Inhibition of Lipid Peroxidation by Sesquiterpenoid in Heterotheca inuloides

A sesquiterpenoid, 7-hydroxy-3,4-dihydrocadalin, isolated from a Mexican medicinal plant Heterotheca inuloides was evaluated as an antioxidant. This sesquiterpenoid inhibited mitochondrial and microsomal lipid peroxidation induced by Fe(III)-ADP/NADH or Fe(III)-ADP/NADPH. Furthermore, 7-hydroxy-3,4-dihydrocadalin protected red cells against oxidative haemolysis. This sesquiterpene was thus shown to be effective in protecting biological systems against oxidative stresses.     

Flavonoid Glycosides and Other Hydrophilic Compounds from Flowers of Heterotheca inuloides

Ten flavonoid glycosides were identified in flowers of HETEROTHECA INULOIDES ("Mexican Arnica"). Their structures were established by spectral data (UV, (1)H-NMR, (13)C-NMR, mass) and total acid hydrolysis as kaempferol 3-beta-glucoside, 3-beta-galactoside, 3-beta-rutinoside, 3-beta-robinobioside, quercetin 3-beta-glucoside, 3-beta-galactoside, 3-beta-glucuronide, 3-beta-glucuronide-6'-methylester, 3-alpha- L-arabinoside, and 3-beta-rutinoside. Additionally, caffeic, protocatechuic, and chlorogenic acid as well as umbelliferone were found.     

Anti-inflammatory activity of standardized dichloromethane extract of Salvia connivens on macrophages stimulated by LPS

Context: A previous study demonstrated that the chloroform extract of Salvia connivens Epling (Lamiaceae) has anti-inflammatory activity.

Objective: Identification of the active components in the dicholorometane extract (DESC), and, standardization of the extract based in ursolic acid.

Material and methods: DESC was prepared by percolation with dichlromethane and after washed with hot hexane, its composition was determined by CG-MS and NMR, and standardized by HPLC. The anti-inflammatory activity was tested on acute TPA-induced mouse ear oedema at doses of 2.0?mg/ear. The cell viability of macrophages was evaluated by MTT method, and pro- and anti-inflammatory interleukin levels were measured using an ELISA kit.

Results: Ursolic acid, oleanolic acid, dihydroursolic acid and eupatorin were identified in DESC, which was standardized based on the ursolic acid concentration (126?mg/g). The anti-inflammatory activities of DESC, the acid mixture, and eupatorin (2?mg/ear) were 60.55, 57.20 and 56.40% inhibition, respectively, on TPA-induced ear oedema. The IC₅₀ of DESC on macrophages was 149.4?μg/mL. DESC (25?μg/mL) significantly reduced TNF-α (2.0-fold), IL-1β (2.2-fold) and IL-6 (2.0-fold) in macrophages stimulated with LPS and increased the production of IL-10 (1.9-fold).

Discussion: Inflammation is a basic response to injuries, and macrophages are involved in triggering inflammation. Macrophage cells exhibit a response to LPS, inducing inflammatory mediators, and DESC inhibits the biosynthesis of the pro-inflammatory and promote anti-inflammatory cytokines.

Conclusion: DESC has an anti-inflammatory effect; reduced the levels of IL-1β, Il-6 and TNF-α; and increases IL-10 in macrophages stimulated with LPS. Ursolic acid is a good phytochemical marker.     

In vivo and in vitro hemostatic activity of Chromolaena odorata leaf extract

Context: Chromolaena odorata (L.) R.M.King & H.Rob. (Asteraceae) or Siam weed has long been used to stop bleeding in Thailand and many countries. Only the aqueous leaf extract was investigated in in vivo and there have been conflicting results of in vitro hemostatic mechanisms of this plant. Objective: The most appropriate C. odorata leaf extract that promoted the highest hemostatic activity and the hemostatic mechanisms of these plant extracts will be investigated. Materials and methods: The lyophilized aqueous leaf extract and alcoholic (50, 70, and 95% ethanol) extracts from the fresh and dried leaves were investigated both in vivo and in vitro. The bleeding time in male Wistar rats was measured to investigate the hemostatic effect. The hemostatic mechanisms were tested using in vitro platelet aggregation and blood coagulation tests in sheep plasma. Results: All extracts displayed significantly reducing bleeding time (<2.5?min) in rats but did not induce platelet aggregation or blood clotting in the in vitro study. The in vitro blood clotting times of all extracts were > 0.6?min. Ethanol extract (70%) from the dried leaves proved to be the extract producing the highest hemostatic activity in vivo with the bleeding time of 1.85?min. Discussion and conclusion: The in vivo study with rats confirmed the significant ability of this plant extract to stop bleeding. However, the sufficient amount of calcium and active compounds which are aggregating and clotting agents to enhance blood coagulation and platelet aggregation in in vitro tests should be further studied.     

