Therapeutic potential of Ceratonia siliqua extract for the management of asthma and hypertension.

The current work was performed to explore the pharmacological mechanisms involved in the management of asthma and hypertension along with the safety profile of the Ceratonia siliqua (C. siliqua/Carob) pods. The bronchorelaxant, vasorelaxant, and cardioselective activities of C. siliqua pods were investigated using isolated rabbit tracheal, aortic, and paired atrial fragments on the Power lab data acquisition system. Normotensive rats were used to study antihypertensive activity. The plant extract and its fractions relaxed the carbachol-induced contraction in the tracheal fragments and shifted the concentration-response curve of carbachol towards the right confirming the muscarinic receptor antagonist activity. The relaxation of phenylephrine-induced contraction in an aortic fragment by the extract showed α- adrenergic blocking activity. Furthermore, the extract produced a cardio-selective response in the paired atria and decreased the blood pressure in anesthetized normotensive rats. The plant extract proved to be non-toxic in oral acute and chronic toxicity studies and did not demonstrate any sign of histopathological lesions. These results suggested that the plant extract was non-toxic and could be used in the management of lifetime therapies of respiratory and cardiovascular disorders without any unwanted effects.

The Spasmolytic, Bronchodilator, and Vasodilator Activities of Parmotrema perlatum Are Explained by Anti-Muscarinic and Calcium Antagonistic Mechanisms.

Parmotremaperlatum is traditionally used in different areas of Pakistan to treat gastrointestinal, respiratory, and vascular diseases. This study evaluates the underlying mechanisms for traditional uses of P. perlatum in diarrhea, asthma, and hypertension. In vitro pharmacological studies were conducted using isolated jejunum, trachea, and aortic preparations, while the cytotoxic study was conducted in mice. Crude extract of P. perlatum(Pp.Cr), comprising appreciable quantities of alkaloids and flavonoids, relaxed spontaneously contracting jejunum preparation, K+ (80 mM)-induced, and carbachol (1 µM)-induced jejunum contractions in a concentration-dependent manner similar to dicyclomine and dantrolene. Pp.Cr showed a rightward parallel shift of concentration-response curves (CRCs) of Cch after a non-parallel shift similarto dicyclomine and shifted CRCs of Ca+2 to rightward much likeverapamil and dantrolene, demonstrating the coexistence of antimuscarinic and Ca+2 antagonistic mechanism. Furthermore, Pp.Cr, dicyclomine, and dantrolene relaxed K+ (80 mM)-induced and Cch (1 µM)-induced tracheal contractions and shifted rightward CRCs of Cch similar to dicyclomine, signifying the dual blockade. Additionally, Pp.Cr also relaxed the K+ (80 mM)-induced and phenylephrine (1 µM)-induced aortic contraction, similarly to verapamil and dantrolene, suggesting Ca+2 channel antagonism. Here, we explored for the first time thespasmolytic and bronchodilator effects of Pp.Crand whether they maybe due to the dual blockade of Ca+2 channels and muscarinic receptors, while the vasodilator effect might be owing to Ca+2 antagonism. Our results provide the pharmacological evidence that P. perlatum could be a new potential therapeutic option to treat gastrointestinal, respiratory, and vascular diseases. Hence, there is a need for further research to explore bioactive constituent of P. perlatum as well as further investigation by suitable experimental models are required to further confirm the importance and usefulness of P. perlatum in diarrhea, asthma, and hypertension treatment.

Studies on antidiarrheal and laxative activities of aqueous-ethanol extract of Asphodelus tenuifolius and underlying mechanisms.

