Evaluation of antisecretory, gastroprotective and in-vitro antacid capacity of Fumaria indica in rats.

Fumaria indica is used for its anthelmintic, antidyspeptic, cholagogue, diaphoretic, diuretic, laxative, stomachic, tonic properties and claimed to possess various properties for the ailments of blood, skin, gastrointestinal systems and central nervous system. The present study was undertaken to evaluate antisecretory, gastroprotective and in-vitro antacid capacity of ethanol extract from F. indica in rats. Evaluation of F. indica extract as antisecretory was carried out by pyloric ligation induced ulcer model. The gastroprotective effect was carried out by absolute ethanol induced ulcer model. Integrity of gastric mucosa was evaluated by estimation of GSH and gastric mucus level. The in-vitro antacid capacity was evaluated by titration method. Ethanol extract of F. indica at 200 mg kg(-1), orally showed inhibition of secretion in pyloric ligation model. GSH level (1.67 µg mg(-1) protein), gastricwall mucus (240.76 µg g(-1) wet glandular tissue) and percentage protection (77.59%) of ulcer were significantly (P < 0.05) increased in absolute ethanol induced ulcer model. The in-vitro antacid capacity of ethanol extract of F. indica was compared with the standard. Conclusively, it appears that F. indica possess antisecretory (inhibition of acid secretion), gastroprotective (potentiation of defensive factors) and in-vitro antacid activity.

Ionotropic Cross-linked Carbo-protein Micro Matrix System: An Approach for Improvement of Drug Release, Compaction and Tableting behavior of Losartan Potassium.

The aim of the present research work is to develop carbo-protein polymeric complex based sustain release microspheres of losartan potassium and investigate the ability of this dosage form to improve the flowability, compressibility and tableting properties of losartan potassium. The influence of silk sericin, alginate and its blend on various physicochemical parameters and in vitro drug release pattern were studied to optimize the concentration of polymeric blend required for 12 h. sustain release. Optimized batch was subjected to different flowability, compressibility and tableting properties studies to observe the effects of carbo-protein microspheres on flow properties. Results indicated that the concentration of sericin was found to be the main influential factor for prolonged drug release. Different micromeritic studies revealed that the poor flowability and compressibility properties of pure losartan potassium were significantly improved by this algino-sericin microspheric dosage form. Research findings also revealed that plasticity, die filling behavior and tableting properties of the pure drug were significantly improved by this microsphere formulation. So these prospective results concluded that carbo-protein polymeric microspheres helps to sustain the drug release for prolong hours as well as improve the flowability, compressibility and tableting properties of losartan potassium.

Assessment of Antisecretory, Gastroprotective, and In-vitro Antacid Potential of Daucus carota in Experimental Rats.

OBJECTIVES: In Indo China, carrots have been reported to regulate the functions of the stomach and intestines. The objective of the present investigation was to unravel the therapeutic potential of 50% ethanol extract from Daucus carota roots (EDC) on antisecretory, gastroprotective, and in vitro antacid capacity using experimental rats. METHODS: Assessment of EDC antisecretory and in vivo antacid capacities was carried out using a pyloric ligation induced ulcer model. The gastroprotective effect was assessed with an absolute ethanol induced ulcer model. The integrity of gastric mucosa was evaluated using the estimation of glutathione and gastric mucus level and with histopathological examination of gastric mucosal cells. The in-vitro antacid capacity was evaluated using a titration method. The effect of the extract on the liver was assessed by measuring serum biochemical parameters. RESULTS: The EDC significantly (p < 0.01-0.001) reduced gastric lesions in both models. Furthermore, the EDC also significantly (p < 0.05-0.001) reduced the volume of gastric content whereas the total acidity was significantly (p < 0.05-0.001) reduced with the doses of 100 mg/kg and 200 mg/kg EDC. Moreover, the mucus content and glutathione level increased significantly (p < 0.05) in the absolute alcohol-induced ulcer. The EDC also showed in-vitro antacid capacity. Histopathological studies further confirmed the potential of EDC by inhibiting congestion, edema, hemorrhage, and necrosis in gastric mucosa. CONCLUSION: The EDC exerted antisecretory, gastroprotective, and in vitro antacid potential. These activities could be attributed due to the presence of glycosides, phenolics, tannins, alkaloids, and flavonoids.