人胎盘提取液的抗炎和抗血小板聚集作用

AIM: To find the anti-inflammatory and anti-platelet aggregatory activity of human placental extract (HPE, Placentrex). METHODS: The HPE was studied for anti-inflammatory effect in Wistar rats on carrageenin, serotonin (5-HT), and prostaglandin E1 (PGE1) induced edema in acute model and cotton pellet induced granuloma on sub-acute model. Anti-platelet aggregation was studied against protection of adinosine diphosphate (ADP)-induced aggregation of human platelet through in vitro study. RESULTS: HPE showed positive results both in acute and sub-acute models of inflammation. Highly significant (P<0.01) results were obtained against 5-HT induced acute inflammation and cotton pellet induced sub-acute inflammation in comparison with standard (diclofenac sodium) and control (normal saline) drugs. The anti-inflammatory property of HPE in animal model was well supported with clinical study of platelet aggregation. There was highly significant (P<0.01) inhibition of platelet aggregation with HPE at different doses against ADP. CONCLUSION: Our data suggest that human placental extract may be useful in suppressing inflammation and platelet aggregation.     

丹参酮ⅡA体内外抗炎作用研究

目的采用体内外炎症模型研究丹参酮IIA抗炎活性作用及其作用机制。方法建立脂多糖(LPS)诱导巨噬细胞RAW264.7细胞体外炎症模型,检测不同浓度丹参酮IIA对炎症因子水平、诱导型一氧化氮合酶(iNOS)、环氧化酶2(COX-2)蛋白表达及其基因表达的影响。建立二甲苯致小鼠耳廓肿胀和角叉菜胶大鼠足跖肿胀炎症模型,探讨不同浓度丹参酮IIA的体内抗炎作用。结果丹参酮IIA对RAW264.7细胞无明显毒性。与LPS组比较,丹参酮IIA剂量在2.5～40 mg/L呈明显剂量相关性地抑制一氧化氮(NO)、白细胞介素-1?(IL-1?)和白细胞介素-6(IL-6)释放(P0.05、0.01)。与LPS组比较,丹参酮IIA呈现剂量相关性地抑制LPS诱导的RAW264.7细胞iNOS和COX-2蛋白的表达(P0.01)。与LPS组比较,丹参酮IIA呈剂量相关性地下调LPS诱导的RAW264.7细胞中的iNOS、COX-2、IL-1?和IL-6基因表达(P0.05、0.01)。丹参酮IIA在10～60 mg/kg对二甲苯所致小鼠耳廓肿胀有不同程度的抑制作用,对角叉菜胶所致大鼠足跖肿胀有不同程度的抑制作用,并呈剂量相关性(P0.05、0.01),且当丹参酮IIA给药剂量达到40 mg/kg时,其抗炎效果强于阿司匹林。结论丹参酮IIA具有抗炎作用,其作用机制可能与减少巨噬细胞炎症介质生成和释放、炎症基因iNOS、COX-2、IL-1?和IL-6的表达密切相关。     

In vivo angiogenic activity of dichloromethane extracts ofAloe vera gel

The angiogenic activity ofAloe vera (Aloe barbadensis), known as a good healing plant, was investigated. We have extracted and fractionated dichloromethane extract (G1M1D1) and methanol soluble fraction of dichloromethane extract (G1M1D1M1) which contain low-molecular weight substances ofAloe vera gel. G1M1D1 and G1M1D1M1 fractions induced a radially arranged, spoke-wheel-like vasculature in chick embryo chorioallantoic membrane (CAM) assay. The angiogenic activity was dose-dependent and the angiogenic pattern in the CAM assay was very similar to that of phorbol 12-myristate-13-acetate (PMA) used as a positive contol. The modified CAM assay, a simple and accurate quantitating method, was used to quantitate the angiogenic activity of G1M1D1M1 fraction. Application of G1M1D1M1 fraction (100 μg/egg) resulted in much more intense angiogenesis than in contol while slightly less intense angiogenesis than in PMA (100 ng/egg).     

