Anti-inflammatory and antinociceptive activities of Homalium letestui

Abstract

Context. Homalium letestui Pellegr (Flacourtiaceae) is used in various decoctions traditionally by the Ibibios of the Niger Delta of Nigeria to treat stomach ulcer, malaria and other inflammatory diseases, as well as an aphrodisiac.

Objective: To investigate the anti-inflammatory and antinociceptive activities of the stem extract of the plant.

Materials and methods: The ethanol stem extract (500, 750, 1000?mg/kg, i.p.) of H. letestui was investigated for anti-inflammatory activity using carrageenan, egg albumin-induced and xylene-induced ear edema models and analgesic activity using acetic acid-induced writhing, formalin-induced paw licking and thermal-induced pain models. The ethanol extract was administered to the animals orally, 30?min to 1?h depending on the model, before induction of inflammation/pain. The LD₅₀ was also determined. GC–MS analysis of dichloromethane fraction was carried out.

Results: The extract caused a significant (p?<?0.05–0.001) reduction of inflammation induced by carrageenan (8.3–70.0%), egg albumin (10.0–71.42%) and xylene (39.39–84.84%). The extract also reduced significantly (p?<?0.05–0.001) pain induced by acetic acid (44.22–73.65%), formalin (55.89–79.21%) and hot plate (93.0–214.5%). The LD₅₀ was determined to be 4.38?±?35.72?g/kg.

Discussion and conclusion: The results of this study suggest that the ethanol stem extract of H. letestui possesses anti-inflammatory and analgesic properties which may in part be mediated through the chemical constituents of the plant as revealed by the GC–MS.     

Assessment of the antidiarrhoeal properties of the aqueous extract and its soluble fractions of Chebulae Fructus (Terminalia chebula fruits)

Context Chebulae Fructus is used as an herbal remedy for diarrhoea in traditional Chinese medicine. However, there is no scientific evidence to support its antidiarrhoeal activity.

Objective This study evaluates the antidiarrhoeal properties of Chebulae Fructus aqueous extract (CFAE) and determines the active fraction.

Materials and methods The antidiarrhoeal effect of CFAE (200–800?mg/kg) was investigated by determining the wet dropping, intestinal transit in BALB/c mice and enteropooling in Wister rats. The protective effects of the CFAE on the intestinal and liver were tested by histopathological analyses. The antidiarrhoeal fraction was determined by castor oil-induced diarrhoea and its main constituents were identified by HPLC-ESI-MS.

Results The extract at doses of 200, 400 and 800?mg/kg reduced the diarrhoea by 9.1, 40.0 and 58.2% and inhibited intestinal transit by 18.3, 24.1 and 35.7%, respectively. Additionally, the CFAE (200, 400 and 800?mg/kg) decreased the volume of enteropooling by 47.1, 58.8 and 64.7%, respectively. Mice treated with castor oil presented morphological alterations in the small intestine and the liver. However, the lesions of mice treated with CFAE were alleviated. Moreover, the ethyl acetate fraction was the active fraction of CFAE, the fraction (41.7, 83.4 and 166.8?mg/kg) reduced the diarrhoea by 9.1, 38.2 and 54.5%, respectively. The major components of the ethyl acetate fraction were tannins, including gallic acid, 3, 4, 6-tri-O-galloyl-β-d-Glc, corilagin and ellagic acid according to the HPLC-ESI-MS analysis.

Conclusion The CFAE possessed antidiarrhoeal property and the ethyl acetate fraction was its main active fraction.     

Antinociceptive activity and chemical composition of Wei–Chang–An–Wan extracts

Abstract

Context: Currently, famous traditional Chinese medicine formulas have undergone re-evaluation and development in China. Wei–Chang–An–Wan (WCAW) as one of them has been used for treating various gastrointestinal diseases for several decades. The secondary development of WCAW is in progress so as to interpret the effective material basis or find new pharmacological activity.

Objective: To evaluate the antinociceptive effect of methanol extract of WCAW (ME) as well as four fractions (P.E., EtOAc, n-BuOH, H₂O) and obtain information on the correlation between the contents of the fractions and antinociceptive effect.