Protective effect of Lygodium flexuosum (family: Lygodiaceae) against excision, incision and dead space wounds models in experimental rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Lygodium flexuosum (Linn) Sw. is a climbing fern, and it is the sole genus in the family Lygodiaceae. It commonly grows epiphytically on moss covered tree trunks and branches as lithophytes on shady boulders along with moss. It has been reported as a traditional folkloric medicine for a variety of ailments particularly useful for carbuncles, inflammation, ulcer, various respiratory diseases, general disorders, muscle sprains and acts as panacea for wounds. However, there are no scientific reports on wound healing activity of the plant L. flexuosum (Linn) Sw. AIM OF THE STUDY: To explore the protective effect of L. flexuosum against excision, incision and dead space wounds models in experimental rats. METHODS: Wistar albino rats of either sex weighing between 180 and 220 g were topically treated with extract formulated in ointment using simple ointment BP as base. Ointments, 4% and 5% (w/w), were applied once daily in excision wound model. L. flexuosum ethanolic extract was given orally at a dose of 100, 200 and 400 mg/kg in incision and dead space wound healing models. Rats of standard groups were treated with 0.2% nitrofurazone ointment topically. The percentage wound contraction, epithelization time in excision wound model; breaking strength in incision wound model and wet and dry granulation weight, hydroxyproline content were measured. RESULTS: Topical application of L. flexuosum in excision wound model increased the percentage of wound contraction, and the epithelization time was decreased. In the incision wound model, the breaking strength of wounds increased and in dead space model the weight of dry and wet granuloma of wounds and hydroxyproline was increased. Conclusively, the data of present study indicated that the leaf extract of L. flexuosum accelerated wound healing in rats and thus supports its traditional use.

A RP-HPLC method for quantification of diclofenac sodium released from biological macromolecules.

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug, were prepared by single water-in-water (w/w) emulsion gelation process using AlCl3 as cross-linking agent in a complete aqueous environment. Pharmacokinetic study of these IPN microbeads was then carried out by a simple and feasible high-performance liquid chromatographic method with UV detection which was developed and validated for the quantification of diclofenac sodium in rabbit plasma. The chromatographic separation was carried out in a Hypersil BDS, C18 column (250 mm × 4.6 mm; 5 m). The mobile phase was a mixture of acetonitrile and methanol (70:30, v/v) at a flow rate of 1.0 ml/min. The UV detection was set at 276 nm. The extraction recovery of diclofenac sodium in plasma of three quality control (QC) samples was ranged from 81.52% to 95.29%. The calibration curve was linear in the concentration range of 20-1000 ng/ml with the correlation coefficient (r(2)) above 0.9951. The method was specific and sensitive with the limit of quantification of 20 ng/ml. In stability tests, diclofenac sodium in rabbit plasma was stable during storage and assay procedure.

Al3+ ion cross-linked interpenetrating polymeric network microbeads from tailored natural polysaccharides.

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a non steroidal anti-inflammatory drug were prepared by single water-in-water (w/w) emulsion gelation process using AlCl(3) as cross-linking agent in a complete aqueous environment. The influence of different variables like total polymer concentration, gelation time and crosslinker content on in vitro physico-chemical characteristics and drug release rate in different media was investigated. Drug loaded microbeads were evaluated through Fourier transform infra-red (FTIR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses. Scanning electron microscopy (SEM) micrograph of the beads suggested the formation of spherical particles. FTIR analysis indicated the stable nature of the drug in the blend microbeads. DSC and XRD analysis revealed amorphous state of drug after encapsulation. The drug release profile in acidic medium was considerably less in comparison to alkaline media. Formulations showed non-Fickian type transport mechanism. These tri-valent ion crosslinked beads not only improve drug encapsulation efficiency but also enhance drug release in phosphate buffer.

Acute, sub-chronic oral toxicity studies and evaluation of antiulcer activity of Sooktyn in experimental animals.

