The antiinflammatory and liver protective effect of Tithonia diversifolia (Hemsl.) gray and Dicliptera chinensis Juss. Extracts in rats

The antiinflammatory and liver protective effect of water extracts of Tithonia diversifolia (Hemsl.) Gray (aerial part), T. diversifolia (stem) and Dicliptera chinensis Juss. (aerial part) against paw oedema induced by carrageenan and acute hepatic damage induced by CCI₄ were determined in rats. The results indicated that treatment with a water extract of the aerial part of T. diversifolia decreased the paw oedema induced by carrageenan (p < 0.001) and the GOT, GPT level elevation caused by CCI₄ were reduced (p < 0.01). The pathological changes of hepatic lesions caused by CCI₄ were improved by treatment with the drug extracts mentioned above.     

Studies on the antiinflammatory principle of Mentzelia chilensis

A crude aqueous extract of Mentzelia chilensis GAY (Loasaceae), the ethyl acetate extraction thereof as well as the molecular weight fraction <1000 Dalton obtained by ultrafiltration showed antiinflammatory activity on carrageenin induced rat paw oedema. Bioassay guided isolation led to the iridoid glycoside mentzeloside (syn. deutzioside) as an active principle. Mentzeloside showed a marked and significant dose dependent inhibitory activity on carrageenin induced rat paw oedema with an ED₅₀ of 40.4 μg/kg. © 1998 John Wiley & Sons, Ltd.     

Analgesic and antiinflammatory activities of Ageratum conyzoides in rats

The water soluble fraction (WSF) obtained from a hydroalcohol extract of A. conyzoides, a medicinal plant used in Brazilian folk medicine, was evaluated for possible analgesic and antiinflammatory activities. It was demonstrated that WSF (20–50 mg/kg; i.p.) treatment reduced the articular incapacitation induced by carrageenin (300 μg) in rats. In this model, naloxone (2 mg/kg) blocked the analgesic action of morphine (2 mg/kg) but did not change the WSF antinociceptive effect. It suggests that endogenous opioids are not involved in the WSF antinociceptive effect. The neutrophil migration induced by carrageenin (300 μg) injection into rat peritoneal cavities and into 6-day-old subcutaneous air-pouches was significantly inhibited (p <0.05) by WSF pre-treatment (30 and 50 mg/kg; s.c.). At the same dose WSF also inhibited (p <0.05) the carrageenin (400 μg/paw)-induced oedema, but failed to modify the oedema induced by dextran (100 μg/paw). Furthermore, the increase in the cutaneous vascular permeability induced by the potent leukocyte chemotactic agent LTB₄ (39 ng co-injected with 500 ng iloprost, i.d.) was significantly blocked by WSF (30 mg/kg; i.p.). However, in the same dose WSF caused a 2-fold increase in the vascular permeability induced by histamine (10 μg), a direct vasoactive mediator. These results suggest that WSF can inhibit the inflammatory reactions induced by neutrophil mobilizing stimuli. © 1997 John Wiley & Sons, Ltd.     

Antioxidant and antiinflammatory effect of Epilobium parviflorum Schreb.

Epilobium parviflorum Schreb. (Onagraceae) is used for the treatment of benign prostatic hyperplasia (BPH), but its biological action is not entirely identified. This paper aims to report data on E. parviflorum with respect to its antioxidant and antiinflammatory effects. The aqueous acetone extract of E. parviflorum showed higher antioxidant effect in the DPPH assay than well known antioxidants and inhibited the lipid peroxidation determined by the TBA assay (IC₅₀ = 2.37 ± 0.12 mg/mL). In concentrations of 0.2–15.0 µg/mL the extract possessed a protective effect, comparable to catalase (250 IU/mL), against oxidative damage, generated in fibroblast cells. In the COX inhibition assay E. parviflorum decreased the PGE₂ release, so showing inhibition of the COX‐enzyme (IC₅₀ = 1.4 ± 0.1 µg/mL). Copyright © 2008 John Wiley & Sons, Ltd.     