Materials and methods: ME was divided into four parts extracted by petroleum ether, ethyl acetate and n-butanol. Antinociceptive activity was evaluated by three models of acetic acid–induced writhing, formalin and hot-plate test in mice after repetitive administration of ME at 200, 400 or 800?mg/kg, P.E. 132?mg/kg, EtOAc 106?mg/kg, n-BuOH 176?mg/kg and H₂O 176?mg/kg for six days. The chemical compounds were analyzed by HPLC-ESI-MS.

Results: ME at 800?mg/kg inhibited acid-induced writhing by 84.69%, and reduced the licking time of second phase in formalin test by 53.23%. The inhibition rates in acid-induced writhing of P.E., EtOAc, n-BuOH and H₂O were 27.79, 33.85, 38.97 and 37.69%, respectively, and in formalin test about 50%. They had no effect on the hot-plate test. HPLC-ESI-MS analysis showed that 68 chemical compounds were detected and 41 compounds were identified from ME.

Discussion and conclusion: The results obtained herein indicate that WCAW possesses the antinociceptive activity that provides a new aspect in clinical application.     

Antinociceptive and anti-inflammatory effects of the ethanol extract of Alpinia conchigera rhizomes in various animal models

Alpinia conchigera Griff. (Zingiberaceae), locally known to the Malays as “lengkuas ranting”, is native to Peninsular Malaysia. The Malays traditionally used it to treat infection and rashes, and as a health drink. This study evaluated the analgesic and anti-inflammatory activities of the ethanol extract of A. conchigera rhizomes in mice and rats, respectively. The analgesic activity was elucidated using the acetic acid-induced writhing test, hot plate test, and formalin test, while the anti-inflammatory activity was determined using carrageenan-induced paw edema. The extract (30, 100, and 300?mg/kg) given intraperitoneally (i.p.) exhibited antinociceptive and anti-inflammatory activities in all tests used. The range of percentage of analgesia obtained for all doses of extract in the writhing test was 50–92%, and in the early and late phases of the formalin test was 25–62% and 63–98%, respectively. In addition, naloxone (5?mg/kg) given subcutaneously (s.c.) was found to reverse the extract (300?mg/kg)-induced antinociceptive activity in the writhing, hot plate, and formalin tests. Based on the results obtained, it can be concluded that the ethanol extract of A. conchigera rhizomes possessed a peripheral and central antinociceptive activity that was mediated, in part, via the opioid receptor, as well as anti-inflammatory activity.     

A mechanistic evaluation of the traditional uses of Nepeta ruderalis in gastrointestinal and airway disorders

Context: Nepeta ruderalis Buch.-Ham. (Lamiaceae), locally known as Badranj Boya, is an aromatic herb used traditionally as an antispasmodic, antidiarrhoeal, and anti-asthamatic remedy.

Objective: Aqueous methanolic extract of N. ruderalis was studied to investigate its traditional uses.

Materials and methods: Study was conducted from September 2015 to February 2016. In vitro spasmolytic and broncho-relaxant activity of crude extract of N. ruderalis (whole plant) was evaluated at 0.01–10?mg/mL final bath concentration in isolated rabbit jejunum and tracheal tissues, using PowerLab data acquisition system (Transonic Systems Inc., Ithaca, NY). In vivo antidiarrhoeal activity was evaluated in castor oil-induced diarrhoeal mice at the dose of 300 and 500?mg of crude extract orally.

Results: Crude extract of N. ruderalis completely relaxed spontaneously contracting, high K⁺ (80?mM) and carbachol (1?μM) induced contracted jejunum with an EC₅₀ value of 5.85 (5.45–6.27), 4.0 (3.80–4.23) and 2.86 (2.48–3.29), similar to verapamil. Nr.Cr relaxed high K⁺ and carbachol induced contractions, at 5 and 10?mg/mL with an EC₅₀ value of 2.37 (2.11–2.67) and 3.26 (2.9–3.67), respectively, and also displaced calcium concentration–response curves toward right at 0.1 and 0.3?mg/mL. Nr.Cr exhibited antidiarrhoeal protection at a dose of 300 and 500?mg/kg, similar to verapamil, whereas no acute toxicity signs were seen up to 5?g/kg in healthy mice.

