus activities of the lignan niranthin isolated from Phyllanthus niruri L.

Ethnopharmacological relevance

Niranthin is a lignan isolated from Phyllanthus niruri L. This plant has long been used in folk medicine for liver protection and antihepatitis B in many Asian countries. This study was designed to evaluate the anti-hepatitis B virus activity of niranthin using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models.

Materials and methods

Niranthin was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after niranthin was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100 mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks.

Results

In the human HBV-transfected liver cell line HepG2.2.15, the secretion of HBsAg and HBeAg were significantly decreased after treatment with niranthin for 144 h, with IC₅₀ values for HBsAg of 15.6 µM, IC₅₀ values for HBeAg of 25.1 µM. In DHBV-infected ducklings, niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of niranthin.

Conclusion

The experimental data demonstrated that niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo.     

In vitro and in vivo antimalarial activity and cytotoxicity of extracts and fractions from the leaves,root-bark and stem-bark of Triclisia gilletii

Ethnopharmacological Relevance

To evaluate the in vitro antiplasmodial activity and cytotoxicity, and the in vivo activity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii (De Wild) Staner (Menispermaceae), used in traditional medicine against malaria.

Materials and Methods

The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root-bark of Triclisia gilletii were tested in vitro for their antiplasmodial activity against a Congolese-sensitive strain of Plasmodium falciparum, against the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum, for cytotoxicity against MRC-5 cells, and in vivo in mice infected with Plasmodium berghei berghei.

Results

Many samples from the three plant parts exhibited pronounced activity against the Congolese chloroquine-sensitive strain of Plasmodium falciparum with some IC₅₀ values <0.02 µg/ml, and against the K1 strain, with some IC₅₀ <0.25; the selectivity was higher against the Congolese strain. At oral doses of 200 and 400 mg/kg body weight in infected mice, the aqueous, 80% methanol and total alkaloid extracts from the three plant parts produced more than 65% and 75% chemosuppression, respectively. The antiplasmodial activity of these three plant parts of Triclisia gilletii can at least in part be attributed to bisbenzylisoquinoline alkaloids, and supports its use for the treatment of uncomplicated malaria in traditional medicine.     

In vivo analgesic activity,toxicity and phytochemical screening of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine

Ethnopharmacological relevance

Psidium cattleianum Sabine is extensively used in Brazilian traditional medicine to treat several diseases including painful disorders. Aim of the study to investigate the toxicity and the possible analgesic activities of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine (ELPCS), to support its use in folk medicine. To screen the major phytochemical constituents of this extract and evaluate their antioxidant activity.

Materials and methods

ELPCS was assessed for its antioxidant activity using the DPPH model. Its analgesic activity was examined using mouse models of acetic acid-induced writhing and hot plate paw licking models. The major phytochemical constituents of the extract were screened; their toxicity on LLC-MK2 mammalian cells was evaluated.

Results

ELPCS exhibited significant peripheral analgesic activity at doses of 60, 80, 100, 200 and 400 mg/kg in mice, but it did not display central analgesic activity and not was toxic to LLC-MK2 cell (LD₅₀>400 µg/mL). The extract exhibited free radical scavenging activity as evidenced by IC₅₀ values (15.9 µg/mL) obtained by the DPPH method. Phytochemical screening detected flavonoids, saponins, cardiac glycosides, anthraquinones, and tannins.

Conclusions

The results of the experimental studies proved the analgesic activity of ELPCS and supported the traditional use of this plant.     

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.     

Antimicrobial,anti-inflammatory,anti-ulcer and antioxidant activities of Carlina acanthifolia root essential oil

The root of Carlina acanthifolia All. (Asteraceae) has been traditionally used in the treatment of various disorders including stomach and skin diseases. We studied antimicrobial, anti-inflammatory, anti-ulcer and antioxidant activities of Carlina acanthifolia root essential oil, in order to validate some of the ethnopharmacological claims. Antimicrobial activity was tested on 15 bacteria and three strains of fungi using the agar diffusion and broth microdilution methods. In assessing anti-inflammatory activity the carrageenan-induced rat paw oedema test was used, while ethanol-induced stress gastric ulcer test in rats was used in testing anti-ulcer activity. Antioxidant properties were evaluated trough the effect of the essential oil on lipid peroxidation (TBA assay) and its capability of quenching 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH radicals. The oil expressed significant antimicrobial activity, being the most active against Gram (+) bacteria: Streptococcus pyogenes, Enterococcus faecalis, Bacillus subtilis and against Candida albicans. In all applied concentrations, Carlina acanthifolia root essential oil reduced carrageenan-induced rat paw oedema in dose-dependent manner, achieving high degree of anti-inflammatory activity. The effect was comparable with that of indomethacin used as a reference drug. In the ethanol-induced stress gastric ulcer test in rats, it was shown that the tested essential oil produced significant dose-dependent gastroprotective activity. The results also pointed out substantial and dose-dependent antioxidant activity of the investigated essential oil, with carlina oxide as the main antioxidant component.