Antiinflammatory activity and acute toxicity (LD50) of the juice of Kalanchoe brasiliensis (comb.) leaves picked before and during blooming

Kalanchoe brasiliensis Comb. (Cassulaceae) extracts from leaves picked before and during plant blooming (extracts 1 and 2, respectively) were tested for their antiinflammatory effect on carrageenin‐induced rat paw oedema and for acute toxicity (LD₅₀). Oral doses of 0.25, 0.5 and 1.0 g/kg of extract 1 significantly inhibited the paw oedema during the first 4 h after injection of 2% carrageenin, while oral doses of 0.5, 1.0 and 2.0 g/kg of extract 2 had no inhibitory activity on the paw oedema induced by carrageenin. The results indicate an antiinflammatory effect of extract 1 and a proinflammatory effect of extract 2. K. brasiliensis extracts 1 and 2 presented no acute toxicity on mice at the doses of 0.25 to 5 g/kg administered intraperitoneally. Copyright © 1999 John Wiley & Sons, Ltd.     

Antiinflammatory Constituents from Eclipta prostrata using RAW264.7 Macrophage Cells

The whole plant extract of Eclipta prostrata and its isolated compounds were tested for their antiinflammatory effects against lipopolysaccharide (LPS)‐induced nitric oxide (NO), prostaglandin E₂ (PGE₂) and tumor necrosis factor‐alpha (TNF‐α) release in RAW264.7 cells, as well as for the antiinflammatory mechanism of the active compound on mRNA expression. Among the isolated compounds, orobol (5) exhibited the highest activity against NO release with an IC₅₀ value of 4.6 μm , followed by compounds 1, 2 and 4 with IC₅₀ values of 12.7, 14.9 and 19.1 μm , respectively. The IC₅₀ value of compound 5 against PGE₂ release was found to be 49.6 μm , whereas it was inactive towards TNF‐α (IC₅₀ > 100 μm ). The mechanism of orobol (5) was found to down‐regulate iNOS and COX‐2 mRNA expression in a concentration‐dependent manner. The present study may support the traditional use of Eclipta prostrata for the treatment of inflammatory‐related diseases. Copyright © 2011 John Wiley & Sons, Ltd.     

The phytochemical and anti‐inflammatory studies of Dillenia suffruticosa leaves

The Dillenia suffruticosa leaves (Dilleniaceae), a folk medicine recommended in Southeast Asia for treating inflammation, were phytochemically studied for the first time and assessed for suppression of λ‐carrageenan‐induced paw oedema in rats. The crude methanolic extract orally administered at 5,000 mg/kg, displayed no toxicity and at 250 to 1,000 mg/kg significantly suppressed the paw oedema. Two‐isolated triterpenoids, betulinic acid (1) and koetjapic acid (2) orally administered at 50 mg/kg, significantly reduced the paw oedema, (p < 0.001) and (p < 0.005) at the fourth h onwards to 47.36% ± 2.23 and 53.43% ± 7.09, respectively, from 95.90% ± 6.88 oedema induced by λ‐carrageenan alone. 1 and the isolated flavonoids of vitexin (3), tiliroside (4), and kaempferol (5), displayed moderately more of cyclooxygenase (COX)‐2 than COX‐1 enzyme inhibition, whereas 2 was slightly more inhibition of COX‐1. The in silico molecular docking studies provided support to the in vitro COX studies that the isolated compounds formed H‐bonding with the amino acid residues at the COX‐2 catalytic sites. The triterpenoids were bound to the peroxidase, possibly inhibiting the peroxidase reaction, whereas the flavonoids interacted more at the cyclooxygenase, resembling celecoxib, therefore providing evidences that these compounds were responsible for the anti‐inflammatory properties of D. suffruticosa.     

Antiinflammatory Properties of the Stem‐bark of Anopyxis klaineana and its Major Constituent,Methyl Angolensate

Anopyxis klaineana (Pierre) Engl. (Rhizophoraceae) is one of the reputed West African folkloric medicines that has never been investigated for its pharmacological effects or phytochemical constituents. In the present study, the antiinflammatory properties of the stem‐bark extracts were evaluated using the carrageenan‐induced paw oedema model in chicks. The petroleum ether, ethyl acetate and methanol extracts all showed a time and dose‐dependent antiinflammatory effect over the 5‐h observation period. Phytochemical analysis of the most active extract (methanol extract) yielded the principal constituent that was identified as methyl angolensate through extensive spectroscopic and X‐ray analysis studies. Although slightly less potent (ED₅₀, 4.05 ± 0.0034 mg/kg, orally) than the positive control, diclofenac (ED₅₀, 2.49 ± 0.023, intraperitoneally n = 5), this first ever compound isolated from A. klaineana showed promising antiinflammatory activity that may account to some of the reported medicinal uses of the plant. Copyright © 2014 John Wiley & Sons, Ltd.     