Sooktyn (SKN), mineralo-herbal drug which is being used largely by the patients for its extremely good therapeutic value to treat the gastric ulcers. The present study was undertaken to evaluate the toxicity studies and antiulcer activity of SKN. Acute and sub-chronic toxicities were studied in male and female Wistar rats. A single acute SKN of 2 000 mg/kg was administered by oral gavage for acute toxicity. Sub-chronic doses were 400 and 800 mg/kg/day. The major toxicological end points examined included animal body weight and food intake, selected tissue weights, and detailed gross necropsy. In addition, we examined blood elements: hematocrit, hemoglobin concentration, erythrocyte count, total leukocyte count and MCH, MCHC and platelets as well as biochemical parameters: urea, sugar, alanine transaminase, aspartate transaminase, alkaline phosphatase, total proteins, and creatinine. Also, anti-ulcer activity was carried out by employing indomethacin, ethanol, pylorus ligation, and hypothermic-stress-induced ulcer models. LD(50) may be greater than 2 000 mg/kg (orally) for SKN and there were no signs of toxicity on 28 days sub-chronic oral administration of 400 and 800 mg/kg of SKN in rats on the basis of blood elements and biochemical parameters. The ulcer indices decrease in all ulcer models with 66.62%, 61.24%, 80.18%, and 74.76% in indomethacin, ethanol, pylorus ligation, and hypothermic-stress-induced ulcer models, respectively. The results suggest that SKN has no signs of toxicity at 2 000 mg/kg body weight of rats orally; sub-chronically. The drug is safe and has antiulcer activity.

Dietary-induced cancer prevention: An expanding research arena of emerging diet related to healthcare system.

Diet plays a vital role in the management of cancer because they are the source of important physiologically functional components. Scientific observations support the idea that dietary supplement can prevent breast cancer recurrences. Strong correlations are established between the high intake of saturated fat and the incidence of different types of cancer. It is found that chronic alcohol consumption is associated with increased risk of cancers of oral cavity, pharynx, esophagus, and larynx. Again, some evidences are also found regarding phosphorous, glutamate level in the body, and incidence of cancer. Different physiologically functional components are found in the dietary materials. Fibers, the major dietary components, have long been recognized for the unique properties in the treatment of cancer, which are related to its antineoplastic functions. Antioxidant rich diet has been added to the list of cancer-preventing dietary components. Also, recently published research has shown that natural carotenoids in the diet leads to a normalization of body epithelial cells and protects against the risk of stomach and esophagus cancer, and improves the immune system's response. Again, fruit juices, processed vegetable juices, orange peel, green tea, vitamins, flavonoids, and trace materials have cancer inhibitory properties. Clearly, there has been increasing recognition of chemoprotective functions. Now, it can be recognized for another kind of functionality for the improvement of the health of mankind.

Preparation and in vitro in vivo evaluation of aceclofenac loaded alginate microspheres: an investigation of effects of polymer using multiple comparison analysis.

The aim of this present research work was to prepare and evaluate alginate microspheres of aceclofenac by ionic gelation method for targeting the drug release in intestinal region and decrease distinct tissue protection in the stomach. This method offers to prepare microspheres which are important in controlling the release rate and the absorption of aceclofenac from the intestinal region. Variation in polymer concentration was studied systemically for their influence on the encapsulation efficacy, particle size and in vitro drug release. The enteric nature of the microspheres showed very less amount of drug released in acidic medium. The mucoadhesion property was strongly dependent on the pH of the medium and the polymer concentration in the formulations. In vitro drug release study proposed a mixed drug release mechanism, partially involving the sphere matrix disintegration and drug diffusion of the microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t50% values among all the microsphere formulations. In vivo studies revealed that the anti-inflammatory effect induced by the aceclofenac loaded alginate microspheres was significantly high and prolonged than that induced by the pure aceclofenac. So, this aceclofenac loaded alginate microspheres exhibited promising properties to improve the patient compliance by controlling and prolonging the systemic absorption of aceclofenac along with a distinct tissue protection in the stomach.

Antihyperglycemic activity and antioxidant role of Terminalia arjuna leaf in streptozotocin-induced diabetic rats.

