Protective effect of Blumea lacera DC aerial parts in indomethacin-induced enterocolitis in rats.

Traditionally Blumea lacera DC is used to treat inflammation and bowel ailments. Lack of specific, curative treatment for IBD enticed us to investigate the therapeutic efficacy of ethanolic extract of aerial parts of Blumea lacera DC (EEBL) against indomethacin-induced enterocolitis. Male Wistar rats were divided into six groups (n = 5) and different doses of EEBL (100 and 200 mg/kg, p.o) and sulphasalazine (100 mg/kg, p.o) were administered for seven days. Enterocolitis was induced by two subsequent doses of indomethacin (7.5 mg/kg, s.c) on 7th and 8th day. Treatments were continued up to 12th day and sacrificed. The protective effect was assessed on the basis of macroscopic scores of ileum strips, changes in biochemical parameters such as serum lactate dehydrogenase (LDH), tissue myeloperoxidase (MPO), lipid peroxidation (LPO), and total thiols (TT). Further, activity was ascertained by histopathological evaluations. HPLC fingerprinting profiling of EEBL was also carried out. Pre-treatment with EEBL or sulphasalazine significantly attenuated the indomethacin-induced proximal ileal damage, elevated levels of serum LDH, tissue MPO, LPO and lower levels of TT. Further, observed activity of EEBL was well correlated with histopathological alterations. The results revealed the protective action of the title plant against the indomethacin-induced enterocolitis in rats, which might be attributed by its antioxidant, anti-inflammatory, antimicrobial, and membrane-stabilizing properties.

Bixin loaded solid lipid nanoparticles for enhanced hepatoprotection--preparation, characterisation and in vivo evaluation.

In the present study, a natural antioxidant drug, bixin was loaded into solid lipid nanoparticles using trimyristin and glycerol monostearate as different lipid matrices and soya and egg lecithin as stabilizers. Developed bixin SLNs were characterized including in vitro drug release and in vivo evaluation of hepatoprotective activity using Wistar rats. Bixin SLNs were prepared by hot homogenisation followed by ultrasonication technique. The particle size ranged from 135.5-352.8 nm with PDI 0.185-0.572. Zeta potential of bixin SLNs was -17.9 to -36.5 mV. Bixin was successfully incorporated into SLNs with entrapment efficiency above 99% and loading efficiency maximum 17.96%. There was no interaction of bixin with selected lipids TM and GMS, confirmed by FTIR studies. DSC studies revealed that preparation method did not change crystallinity of bixin and TM whereas GMS crystallinity was reduced. In vitro drug release studies in Sorensen buffer, pH 7.7 exhibited initial burst effect followed by a sustained release of bixin. Drug release kinetic studies showed that the release was first order diffusion controlled and the n-values obtained from the Korsmeyer-Peppas model indicated the release mechanism was non-Fickian type. In vivo studies revealed better treatment of paracetamol induced hepatotoxicity by bixin SLNs indicating significant localisation of them in liver.

Protective effect of Calendula officinalis Linn. flowers against 3-nitropropionic acid induced experimental Huntington's disease in rats.

Oxidative stress (OS) and nitric oxide mechanisms have been recently proposed in 3-nitropropionic acid (3-NP)-induced neurotoxicity. The compounds, having antioxidant, anti-inflammatory and estrogenic effects, have been suggested for neuroprotection in different experimental models. Calendula officinalis Linn. flower extract (COE) is known for its potent antioxidant, anti-inflammatory, estrogenic and neuroprotective activities. Hence, the present study was designed to evaluate the neuroprotective effect of COE on 3-NP-induced neurotoxicity in rats by observing behavioral changes, OS and striatal damage in rat brain. Adult female Wistar rats were pretreated with vehicle or COE (100 and 200 mg/kg) for 7 days, followed by cotreatment with 3-NP (15 mg/kg, intraperitoneally) for the next 7 days. At the end of the treatment schedule, rats were evaluated for alterations in sensory motor functions and short-term memory. Animals were sacrificed and brain homogenates were used for the estimation of lipid peroxidation (LPO), glutathione, total thiols, glutathione S-transferase, catalase and nitrite. A set of brain slices was used for the evaluation of neuronal damage in the striatal region of the brain. 3-NP caused significant alterations in animal behavior, oxidative defense system evidenced by raised levels of LPO and nitrite concentration, and depletion of antioxidant levels. It also produced a loss of neuronal cells in the striatal region. Treatment with COE significantly attenuated behavioral alterations, oxidative damage and striatal neuronal loss in 3-NP-treated animals. The present study shows that COE is protective against 3-NP-induced neurotoxicity in rats. The antioxidant, anti-inflammatory and estrogenic properties of COE may be responsible for its neuroprotective action.

Synthesis and evaluation of analgesic and anti-inflammatory activities of most active free radical scavenging derivatives of embelin-A structure-activity relationship.

Antioxidant and related properties of the plant Embelia ribes and embelin are well known. In the present study embelin was condensed with various aromatic substituted primary amines to yield ten new and one reported derivatives along with monomethyl embelin. All these compounds along with embelin were evaluated for in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picryl hydrazyl (DPPH) methods. Two para-substituted embelin derivatives showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and both of its derivatives almost completely abolished the acetic acid induced writhing. p-Sulfonylamine phenylamino derivative showed better anti-inflammatory activity than embelin.

Protective effect of embelin against acetic acid induced ulcerative colitis in rats.

The aim of the present study is to evaluate the effect of embelin isolated from Embelia ribes on acetic acid induced colitis in rats. Experimental animals received embelin (25 and 50 mg/kg, p.o.) and sulfasalazine (100mg/kg, p.o.) for five consecutive days before induction of colitis by intra-rectal acetic acid (3% v/v) administration and the treatment continued up to 7 days. The colonic mucosal injury was assessed by clinical, macroscopic, biochemical and histopathological examinations. Embelin treatment significantly decreased clinical activity score, gross lesion score, percent affected area and wet colon weight when compared to acetic acid induced controls. The treatment also reduced significantly the colonic myeloperoxidase activity, lipid peroxides and serum lactate dehydrogenase and significantly increased the reduced glutathione. The histopathological studies also confirmed the foregoing findings. The protective effect may be due to its antioxidant and anti-inflammatory activities.