Discussion and conclusion: Results suggest the presence of spasmolytic and broncho-relaxant effects in the crude extract of N. ruderalis, possibly mediated through calcium channel-blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal and airway disorders.     

Anticonvulsant activity of ethanol extracts of Vetiveria zizanioides roots in experimental mice

?Abstract

Context: Vetiveria zizanioides Linn. (Gramineae), an aromatic plant commonly known as vetiver, is traditionally used for various ailments. Ethanol and aqueous extract of this plant found extensive use in Indian folklore medicine and used in treatment of a wide range of disorders including seizure. However, the anticonvulsant activity of this plant has not been studied.

Objective: To evaluate anticonvulsant activity of ethanol extract of V. zizanioides (EEVZ) in experimental mice.

Materials and methods: Anticonvulsant activity of EEVZ was determined by maximal electroshock stimulation (MES) and pentylenetetrazole (PTZ) in mice for 8?d experimental protocol. The extract at a dose of 100, 200 and 400?mg/kg body weight was administered once by oral route.

Results: LD₅₀ value of EEVZ in mice was found at a dose of 600?mg/kg body weight. EEVZ at a dose of 400?mg/kg significantly (p?<?0.001) reduced flexion (l5.98 to 3.73?s), extension (13.73 to 0.96?s), clonus (14.07 to 4.93?s), stupor (6.29 to 1.22?s) in the MES model. Further, it increases onset of clonic (88.25 to 708.32?s/30?min) and tonic (139.52 to 1126.39?s/30?min) in the PTZ model. In the PTZ model, 33% normal control and 83% EEVZ (100?mg/kg) animals were alive, while 100% protection was achieved in standard drug phenobarbital (20?mg/kg), EEVZ (200?mg/kg) and EEVZ (400?mg/kg) animals.

Discussion and conclusion: Findings demonstrate that V. zizanioides shows significant anticonvulsant activity in mice.     

Hepatoprotective effect of Stachys pilifera ethanol extract in carbon tetrachloride-induce hepatotoxicity in rats

Context: Stachys pilifera Benth (Lamiaceae) has long been used to treat infectious diseases, respiratory and rheumatoid disorders in Iranian folk medicine. Antitumor and antioxidant activity of the plant have been reported.

Objective: The study was designed to assess the hepatoprotective activity of ethanol extract of Stachys pilifera in carbon tetrachloride (CCl₄)-induced hepatotoxicity in rats.

Materials and methods: The rats were randomly divided into six equal groups (n?=?7). Group I was treated with normal saline; Group II received CCl₄ (1?mL/kg. i.p., twice a week) for 60 consecutive days; Groups III, IV and V were given CCl₄ plus Stachys pilifera (100, 200 and 400?mg/kg/d,p.o.); Group VI received the extract (400?mg/kg/d, p.o.). Histopathological analysis and measurement of serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), malondialdehyde (MDA), total protein (TP) and albumin (ALB) were performed.

Results: CCl₄ caused a significant increase in the serum levels of AST, ALT, ALP and MDA as well as decreased ALB, and TP serum levels (p?4-elevated levels of ALT, AST, ALP and MDA (p?4 group (p4.

Discussion: The results revealed that the Stachys pilifera extract could provide considerable protection against CCl₄ hepatotoxicity in rats that may be related to its antioxidant properties.     

Antinociceptive and anti-inflammatory effects of the aerial parts of Artemisia dracunculus in mice

Context: Tarragon (Artemisia dracunculus L., Asteraceae) is an ancient herb, which is widely used as a medicine, flavoring, or fragrance.

Objective: To determine the antinociceptive and anti-inflammatory effects of aerial parts of tarragon, we investigated the effects of ethanolic extract of the plant in adult male Balb/c mice.

Materials and methods: Antinociceptive activity was determined using formalin, hot-plate, and writhing tests. The effect of the ethanolic extract on acute inflammation was evaluated by xylene-induced ear edema in mice. The ethanolic extract was administered at doses of 5, 10, 50, and 100?mg/kg, i.p. The control group received saline as vehicle of ethanolic extract.