CONTEXT: Terminalia arjuna Roxb. (Combretaceae), commonly known as Arjuna, is a large tree grown throughout the Indian peninsula and used traditionally for several medicinal purposes. OBJECTIVE: To evaluate antihyperglycemic and antioxidant role of methanol extract of T. arjuna leaf (META) in Wistar rats. MATERIALS AND METHODS: Hyperglycemia was induced in rats by single intraperitoneal injection of streptozotocin (STZ, 65 mg/kg body weight). Three days after STZ induction, the hyperglycemic rats were treated with META orally at the dose of 100 and 200 mg/kg body weight daily for 15 days. Glibenclamide (0.5 mg/kg, orally) was used as reference drug. The fasting blood glucose levels were measured on every fifth day during the 15-day treatment. Serum biochemical parameters such as serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP), cholesterol, and total protein were estimated. Antioxidant properties were assessed by estimating hepatic lipid peroxidation, reduced glutathione (GSH), and catalase (CAT). RESULTS AND DISCUSSION: META at the dose of 100 and 200 mg/kg orally significantly (P < 0.001) and dose-dependently reduced and normalized blood glucose levels as compared with that of STZ control group. Serum biochemical parameters were significantly (P < 0.001) restored toward normal levels in META-treated rats as compared with STZ control. META treatment also significantly (P < 0.001) decreased lipid peroxidation and recovered GSH level and CAT activity toward normal as compared with STZ control. CONCLUSION: The present study infers that T. arjuna leaf demonstrated remarkable antihyperglycemic activity in STZ-induced diabetic rats. The potential antihyperglycemic action is plausibly due to its underlying antioxidant role.

Paralytic and lethal effects of Trichosanthes dioica root extracts in experimental worms.

CONTEXT: Trichosanthes dioica Roxb. (Cucurbitaceae), called pointed gourd in English, is a dioecious climber and its roots are traditionally used in India as a hydrogouge cathartic, tonic, and febrifuge, and in the treatment of jaundice, anasarca, and ascites. OBJECTIVE: To evaluate the in vitro effects of different solvent extracts of T. dioica root in experimental worms, viz. annelids and nematodes. MATERIALS AND METHODS: The in vitro paralytic and lethal effects of defatted dichloromethane (DCTD), methanol (METD), and aqueous (AQTD) extracts of T. dioica root were evaluated against Pheretima posthuma (Annelida) and Ascaridia galli (Nematoda) by keeping the worms in different concentrations of each test extract under specific experimental conditions followed by determination of mean paralysis and lethal times. Albendazole was used as the reference drug. RESULTS AND DISCUSSION: All the extracts demonstrated concentration-dependent paralytic and lethal effects on P. posthuma and lethal effects on A. galli. The DCTD was found to be the most potent followed by the METD and AQTD. A. galli was found to be more sensitive than P. posthuma against all extracts, indicating T. dioica root as an effective nematocide. CONCLUSION: The present study establishes the in vitro wormicidal property of T. dioica root extracts against the experimental worms, showing promising nematocidal (and hence anthelmintic) potential.

Antioxidant and free-radical-scavenging effects of fruits of Dregea volubilis.

This study evaluated the in vitro antioxidant potential of petroleum ether (60-80°C), chloroform, and methanol extract of the fruits of Dregea volubilis Benth (Asclepiadaceae). The different antioxidant assays, including total antioxidant activity, reducing power, free radical, super oxide anion radical, nitric oxide scavenging, lipid peroxidation, and total phenolic content were studied. The extracts exhibited potent total antioxidant activity that increased with increasing amount of extract concentration, which was compared with standard drug vitamin C at different concentrations as extracts. The different concentrations of all the extracts and vitamin C showed inhibition on lipid peroxidation. In addition, all the extracts had effective reducing power, free radical scavenging, super oxide anion scavenging, nitric oxide scavenging, lipid peroxidation, and total phenolic content depending on concentration. These various antioxidant activities were compared with standard antioxidant such as vitamin C at different concentration as different extracts.

Microsponges: A novel strategy for drug delivery system.

Microsponges are polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles with a large porous surface. Moreover, they may enhance stability, reduce side effects and modify drug release favorably. Microsponge technology has many favorable characteristics, which make it a versatile drug delivery vehicle. Microsponge Systems are based on microscopic, polymer-based microspheres that can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is typically porous, allowing a sustained flow of substances out of the sphere. Microsponges are porous, polymeric microspheres that are used mostly for topical use and have recently been used for oral administration. Microsponges are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects, and modify drug release.