Herbal medicine Catuama induces endothelium-dependent and -independent vasorelaxant action on isolated vessels from rats,guinea-pigs and rabbits

The present study was designed to examine the vasorelaxant action of the herbal medicine Catuama and the hydroalcoholic extracts (HE) of each plant present in this product and to compare their effects with that caused by acetylcholine (ACh) in intact (⁺E) or in endothelium-rubbed (⁻E) rings of rat thoracic aorta (RA), guinea-pig pulmonary artery (GPPA), guinea-pig mesenteric artery (GPMA), rabbit pulmonary artery (RPA), rabbit mesenteric artery (RMA) precontracted with noradrenaline (NA) or phenylephrine (PE). The extract of Catuama (1-3000 μg/mL) produced graded relaxation of RA, ⁺E or ⁻E, with mean EC₅₀ of 430 μg/mL and ≊ 3000 μg/mL and E_max of 81 % ± 15 % and 47% ± 4 %, respectively. The nitric oxide (NO) synthase inhibitor, N^ω-nitro-L -arginine (L -NOARG, 100 μM ), inhibited in vasorelaxant action (p < 0.05) in RA (⁺E), while indomethacin (3 μM ), propranolol (1 μM ), glibenclamide (1 μM ), methylene blue (10 μM ) and apamin (0.1 μM ) had no significant effect. ACh (1-1000 μM ) caused graded relaxation in RA with ⁺E, these effects being markedly antagonized by L -NOARG (100 μM ), methylene blue (10 μM ) and partially by apamin (0.1 μM ), but not by indomethacin (3 μM ), glibenclamide (1 μM ) or propranolol (1 μM ). The Catuama extract (1-3000 μg/mL) produces partial relaxations in rings of RMA (mean EC₅₀ of 1073 μg7/ml and E_max of 56 % ± 13 %), an effect which was antagonized by L -NOARG (100 μM ). In RPA (⁺E) the extract produces partial relaxation followed by contraction (E_max 28 % ± 6 %), an effect which was abolished by L -NOARG (100 μM ) or methylene blue (10 μM ). The extract caused graded relaxation in rings of GPPA and GPMA with mean EC₅₀ values of 60 μg/mL and 1148 μg/mL and E_max 96% ± 2% and 88% ± 12%, respectively. L -NOARG (100 μM ) blocked the Catuama extract vasorelaxation in GPPA and only partially in GPMA, but markedly antagonized the vasorelaxations caused by ACh in both GPPA andRMA. The HE Paullinea cupana, Zinziber officinalis and Trichilia catigua (1-3000 μg/mL) caused a graded vasorelaxant effect ⁺E of RA with a mean EC₅₀ of 22, 55 and 1793 μg/mL and E_max 100%, 86% ± 7% 70% ± 2%, respectively. In addition the HE of P. cupana also caused graded relaxation in ⁻E of RA with EC₅₀ and E_max of 233 μg/mL and 100%, respectively, while T. catigua and Z. officinalis produced partial relaxation in RA ⁺E. In contrast the HE of Ptychopetalum olacoides caused little contraction (46% ± 14%). These results demonstrate that the medicinal herb Catuama produces significant vasorelaxation responses in vessels from different animal species, and show that its effects are in great part dependent on the release of NO or NO-derived substances. Our results also demonstrate that the vasorelaxant action of the product Catuama seems to be due to the action of the active principles present mainly in P. cupana; T. catigua and, to a lesser extent, in Z. officinalis. Such results may contribute to the explanation of its beneficial effect of Catuama herbal medicine in the management of cardiovascular disturbances. © 1997 John Wiley & Sons, Ltd.     

Reduction of agonist-induced contractions of guinea-pig isolated ileum by flavonoids

The effect of 13 flavonoids on the contraction of guinea-pig isolated ileum induced by prostaglandin E₂ (PGE₂) and leukotriene D₄ (LTD₄) have been investigated. Apigenin, quercetin and kaempferol at a concentration of 10 μM significantly (p<0.001) reduced the contraction to either agonist. Crysin and flavone antagonized only PGE₂ (p<0.01). The other flavonoids were inactive. The blocking effect of apigenin, quercetin and kaempferol against PGE₂ was also concentration- and time-dependent, and was augmented by the calcium channel blocker verapamil or by lowering the extracellular calcium to 25%, consistent with a calcium-mediated mechanism of protection which these flavonoids, at the same concentration, also showed against barium chloride (BaCl₂)- or acetylcholine (ACh)-induced contraction (p<0.05–0.001).     