Results: Our results showed that the ethanolic extract (50 and 100?mg/kg) decreased both phases of pain in the formalin test (ED₅₀?=?109.66 and 87.13?mg/kg, respectively). In the hot-plate test, the extract (50 and 100?mg/kg) increased pain threshold during 60?min (ED₅₀?=?81.03?mg/kg). The extract (50 and 100?mg/kg) exhibited antinociceptive activity against acetic acid-induced writhing (ED₅₀?=?66.99?mg/kg). The extract (50 and 100?mg/kg) showed significant activity in the xylene ear edema test (ED₅₀?=?78.20?mg/kg). Pretreatment of the animals with naloxone decreased the analgesia induced by the extract in hot-plate and formalin tests; therefore, opioid receptors may be involved, at least partly, in the analgesic effect of tarragon extract.

Discussion and conclusion: The results suggested that tarragon have significant analgesic and anti-inflammatory effects in mice, and, therefore, further studies are required to evaluate these effects and additional potential of the plant.     

Antinociceptive effect of methanol extract of Capparis ovata in mice

Context: Capparis ovata Desf. (Capparaceae) grows widely in Turkey. Flower buds and fruits of the plant are used in folk medicine for their analgesic, antirheumatismal, and diuretic effects.

Objective: This study evaluated the possible antinociceptive effect of the methanol extract of C. ovata (CME) in mice.

Materials: The antinociceptive effect of methanol extract, prepared with the C. ovata flower buds, was studied at the doses of 50, 100, and 200?mg/kg (i.p.) using tail-immersion, hot-plate, and writhing tests in mice. Morphine sulfate (5?mg/kg; i.p.) and dipyrone (100?mg/kg; i.p.) were used as reference analgesic agents. Naloxone (5?mg/kg; i.p.) was also tested.

Results: It was observed that the C. ovata extract had a significant antinociceptive effect in these tests. In the hot-plate and tail-immersion test results, the doses of 50, 100, and 200?mg/kg increased the percentage of the maximum possible effect (MPE%) value for nociception significantly according to the control value (P?<?0.001). All doses of the extract decreased the number of acetic acid-induced abdominal constrictions in mice when compared with control group (P?<?0.001). These effects were inhibited by pretreatment with naloxone.

Discussion and conclusion: Based on the results obtained, it can be concluded that CME is a potentially antinociceptive agent which acts as both at the peripheral and central levels.     

Anticholinesterase,antioxidant, analgesic and anti-inflammatory activity assessment of Xeranthemum annuum L. and isolation of two cyanogenic compounds

Context: Xeranthemum annuum L. (Asteraceae) (XA) is an ornamental and medicinal species with limited bioactivity and phytochemical data.

Objective: Identification of anticholinesterase, antioxidant, anti-inflammatory and analgesic effects of the flower and root–stem (R-S) extracts of XA.

Materials and methods: Anticholinesterase (at 100?μg mL^?1) and antioxidant (at 1000?μg mL^?1) effects of various extracts were evaluated via microtiter assays, while anti-inflammatory and analgesic effects of the R-S extracts were tested using carrageenan-induced hind paw oedema (100 and 200?mg kg^?1) and p-benzoquinone (PBQ) writhing models (200?mg kg^?1) in male Swiss albino mice. The R-S ethanol extract of XA was subjected to isolation studies using conventional chromatographic methods.

Results: Most of the extracts showed inhibition over 85% against butyrylcholinesterase and no inhibition towards acetylcholinesterase. The flower chloroform and the R-S ethyl acetate extracts were most effective (97.85?±?0.94% and 96.89?±?1.09%, respectively). The R-S ethanol extract displayed a remarkable scavenging activity against DPPH (77.33?±?1.99%) and in FRAP assay, while the hexane extract of the R-S parts possessed the highest metal-chelating capacity (72.79?±?0.33%). The chloroform extract of the R-S caused a significant analgesic effect (24.4%) in PBQ writhing model. No anti-inflammatory effect was observed. Isolation of zierin and zierin xyloside, which were inactive in anticholinesterase assays, was achieved from the R-S ethanol extract.