黄芩素体外抑菌与体内抗炎作用研究

目的:研究黄芩素体外抑菌与体内抗炎作用。方法:采用滤纸片研究黄芩素(10 mg/ml)对大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌、白色念珠菌、黑曲霉的抑制作用;采用试管二倍稀释法测定黄芩素对上述5种菌株的最低抑菌浓度(MIC)。二甲苯诱发小鼠急性炎症,测定小鼠耳廓肿胀度与小鼠血清肿瘤坏死因子(TNF)-α、白细胞介素(IL)-1含量。结果:10 mg/ml黄芩素对5种菌株具有一定的抑制作用。5种菌株MIC分别为0.312 5、0.312 5、0.625 0、0.312 5、0.625 0 mg/ml。0.20、0.10 mg/kg黄芩素可明显抑制模型小鼠耳廓肿胀,0.20、0.10 mg/kg黄芩素可明显降低模型小鼠血清TNF-α含量,0.20 mg/kg黄芩素可明显降低模型小鼠血清IL-1含量。结论:黄芩素具有一定的体外抗菌与体内抗炎作用。     

Anti-inflammatory activity of aqueous leaf extract of Chromolaena odorata

The anti-inflammatory activity of the aqueous extract of Chromolaena odorata was investigated in rats using the carrageenan-induced oedema, cotton pellet granuloma and formalin-induced oedema methods. The extract was administered orally at doses of 25, 50, 100 and 200 mg/kg. In the carrageenan method the paw oedema was significantly reduced by all the doses of the extract administered, with the 200 mg/kg dose producing the highest oedema inhibition (80.5%). In the cotton pellet method, granuloma weight was significantly reduced from 14 ± 0.1 to 9.0 ± 0.1 mg, while in the formaldehyde induced arthritis the extract inhibited the oedema during the 10-day period. In conclusion, this study has established the anti-inflammatory activity of C. odorata and, thus, justifies the traditional uses of the plant in the treatment of wounds and inflammation.     

Anti-inflammatory activity of an extract of Petasites hybridus in allergic rhinitis

Previous studies have suggested that histamine and leukotrienes (LTs) play an important pathobiological role in IgE-mediated allergic diseases. In vitro studies suggested that an extract of Petasites hybridus (Ze339) blocks LT synthesis in monocytes and granulocytes. Petasins are considered to be the pharmacologically active fraction within Ze339. Patients suffering from allergic rhinitis received three times a day two tablets of Ze339 standardized to 8 mg petasins within a time period of 1 week. After 5 days of treatment, Ze339 significantly improved primary end points, which were day- and nighttime nasal symptoms. Nasal resistance, which was measured by rhinomanometry, gradually decreased as a consequence of Ze339 treatment reaching normal levels after 5 days (rhinomanometry: from 403.5+/-62.0 to 844.8+/-38.8 ml). Levels of inflammatory mediators in nasal fluids and serum were measured 90 min after drug administration every day in the morning. After 5 days of treatment, a significant reduction of histamine (from 153.7+/-32.1 to 53.0+/-8.4 pg/ml) and LT levels (LTB4: from 313.1+/-46.5 to 180.6+/-32.2 pg/ml; cysteinyl-LT: from 137.0+/-42.2 to 70.1+/-16.5 pg/ml) could be observed. Moreover, quality-of-life scores significantly improved. The drug had no effect on the distribution of lymphocyte subpopulations in the blood as well as on the capacity of blood leukocytes to generate cytokines and lipid mediators. These results suggest that Ze339 is effective in treating allergic rhinitis patients by decreasing levels of nasal inflammatory mediators.     

Anti-inflammatory activity of crude extract and fractions of Nectandra falcifolia leaves

The present study evaluated the effect of the crude extract of the leaves of Nectandra falcifolia (NEES) Castiglioni and its fractions in different experimental models of inflammation (paw edema, pleurisy, and ear edema). Carrageenan-induced edema of the paw and pleurisy were evaluated in Wistar rats (180-220 g), which were treated with different doses of the total extract (250, 500 mg.kg-1). Edema of the ear, induced by croton oil, and determination of myeloperoxidase activity were evaluated in Swiss mice (25-35 g). In this experiment, the crude extract of Nectandra falcifolia (Nf) (1.25, 2.5, 5.0, 7.5 mg) and the hexane, chloroform, ethyl-acetate and hydromethanol fractions (5.0 mg) were applied topically, immediately after application of the oil. The crude extract of Nf (500 mg.kg-1) significantly reduced edema of the paw compared to the control group. Similarly, at doses of 250 and 500 mg.kg-1 it significantly reduced the volume of pleural inflammatory exudate compared to the control animals. However, it did not change the number of migrated cells. At doses of 2.5, 5.0 and 7.5 mg, the crude extract significantly inhibited edema of the ear and the influx of neutrophils. The fractions from Nectandra falcifolia (hexane, chloroform, ethyl acetate and hydromethanol) also inhibited edema of the ear. Taken together, the results demonstrated that the crude extract and its fractions administered to animals orally or topically showed an anti-inflammatory effect.     