Synthesis and antimalarial evaluation of some 4-quinazolinone derivatives based on febrifugine.

A series of 2-substituted and 2,3-substituted quinazolin -4(3H)-one derivatives were designed and synthesized based on the structure of febrifugine. The structures of the new compounds were confirmed by spectral analysis. The in vivo biological activity test results indicated that those compounds exhibited antimalarial activities against Plasmodium berghei in mice, at a dose of 5 mg/kg. Compared to Chloroquine and Artemisinin, these compounds have the advantages of shorter synthetic routes and consequently are highly cost effective in nature.

In vitro anti-leishmanial and anti-tumour activities of a pentacyclic triterpenoid compound isolated from the fruits of Dregea volubilis Benth Asclepiadaceae

Purpose: Dregea volubilis Benth, commonly known as Jukti in Bengal, is used in the treatment of boils and abscesses from ancient times. The purpose of this study is to elucidate the active compounds and as well as their anti-leishmanial and anti-tumour activities. Methods: Dried and crushed fruits of Dregea volubilis were extracted by petroleum ether (40 - 60°C); the best solvent system had first been verified by analytical Thin Layer Chromatography (TLC). The extract was subjected to TLC and column chromatography (CC) to isolate the pure compounds. Spectra data were obtained by Infra Red pectroscopy, Mass Spectroscopy and Nuclear Magnetic Resonance - Proton Magnetic Resonance (PMR), Carbon Magnetic Resonance (CMR) and Distortionless Enhancement by Polarization Transfer (DEPT) - for structure elucidation of the isolated compound(s). One of the compounds isolated was screened for anti-leishmanial activity against promastigotes of Leishmania donovani and anti-tumour activity on K562 leukemic cell line. Results: A pentacyclic triterpenoid compound was isolated and designated as taraxerone, and then characterized as d-friedoolean-14-en, 3 one together with ß-sitosterol and a long chain lipid fraction.. This compound showed in vitro anti-leishmanial activity against promastigotes of Leishmania donovani(strain AG 83) and anti-tumour activity on K562 leukemic cell line. Conclusion: A pentacyclic triterpenoid compound designated as taraxerone and characterized as Dfriedoolean-14-en, 3 one together was successfully isolated. The structure was determined on the basis of spectral analysis (IR, MASS, NMR (PMR, CMR and DEPT) and the compound demonstrated in vitro anti-leishmanial and anti-tumour activities

Antibacterial activity of Abies webbiana.

The methanol extract of the dried leaves of Abies webbiana was evaluated for antimicrobial activity. The methanol extract showed a broad spectrum of antibacterial activity.

Synergistic effect of methanol extract of Abies webbiana leaves on sleeping time induced by standard sedatives in mice and anti-inflammatory activity of extracts in rats.

During the determination of LD50 values of extracts of Abies webbiana, it was observed that the methanol extract (MEAW) produces sedation of animals. This led to investigation of the effect of MEAW on sleeping time in mice. When various doses of the methanol extract (100, 150, and 200 mg/kg body weight) were administered alone, no hypnotic activity was observed. However, these exhibited significant synergistic effects (P < 0.001) at those dose levels in mice when administered prior to the administration of standard sedatives (pentobarbitone sodium: 50 mg/kg and diazepam: 6 mg/kg, respectively). In addition anti-inflammatory effects of methanol, chloroform, and petroleum ether extracts of Abies webbiana leaves in rats were performed to assess scientific validity of the medicinal claim of Indian folk medicine. The effects of leaf extracts (methanol, chloroform, and petroleum ether) against inflammation were studied by carrageenan-induced paw edema model in rats. The methanol extract (400 mg/kg p.o.) of leaves of Abies webbiana showed the best significant anti-inflammatory activity as compared to that of diclofenac sodium (150 mg/kg p.o.). The LD50 values of methanol, chloroform, and petroleum ether extracts were found to be 986, 1387, and > 3200 mg/kg, respectively. Thus, the therapeutic index of methanol extract may be favorable to open a new vista on combination therapy of hypnotics and may also against inflammation.