Discussion and conclusion: This is the first report of anticholinesterase, antioxidant, analgesic and anti-inflammatory activities and isolation of zierin and zierin xyloside from XA. Therefore, XA seems to contain antioxidant and BChE-inhibiting compounds.     

Analgesic Activity of Dalbergia lanceolaria. Bark Extract in Swiss Albino Mice

Abstract

The ethanol extract of Dalbergia lanceolaria. Linn. bark was subjected to pharmacological screening using various animal models. The extract showed analgesic activity when tested in acetic acid–induced writhing, tail-flick response, and formalin-induced licking tests in Swiss albino mice. The plant extract, at doses of 100, 200, and 400 mg/kg body weight, showed significant central as well as peripheral analgesic activity by oral route. Therefore, the current study indicates that the ethanol extract of Dalbergia lanceolaria. bark has significant central and peripheral analgesic activity.     

Lipid-lowering property of Clausena anisum-olens in hypercholesterolemic rats

Context: Clausena anisum-olens (Blanco) Merr. (Rutaceae) is a medicinal shrub which has been reported to have various pharmacological uses. No study regarding the effects of C. anisum-olens on cholesterol-lowering has been reported.

Objective: The effects of the ethanol extract of C. anisum-olens leaves on the cholesterol level of hypercholesterolemic rats were evaluated.

Materials and methods: Acute oral toxicity of the extract (175, 550 and 2000?mg/kg) was determined using female Sprague-Dawley rats, as described in OECD 425 Main test guidelines. The lipid-lowering assay utilized 30 male Sprague-Dawley rats divided into five groups (A–E). Triton X-100 was administered to induce hypercholesterolemia. After hypercholesterolemia induction, oral treatment of Atorvastatin and crude ethanol extract was given daily to the treatment groups for 14 days. The total cholesterol, triglycerides, HDL and LDL were determined before induction, after induction, after first week of treatment and after second week of treatment.

Results: Acute oral toxicity showed the crude extract is nontoxic up to 2000?mg/kg. The lipid-lowering assay indicated reduction of serum cholesterol (87.21?±?5.10?mg/dL), triglycerides (58.09?±?4.10?mg/dL) and LDL (27.82?±?4.11?mg/dL) for 200?mg/kw extract. Reduction in serum cholesterol (74.72?±?3.64?mg/dL), triglycerides (52.79?±?2.98?mg/dL) and LDL (12.06?±?5.51?mg/dL) were observed for 400?mg/kg group. The result is comparable to Atorvastatin, which showed serum cholesterol (80.90?±?9.72?mg/dL), triglycerides (55.94?±?7.19?mg/dL) and LDL (22.09?±?7.60?mg/dL) reduction.

Discussion and conclusion: The crude extract of C. anisum-olens proved to be useful in lowering of cholesterol.     

Antidepressant and anxiolytic activity of Lavandula officinalis aerial parts hydroalcoholic extract in scopolamine-treated rats

Context: Anxiety and depression are common in Alzheimer’s disease (AD). Despite some evidence, it is difficult to confirm Lavandula officinalis Chaix ex Vill (Lamiaceae) as an anxiolytic and antidepressant drug.

Objective: The effects of L. officinalis extract were studied in scopolamine-induced memory impairment, anxiety and depression-like behaviour.

Materials and methods: Male NMRI rats were divided into control, scopolamine alone-treated group received scopolamine (0.1?mg/kg) intraperitoneally (i.p.), daily and 30?min prior to performing behavioural testing on test day, for 12 continuous days and extract pretreated groups received aerial parts hydro alcoholic extract (i.p.) (100, 200 and 400?mg/kg), 30?min before each scopolamine injection. Memory impairment was assessed by Y-maze task, while, elevated plus maze and forced swimming test were used to measure anxiolytic and antidepressive-like activity.