Antiinflammatory Activity of Fractions of Latex of Calotropis procera in Carrageenan Induced Rat Paw Oedema

The crude dry latex of Calotropis procera possesses a potent antiinflammatory activity. The antiinflammatory activity of petroleum ether, acetone, methanol and aqueous extracts of dry latex of Calotropis procera was tested in the carrageenan induced rat paw oedema model. All the fractions exhibited antiinflammatory activity but inhibition of oedema was found to be greatest with the acetone and aqueous extracts. © 1997 by John Wiley & Sons, Ltd.     

Analgesic and antiinflammatory activity of kaur-16-en-19-oic acid from Annona reticulata L. bark

Kaur‐16‐en‐19‐oic acid was isolated from the bark of Annona reticulata and studied for its analgesic and antiinflammatory activity. Analgesic activity was assessed using the hot plate test and acetic acid‐induced writhing, and the antiinflammatory activity using the carrageenan induced rat paw oedema method. Kaur‐16‐en‐19‐oic acid, at doses of 10 and 20 mg/kg, exhibited significant (p < 0.05) analgesic and antiinflammatory activity. These activities were comparable to the standard drugs used, and furthermore the analgesic effect of kaur‐16‐en‐19‐oic acid was blocked by naloxone (2 mg/kg) in both analgesic models. Copyright © 2011 John Wiley & Sons, Ltd.     

Studies on antiinflammatory effect of Cassia tora leaf extract (fam. Leguminosae)

The antiinflammatory effect of the methanol extract of the leaves of Cassia tora was investigated against carrageenin, histamine, serotonin and dextran-induced rat hind paw oedema. It exhibited significant antiinflammatory activity against all these agents. The extract (400 mg/kg) showed maximum inhibition of oedema of 40.33%, 31.37%, 53.57% and 29.15% at the end of 3 h with carrageenin, dextran, histamine and serotonin-induced rat paw oedema, respectively. Using a chronic test, the granuloma pouch in rats, the extract exhibited a 48.13% reduction in granuloma weight. © 1998 John Wiley & Sons, Ltd.     

Antiinflammatory activity and effects on isolated smooth muscle of extracts from different Teucrium species

The present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan-induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti-inflammatory effect through the 24 h experimental period and reduced the E_max induced by histamine and serotonin in vitro on guinea-pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and noradrenaline on rat vas deferens. The methanol extracts of T. pumillum (50 mg/kg, i.p.) and T. buxifolium (26 mg/kg, i.p.) exhibited significant antiinflammatory effects only in the acute phase of the oedema (2 h) without affecting the chronic phase (24 h). In guinea-pig ileum, rat uterus and rat vas deferens, the methanol extract of T. pumillum reduced the maximal effect induced by histamine, serotonin and noradrenaline, respectively, whereas the methanol extract of T. buxifolium lacked any effect on the contractile activity induced by various agonists in vitro. When tested for antiinflammatory activity the methanol (200 mg/kg, i.p.) and dichloromethanol (200 mg/kg, i.p.) extracts of T. cartaginenses did not modify the oedematous response induced by carrageenan administration.     

Evaluation of pharmacological activity of a crude hydroalcoholic extract from Jatropha elliptica

The pharmacological effect of the hydroalcoholic extract of Jatropha elliptica was analysed in in vivo and in vitro models. When given orally in mice, the extract showed a low acute toxicity (LD₅₀ 5 g/kg). In a dose of 0.5 or 1 g/kg p.o. the extract did not interfere with diuresis in the rat, but was found to be effective in blocking rat paw oedema induced by carrageenan and partially, serotonin-induced oedema. In the same dose, the extract failed to inhibit rat paw oedema induced by dextran and the increase of rat cutaneous vascular permeability caused by Bothrops Jararaca venom, dextran, histamine, PAF-acether and serotonin. Pre-incubation of the isolated rat uterus and guinea-pig ileum with the extract (0.2–0.8 mg/mL), produced a concentration-related and non-competitive inhibition of contractions induced by acetylcholine and bradykinin. However, the extract was about 2-fold more potent in inhibiting the contraction of both agonists in guinea-pig ileum than in rat uterine muscle. In rat aorta, the extract (50–100 μg/mL) caused a concentration-dependent inhibition of noradrenaline-evoked contractions, being about 5-fold more potent when compared to the IC₅₀ values obtained in rat uterus.     