BACKGROUND: Asphodelus tenuifolius Cav. (Asphodelaceae) has traditional reputability in treatment of diarrhea and constipation but no scientific study has been reported for its gastrointestinal effects. Present study was conducted to evaluate antidiarrheal and laxative activities of the plant. METHODS: Aqueous-ethanol crude extract of Asphodelus tenuifolius (At.Cr) was subjected to phytochemical screening and liquid-liquid fractionation. In vivo studies of charcoal meal intestinal transit test, antidiarrheal activity against castor oil induced diarrhea and laxative activity were performed in mice. In vitro experiments were conducted upon rabbit jejunum preparations using standard tissue bath techniques. RESULTS: Phytochemical screening indicated presence of alkaloids, anthraquinones, flavonoids, saponins, steroids, tannins and phenols in At.Cr. In charcoal meal intestinal transit test, At.Cr increased (p < 0.001) intestinal motility at 100 mg/kg dose, but decreased (p < 0.001) it at 500 mg/kg dose, when compared to the control group. At.Cr (300-700 mg/kg) provided protection from castor oil induced diarrhea in mice, which was significant (p < 0.001) at 500 and 700 mg/kg doses, as compared to the saline treated control group. At.Cr (50 and 100 mg/kg) enhanced total and wet feces counts in normal mice, as compared to saline treated control. In jejunum preparations, At.Cr inhibited spontaneous, K+ (80 mM) and K+ (25 mM) mediated contractions, similar to verapamil. Pre-incubation of jejunum preparations with At.Cr resulted in rightward nonparallel shift in Ca+ 2 concentration response curves, similar to verapamil. The spasmolytic activity was concentrated in ethylacetate fraction. Aqueous fraction exhibited spasmogenicity upon spontaneous contractions, which was blocked in presence of verapamil, but remained unaffected by other tested antagonists. CONCLUSION: The Asphodelus tenuifolius crude extract possesses gut modulatory activity, which may normalize gut functions in diarrhea and constipation. The spasmolytic activity of the extract was found to be mediated through Ca+ 2 channel blocking action. The spasmogenic activity, found partitioned in aqueous fraction, possibly involves Ca+ 2 influx through voltage gated Ca+ 2 channels. The study supports ethnic uses of the plant in diarrhea and constipation.

Pharmacological validation of the folkloric uses of Cyperus rotundus L. in different ailments: An in vivo and in vitro research.

In vivo and in vitro research study was conducted on Cyperus rotundus to evaluate the sound mechanistic background in the treatment of gastrointestinal, bronchial and vascular disorders as well as in pain, emesis, pyrexia and bacterial infections. Results showed that crude extract of Cyperus rotundus (Cr.Cr) exhibited the dose-dependent spasmolytic effect in rabbit jejunum by inhibiting the spontaneous and K+ (80 mM)-induced contractions. Pretreatment of tissue with Cr. Cr caused the rightward shift of calcium concentration response curves, similar to verapamil. Cr. Cr also caused the relaxation of K+(80 mM)- and carbachol (1 µM)-induced contractions of trachea preparations, similar to that of verapamil. Moreover, Cr. Cr also relaxed the contraction induced by the K+ (80 mM) and phenylephrine (1 µM) of aorta preparations. Data show that C. rotundus possess the spasmolytic, bronchodilator and vasodilator activities possibly through calcium channels blockade; validating its folkloric use in diarrhea, dyspepsia, bronchitis, asthma and hypertension in addition to antibacterial, antiemetic, antipyretic and analgesic activities.

Antispasmodic and bronchorelaxant activities of Salsola imbricata are mediated through dual Ca+2 antagonistic and ß-adrenergic agonistic effects.

CONTEXT: Salsola imbricata Forssk. (Chenopodiaceae) has folkloric repute for the treatment of various gastrointestinal and respiratory ailments. OBJECTIVE: The present study investigates spasmolytic and bronchorelaxant effects of S. imbricata. MATERIALS AND METHODS: The crude aqueous-ethanol extract of the aerial parts of S. imbricata and its fractions, in cumulative concentrations (0.01-10 mg/mL), were tested on contractions of isolated rabbit jejunum and tracheal preparations. Furthermore, concentration response curves (CRCs) of Ca+2 and carbachol were constructed in the absence and presence of the extract. Standard organ bath methods were used. RESULTS: The crude extract relaxed spontaneous, K+ (80 mM) and carbachol (1 µM)-induced contractions in jejunum preparations with respective EC50 values of 0.40 (0.35-0.46), 0.69 (0.60-0.79) and 0.66 (0.57-0.75) mg/mL. It shifted Ca+2 CRCs rightward in nonparallel manner. In isolated tracheal preparations, the crude extract caused relaxation of K+ (80 mM) and carbachol (1 µM)-induced contractions with EC50 values of 0.86 (0.75-0.98) and 0.74 (0.66-0.84) mg/mL, respectively. It displaced carbachol CRCs rightward with suppression of maximal response. In both tissues, pretreatment with propranolol (1 µM) caused rightward shift in inhibitory CRCs of the extract against carbachol-induced contractions. The ethyl acetate fraction was found more potent in relaxing smooth muscle contractions than the parent extract and its aqueous fraction. DISCUSSION AND CONCLUSION: The results suggest that the spasmolytic and bronchorelaxant activities of S. imbricata are related to Ca+2 antagonistic and ß-adrenergic agonistic effects, thus justifying some of the traditional uses of the plant.

Pharmacological justification of use of Solena heterophylla Lour. in gastrointestinal, respiratory and vascular disorders.