Results: Spontaneous alternation percentage in Y maze is reduced by scopolamine (36.42?±?2.60) (p?≤?0.001), whereas lavender (200 and 400?mg/kg) enhanced it (83.12?±?5.20 and 95?±?11.08, respectively) (p?≤?0.05). Also, lavender pretreatment in 200 and 400?mg/kg enhanced time spent on the open arms (15.4?±?3.37 and 32.1?±?3.46, respectively) (p?≤?0.001). On the contrary, while immobility time was enhanced by scopolamine (296?±?4.70), 100, 200 and 400?mg/kg lavender reduced it (193.88?±?22.42, 73.3?±?8.25 and 35.2?±?4.22, respectively) in a dose-dependent manner (p?≤?0.001).

Discussion and conclusion: Lavender extracts improved scopolamine-induced memory impairment and also reduced anxiety and depression-like behaviour in a dose-dependent manner.     

Pereskia aculeata: A plant food with antinociceptive activity

Abstract

Context: Pereskia aculeata Miller (Cactaceae) is a cactus distributed from south to northeast of Brazil, where its leaves are commonly used as a vegetable, in skin wound healing, and to treat inflammation.

Objectives: The objective of this study was to perform the chemical characterization and to evaluate the antinociceptive activity of the hydromethanolic fraction obtained from the methanol extract of P. aculeata leaves.

Materials and methods: Chemical characterization was performed by UPLC–MS analysis. The antinociceptive activity was evaluated by the acetic acid-induced writhing, formalin, and tail-flick tests in mice, administering the single oral doses of 100, 200, and 300?mg/kg 1?h before each test.

Results: Tryptamine, abrine, mescaline, hordenine, petunidin, di-tert-butylphenol isomers, and quercetin were identified. The antinociceptive activity was inversely proportional to the administered doses in the acetic acid test, as the dose of 100?mg/kg reduced by 78% the number of writhings, while the doses of 200 and 300?mg/kg reduced by 64% and 41%, respectively. In the formalin test, the dose of 300?mg/kg inhibited by 50% and 86% the licking paw time in the first and second phases, respectively, while the doses of 200?mg/kg (45% and 62%, respectively) and 100?mg/kg (15% and 48%, respectively) were less effective. The sample did not respond to the tail-flick test. Those results suggested a peripheral and central antinociception devoid of an opioid effect.

Conclusion: Pereskia aculeata not only is a plant food with high nutritional value but also presents analgesic potential. It is the first time that this bioactivity is reported for this species.     

The stem bark extracts of Cenostigma macrophyllum attenuates tactile allodynia in streptozotocin-induced diabetic rats

Abstract

Context. Cenostigma macrophyllum Tul. var. acuminata Teles Freire (Leguminosae- Caesalpinioideae) is popularly known as “caneleiro”. Previous studies showed antioxidant action and analgesic effects of the ethanol extract from the leaves of C. macrophyllum. The phytochemical evaluation of the stem bark revealed the presence of antinociceptive compounds.

Objective: To investigate the antinociceptive actions of the ethanol extract and ethyl acetate fraction from C. macrophyllum stem bark in streptozotocin (STZ)-induced diabetic rats and the involvement of opioid and nitrergic mechanisms.

Materials and methods: STZ-rats received the ethanol extract (E.EtOH 200 and 300?mg/kg, p.o.) during 5 weeks. In acute experiments, untreated diabetic rats were treated with the ethyl acetate fraction (F.EtOAc 250 and 500?mg/kg, p.o.), on the 28th day of diabetes induction when the opioid and nitrergic mechanisms were investigated. The mechanical nociceptive threshold (MNT) was determined by application of von Frey filaments.

Results: Data show that STZ-induced diabetic rats developed a significant tactile allodynia during 5 weeks. Diabetic rats that received E.EtOH (200 and 300?mg/kg) and F.EtOAc (250 and 500?mg/kg) had a pain threshold higher than those in the STZ-vehicle group. F.EtOAc effects were inhibited by pretreatment with naloxone and were not influenced by .-arginine.

Discussion and conclusion: The results suggest that the ethanol extract and ethyl acetate fraction of C. macrophyllum presented antinociceptive activity. Thus, F.EtOAc may be exerting its effect by affecting the opioid system, but nitrergic mechanisms are not detectable. The observed activity may be due to its gallic acid, lupeol and bergenin content.     