Biological activities of xanthatin from Xanthium strumarium leaves

The objective of the present work was to evaluate the biological activities of the major bioactive compound, xanthatin, and other compounds from Xanthium strumarium (Asteraceae) leaves. Inhibition of bloodstream forms of Trypanosoma brucei brucei and leukaemia HL‐60 cell proliferation was assessed using resazurin as a vital stain. Xanthatin was found to be the major and most active compound against T. b. brucei with an IC₅₀ value of 2.63 µg/mL and a selectivity index of 20. The possible mode of action of xanthatin was further evaluated. Xanthatin showed antiinflammatory activity by inhibiting both PGE₂ synthesis (24% inhibition) and 5‐lipoxygenase activity (92% inhibition) at concentrations of 100 µg/mL and 97 µg/mL, respectively. Xanthatin exhibited weak irreversible inhibition of parasite specific trypanothione reductase. Unlike xanthatin, diminazene aceturate and ethidium bromide showed strong DNA intercalation with IC₅₀ values of 26.04 µg/mL and 44.70 µg/mL, respectively. Substantial induction of caspase 3/7 activity in MIA PaCa‐2 cells was observed after 6 h of treatment with 100 µg/mL of xanthatin. All these data taken together suggest that xanthatin exerts its biological activity by inducing apoptosis and inhibiting both PGE₂ synthesis and 5‐lipoxygenase activity thereby avoiding unwanted inflammation commonly observed in diseases such as trypanosomiasis. Copyright © 2011 John Wiley & Sons, Ltd.     

In vivo Study of the Absorption of Seaweed Minerals by Perfused Rat Intestine

The intestinal absorption of seaweed minerals (Ca, Zn, Fe) was compared with their inorganic salts, in vivo , using a perfused intestinal loop in the rat. A similar uptake of Ca from both sources was observed (19.1±21.0 vs 9.9±14.7 μmol/cm/min, NS), (mean±1 SD), as for Zn (38.8±26.5 vs 47.4±35.0 μmol/cm/min, NS) seaweed Fe absorption was lower than gluconate Fe (26.4±27.7 vs 76.8±7.6 nmol/cm/min, p <0.001). The overall intestinal uptake of these minerals could be explained by their biological form.     

Blood Glucose‐lowering Effect of T. procumbens L.: A Pilot Clinical Study in Individuals with Type 2 Diabetes

Traditional knowledge, in vitro studies, and studies using animal models suggest that Tridax procumbens L. exhibits blood glucose‐lowering properties and antiinflammatory effects. In this study, we evaluated the blood glucose‐lowering effect of T. procumbens supplementation in individuals with type 2 diabetes. An extract (asava) of T. procumbens L. was prepared following Ayurveda guidelines. Chemical and microbial analyses indicated presence of phenolics, flavonoids, and carotenoids, and absence of microbial contamination, aflatoxins, heavy metals, and pesticide residues. A chemical fingerprint of T. procumbens L. asava, developed using Ultra high pressure liquid chromatography/electron spray ionization‐mass spectrometry (UPLC/ESI‐MS) in negative mode, suggest the presence of several compounds including polyphenols. T. procumbens asava demonstrated strong total antioxidant capacity, Fe³⁺ reducing potential, Fe²⁺ chelation, H₂O₂ scavenging activity, and inhibition of lipid peroxidation. We recruited 20 type 2 diabetic individuals from Kolhapur, India. Participants received 15 mL of T. procumbens asava, twice daily, for 4 weeks, while continuing their prescribed antidiabetic medications. Fasting blood glucose decreased by 11% in men (p < 0.01) and 20% in women (p < 0.05), and post‐prandial blood glucose concentrations were lowered by 26% in men (p < 0.001) and 29% in women (p < 0.001) following 4 weeks of asava supplementation. No adverse events or side effects were reported. This is the first clinical study demonstrating a significant blood glucose‐lowering effect of T. procumbens asava in type 2 diabetes. Copyright © 2015 John Wiley & Sons, Ltd.