Anticancer activity of Kalanchoe tubiflora extract against human lung cancer cells in vitro and in vivo

Uncontrolled cell proliferation is a common feature of human cancer. Some of herbal extract or plant‐derived medicine had been shown as an important source of effective anticancer agents. We previously reported that an n‐BuOH‐soluble fraction of Kalanchoe tubiflora has antiproliferative activity by inducing mitotic catastrophe. In this study, we showed that the H₂O‐soluble fraction of Kalanchoe tubiflora (KT‐W) caused cell cycle arrest, and senescence‐inducing activities in A549 cells. We used 2 dimensional PAGE to analyze the protein expression levels after KT‐W treatment, and identified that the energy metabolism‐related proteins and senescence‐related proteins were disturbed. In vivo experiments showed that the tumor growths in A549‐xenografted nude mice were effectively inhibited by KT‐W. Our findings implied that KT‐W is a putative antitumor agent by inducing cell cycle arrest and senescence. © 2015 Wiley Periodicals, Inc. Environ Toxicol 31: 1663–1673, 2016.     

In vitro and in vivo anti-Helicobacter/Campylobacter activity of the aqueous extract of Enantia chlorantha

The aqueous extract of Enantia chlorantha Oliver (Annonaceae) stem bark, a plant widely used in Cameroon for the traditional treatment of gastritis and stomach problems, was assessed for in vitro and in vivo anti-Helicobacter/Campylobacter properties using the well diffusion assay, agar dilution assay, and killing rate determination. The in vitro activity was dose-dependent, and the same antimicrobial parameters (MAQ?=?0.63?mg; MIC?=?0.39?mg/mL; MBC?=?1.56?mg/mL; ET₁₀₀?=?8?h) were obtained for both H. pylori and C. jejuni/coli. When the plasma active principle concentration equivalence was determined in vitro using plasma from rats exposed to a single dose (3000?mg/kg) of the extract, the peak absorption of E. chlorantha active principle against H. pylori occurred at 2?h. Plasma activity was nil 8?h after extract administration. The in vivo H. pylori eradication potency of the extract was assessed using mice infected with H. pylori. Antral mucus sample cultures from mice treated with E. chlorantha extract (500 and 1000?mg/kg for 3 days) did not yield any growth. The results suggest that in addition to its in vitro activity, E. chlorantha water extract also possesses in vivo antibiotic effects against H. pylori.     

Anti-inflammatory activity of phycocyanin extract in acetic acid-induced colitis in rats.

The anti-inflammatory effect of c-phycocyanin extract was studied in acetic acid-induced colitis in rats. Phycocyanin (150, 200 and 300 mg kg(-1) p.o.) was administered 30 min gbefore induction of colitis with enema of 1 ml of 4% acetic acid per rat. Twenty-four hours later myeloperoxidase (MPO) activity was determined as well as histopathological and ultrastructural studies were carried out in colonic tissue. Phycocyanin substantially reduced MPO activity which was increase din the control colitis group. Also, histopathological and ultrastructural studies were carried out in colonic tissue. Phycocyanin substantially reduced MPO activity which was increased in the control colitis group. Also, histopathological and ultrastructural studies showed inhibition in inflammatory cell infiltration and reduction to some extent in colonic damage in rats treated with phycocyanin. The probable role of antioxidative and the scavenging properties of phycocyanin against reactive oxygen species in the anti-colitic effect is discussed in this paper. To our knowledge this is the first report on the anti-inflammatory effect of phycocyanin in an experimental model of colitis.     

In vivo and in vitro anti-inflammatory activity of Mangifera indica L. extract (VIMANG).