Hydroalcoholic extract of Myrtus communis can alter anxiety and sleep parameters: a behavioural and EEG sleep pattern study in mice and rats

Context: Myrtus communis L. (Myrtaceae), myrtle, is an evergreen shrub with strong antibacterial, anti-inflammatory, antihyperglycemic and antioxidant activities. Also, it is used as a sedative-hypnotic plant in Iranian traditional medicine.

Objective: This study evaluates the effect of 80% ethanolic extract of M. communis leaves on sleep and anxiety in mice and rats.

Materials and methods: Male NMRI mice were subjected to open field, righting reflex, grip strength and pentylentetrazole-induced seizure tests. Male Wistar rats were used to evaluate the alterations in rapid eye movement (REM) and non-REM (NREM) sleep. They were treated with 25–400?mg/kg doses of the extract intraperitoneally.

Results: The applied doses (50–200?mg/kg) of M. communis extract increased vertical (ED_50?=_?40.2?±?6.6?mg/kg) and vertical and horizontal activity (ED_50?=_?251?±?55?mg/kg), while treatment with 200 and 400?mg/kg attenuated muscle tone significantly compared to vehicle treated animals (p?<?0.001 for all) in a dose-independent manner. Also, a significant hypnotic and not anticonvulsant effect was observed when animals were treated with 200?mg/kg of the extract (p?<?0.01). In this regard, electroencephalography results showed that REM sleep time was decreased (2.4?±?0.5%), while total and NREM sleep times were increased significantly compared to the control group of mice (82.5?±?7.6%).

Discussion and conclusion: The data show the anxiolytic and muscle relaxant effect of the extract without anticonvulsant activities. The anxiolytic, myorelaxant and hypnotic effects without effect on seizure threshold are in line with the effect of a alpha 2 GABA receptor agonist.     

Anti-inflammatory,Antinociceptive, and Neuropharmacological Activities of Clerodendron viscosum.

Abstract

The crude methanol extract of Clerodendron viscosum. Vent. (Verbenaceae) leaves was evaluated for its anti-inflammatory, antinociceptive, and neuropharmacological activities. When given orally to rats at doses of 200 and 400 mg/kg of body weight, the extract showed a significant (p < 0.001) anti-inflammatory activity against carrageenan-induced rat paw edema comparable with the standard drug phenylbutazone at the dose of 100 mg/kg of body weight. It also produced a significant writhing inhibition in acetic acid–induced writhing in mice at the oral dose of 250 and 500 mg/kg of body weight (p < 0.001), which was comparable with the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. Moreover, when given intraperitoneally to albino mice, it potentiated the pentobarbital-induced sleeping time (p < 0.001), decreased the open field score in open field test (p < 0.001), decreased the number of holes crossed from one chamber to the other in the hole-cross test (p < 0.001), and decreased the head dip responses in the hole-board test (p < 0.001) at the dose of 250 and 500 mg/kg of body weight. The overall results tend to suggest the anti-inflammatory, antinociceptive, and central nervous system depressant activities of the crude methanol extract of Clerodendron viscosum..     

Pharmacological properties of lichen Cladonia clathrata

Cladonia clathrata Ahti & L. Xavier-Filho (Cladoniaceae) is a lichen; several Cladonia species extracts have been used for various remedies in folk medicine. In order to evaluate the actions of this lichen, studies were performed on antinociceptive, anti-inflammatory, and antioxidant activities. The hydroalcoholic extract (HE) of C. clathrata stems was used in the following experiments. Oral treatment with the HE of C. clathrata elicited inhibitory activity (p?<?0.001) on acetic acid-induced abdominal writhes at 100 (47.2%), 200 (47.2%), and 400?mg/kg (86.4%), and reduced the formalin-induced nociception on both the neurogenic (400?mg/kg, p?<?0.01) and inflammatory phases (200 and 400?mg/kg, p?<?0.01). It was not associated with non-specific effects, such as muscle relaxation or sedation. The HE reduced the carrageenan-induced edema formation at 100, 200, and 400?mg/kg (p?<?0.05) and inhibited neutrophil migration into the peritoneal cavity at 400?mg/kg (p?<?0.001). The HE of C. clathrata reacted with the DPPH radical and reduced the same by 50.19%, and exhibited an IC₅₀ value of 69.25?±?0.65 μg/mL. The HE of C. clathrata stems shows antinociceptive and anti-inflammatory activities, with a moderate antioxidant potential.     

Antioxidant,anti-collagenase and anti-elastase activities of Phyllanthus emblica,Manilkara zapota and silymarin: an in vitro comparative study for anti-aging applications

Context Phyllanthus emblica L. (Euphorbiaceae) (amla), Manilkara zapota L.P. Royen (Sapotaceae) (sapota) and silymarin are reported to contain antioxidant effects. However, information on other biological activities relating to the anti-aging properties is limited.

Objective To compare in vitro antioxidants, anti-collagenase (MMP-1 and MMP-2) and anti-elastase properties as well as the phenolic and flavonoid contents of amla, sapota and silymarin as potential anti-aging ingredients.

Materials and methods The ethanol amla and sapota fruit extracts were prepared by three cycles of maceration with 24 h duration each. The total phenolic (TPC) and flavonoid (TFC) contents were determined. The antioxidant capacity was evaluated by DPPH and ABTS assays. The effects of MMP-1, MMP-2 and elastase inhibitions were determined by using the EnzChek® assay kits (Molecular-Probes, Eugene, OR).

Results Amla exhibited the highest in TPC (362.43?±?11.2?mg GAE/g) while silymarin showed the highest in TFC (21.04?±?0.67?mg QE/g). Results of antioxidant activity by DPPH and ABTS methods showed that amla possessed the most potent capacity with IC₅₀ values of 1.70?±?0.07 and 4.45?±?0.10?μg/mL, respectively. Highest inhibitions against MMP-1, MMP-2 and elastase were detected for sapota with IC₅₀ values of 89.61?±?0.96, 86.47?±?3.04 and 35.73?±?0.61?μg/mL, respectively.

Discussion and conclusion Test extracts offered anti-aging properties in different mechanisms. Amla showed the highest phenolic content and antioxidant property with moderate anti-collagenase. Silymarin exhibited measurable flavonoid content with anti-elastase effect. Sapota showed the highest collagenase and elastase inhibitions with moderate antioxidant effect. Thus, extracts might be added as a mixture to gain the overall anti-aging effects.     

Appraisal of anti-arthritic and nephroprotective potential of Cuscuta reflexa

Context: Cuscuta reflexa Roxb. (Cuscutaceae) has been used traditionally for treating sore knees and kidney problems, but its efficacy has not been scientifically examined in treating arthritis and nephrotoxicity.

Objective: Present study determines antiarthritic and nephroprotective potential of the aqueous methanolic extract of Cuscuta reflexa (AMECR).

Materials and methods: Antiarthritic activity of Cuscuta reflexa in formaldehyde and turpentine oil-induced rat arthritis models was appraised at 200, 400 and 600?mg/kg doses for 10 days and 6?h period, respectively, and in vitro protein denaturation (bovine serum albumin, egg albumin) inhibition was studied at 25–800?μg/mL concentration. The nephroprotective effect involved gentamicin-induced nephrotoxicity in rats at 200, 400 and 600?mg/kg doses.

Results: Plant extract at 600?mg/kg significantly reduced paw oedema and joint swelling with maximal inhibition of 71.22% at the 6th hour for turpentine oil and 76.74% on 10th day for formaldehyde. Likewise, in vitro results corroborated significant concentration-dependent increase in percentage protection at 800?μg/mL against both bovine serum albumin (89.30%) and egg albumin (93.51%) denaturation. Similarly, 600?mg/kg dose showed maximum nephroprotection by reducing serum urea (41.400?±?0.510?mg/dL), uric acid (0.740?±?0.032?mg/dL), blood urea nitrogen (18.370?±?0.328), creatinine (3.267?±?0.076) and minimizing kidney weight gain (0.586?±?0.005) and histopathological alterations on 8th day. Furthermore, phytochemical and HPLC analysis revealed the presence of important phytoconstituents.

Discussion and conclusions: These results suggest that AMECR provides protection against arthritis and nephrotoxicity that might be due to the existence of phytoconstituents, thus supporting folkloric claim.