A standard aqueous extract of Mangifera indica L., used in Cuba as an antioxidant under the brand name of VIMANG, was tested in vivo for its anti-inflammatory activity using commonly accepted assays. M. indica extract, administered topically (0.5-2 mg per ear), reduced ear edema induced by arachidonic acid (AA) and phorbol myristate acetate (PMA, ED50 = 1.1 mg per ear) in mice. In the PMA model, M. indica extract also reduced myeloperoxidase (MPO) activity. This extract p.o. administered also inhibited tumor necrosis factor alpha (TNFalpha) serum levels in both models of inflammation (AA, ED50 = 106.1 mg kg(-1) and PMA, ED50 = 58.2 mg kg(-1)). In vitro studies were performed using the macrophage cell line RAW264.7 stimulated with pro-inflammatory stimuli (LPS-IFNgamma or the calcium ionophore A23187) to determine PGE2 or LTB4 release, respectively. The extract inhibited the induction of PGE2 with IC50 = 64.1 microg ml(-1) and LTB4 IC50 = 22.9 microg ml(-1). M. indica extract also inhibited human synovial secretory phospholipase (PL)A2 with IC 50 = 0.7 microg ml(-1). These results represent an important contribution to the elucidation of the mechanism involved in the anti-inflammatory and anti-nociceptive effects reported by the standard M. indica extract VIMANG.     

Anti-inflammatory activity of creatine supplementation in endothelial cells in vitro

1 Creatine (CR) supplementation augments muscle strength in skeletal muscle cells by increasing intracellular energy pools. However, the effect of CR supplementation on endothelial cells remains to be clarified. 2 In this study, we investigated whether CR supplementation had any anti-inflammatory activity against human pulmonary endothelial cells in culture. 3 We confirmed that supplementation with 0.5 mM CR significantly increased both intracellular CR and phosphocreatine (PC) through a CR transporter while keeping intracellular ATP levels constant independent of CR supplementation and a CR transporter antagonist. 4 In the assay system of endothelial permeability, supplementation with 5 mM CR significantly suppressed the endothelial permeability induced by serotonin and H(2)O(2). 5 In cell adhesion experiments, supplementation with 5 mM CR significantly suppressed neutrophil adhesion to endothelial cells. 6 In the measurement of adhesion molecules, CR supplementation with more than 0.5 mM CR significantly inhibited the expressions of ICAM-1 and E-selectin on endothelial cells, and the inhibition was significantly suppressed by an adenosine A(2A) receptor antagonist. 7 The present study suggests that CR supplementation has anti-inflammatory activities against endothelial cells.     

Antioxidant potential of Biophytum sensitivum extract in vitro and in vivo

An extract of the medicinal plant, Biophytum sensitivum (L.) DC (Oxalidaceae), was evaluated for its antioxidant potential in vitro and in vivo. Biophytum sensitivum was found to scavenge superoxide radicals generated by the photoreduction of riboflavin and hydroxyl radicals generated by the Fenton reaction and inhibited in vitro lipid peroxidation at concentrations of 50, 95, and 20 microg mL(-1) (50% inhibition [IC50]), respectively. The drug also scavenged nitric oxide (IC50 = 100 microg mL(-1)). The extract also induced the dose-dependant scavenging of nitric oxide in culture. Intraperitoneal administration of Biophytum extract inhibited superoxide generation in macrophages in vivo. The administration of B. sensitivum to mice significantly increased the catalase activity. The extract produced a significant increase in glutathione levels in blood and liver. The levels of glutathione-S transferase and glutathione reductase increased and those of glutathione peroxidase decreased after administering the Biophytum extract. The results of this study indicate that B. sensitivum has significant antioxidant activity both in vitro and in vivo.     

Anti-inflammatory and antiallergic activity in vivo of lipophilic Isatis tinctoria extracts and tryptanthrin

The effects of a supercritical CO2 (SFE) extract, a dichloromethane (DCM) extract from Isatis tinctoria leaf and the alkaloidal constituent tryptanthrin were studied in acute and subchronic experimental models of inflammation. The SFE and DCM extracts showed anti-inflammatory activity in the carrageenan-induced acute mouse paw oedema (ED50 values of 78 mg/kg and 165 mg/kg P. O., respectively) and in the acute tetradecanoylphorbol acetate (TPA)-induced mouse ear oedema in oral (62% and 32% oedema reduction at 100 and 125 mg/kg, respectively) and topical application (37% and 33% reduction of oedema at 0.5 mg/ear). In contrast, tryptanthrin showed no significant anti-inflammatory effect. The DCM extract inhibited oedema formation and neutrophil infiltration in subchronic inflammation in mice induced by repeated application of TPA. The extract showed activity after oral and topical administration by reducing the various parameters of the inflammatory response. The DCM extract (1 mg/ear) inhibited the delayed-type hypersensitivity (DTH) reaction induced by application of dinitrofluorobenzene (DNFB) after topical application. The response during the induction phase (24 h) was decreased by 48%, and the inflammatory phase (48 to 96 h) was reduced by 53 to 56%. The extract had no effect in this model when administered orally. The DCM extract (200 mg/kg P. O.) inhibited the acetic acid-induced writhing by 49%.