BACKGROUND: Solena heterophylla Lour. has traditionally been used in the management of diseases pertaining to gastrointestinal, respiratory and vascular system and present study was undertaken to validate its traditional uses. METHODS: The aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) was tested in-vitro on isolated rabbit jejunum, tracheal and aorta preparations. The responses of tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system. RESULTS: The aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) (0.03-1.0 mg/ml) on application to spontaneous contractions in isolated rabbit jejunum preparation exerted relaxant effect through decrease in magnitude and frequency of contractions, caused relaxation of K(+)(80 mM)-induced contractions and shifted the Ca(2+) concentration response curves toward right in isolated rabbit jejunum preparations in a manner similar to verapamil (a standard Ca(2+) channel blocker), thus confirming its Ca(2+) channel blocking activity. The Sh.Cr also caused relaxation of carbachol (1 µM)- and K(+)(80 mM)-induced contractions in isolated rabbit tracheal preparations in a manner comparable to dicyclomine. CONCLUSIONS: The observed relaxant effect may be outcome of anti-muscarinic and Ca(2+) channel blocking activities. The Sh.Cr (0.03-1.0 mg/ml) against phenyephrine (1 µM)- and K(+)(80 mM)-induced contractions in isolated rabbit aortic preparations exerted a relaxant effect, possibly through Ca(2+) channel blocking activity. These findings provide a rationale for the folkloric uses of the plant in the management of ailments pertaining to gastrointestinal, respiratory and vascular system.

Validation of ethnopharmacological uses of Murraya paniculata in disorders of diarrhea, asthma and hypertension.

BACKGROUND: Murraya paniculata is traditionally used for management of gut, air way and cardiovascular disorders. The study was conducted for provision of pharmacological rationalization for folkloric uses of Murraya paniculata in gut, air way and cardiovascular problems. METHODS: Aqueous-ethanolic extract of Mp.Cr was tested using in vitro techniques on isolated tissue of rabbit (jejunum, trachea and aorta) to detect the possible presence of spasmolytic activity. The responses of tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system. RESULTS: Application of the extract of Mp.Cr relaxed spontaneous and high K(+) (80mM)-induced contraction in rabbit jejunum preparation. Because it shifted the CRCs (Calcium response curve) towards the right side so the possible blockade was of calcium channel similar to verapamil. In rabbit trachea, extract of Mp.Cr produced relaxation of carbachol and high K(+) induced contractions. When plant extract was checked further on isolated aorta for its possible vasodilator effect, it caused relaxation of phenylephrine and high K(+)-induced spastic contractions at different doses. CONCLUSION: These results indicate that Murraya paniculata shows anti-spasmodic, bronchodilator and vasodilator activity facilitated through Ca(++) antagonist mechanisms.

In-vitro and in-vivo validation of ethnopharmacological uses of methanol extract of Isodon rugosus Wall. ex Benth. (Lamiaceae).

BACKGROUND: Isodon rugosus is used in folk Pakistan traditional practices to cure ailments related to gastrointestinal, respiratory and cardiovascular problems. Present study was undertaken to validate these folkloric uses. METHODS: A crude methanol extract of the aerial parts of Isodon rugosus (Ir.Cr.) was used for both in vitro and in vivo experiments. The plant extract was tested on isolated rabbit jejunum preparations for possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract. Acetylcholinesterase and butyrylcholinesterase inhibitory activities of Ir.Cr were also determined as well as its antioxidant activity. The in vivo antiemetic activity of the extract was evaluated by using the chick emesis model, while the analgesic and antipyretic activities were conducted on albino mice. RESULTS: The application of the crude extract of I. rugosus to isolated rabbit jejunum preparations exhibited relaxant effect (0.01-0.3 mg/ml). The Ir.Cr also relaxed K+(80 m M)-induced spastic contractions in isolated rabbit jejunum preparations and shifted the Ca+2 concentration response curves towards right (0.01-0.3 mg/ml). Similarly, the extract, when applied to the isolated rabbit tracheal preparations relaxed the carbachol (1 µM)--as well as K+ (80 mM)-induced contractions in a concentration range of 0.01-1.0 mg/ml. Moreover, it also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 µM)- and K+ (80 mM)-induced contractions in isolated rabbit aorta preparations. The Ir.Cr (80 mg/kg) demonstrated antipyretic activity on pyrogen-induced pyrexia in rabbits as compared to aspirin as standard drug. The Ir.Cr also exhibited anti-oxidant as well as inhibitory effect on acetyl- and butyryl-cholinesterase and lipoxygenase (0.5 mg/ml). CONCLUSIONS: The observed relaxant effect on isolated rabbit jejunum, trachea and aorta preparations caused by Ir.Cr is possibly to be mediated through Ca+2 channel blockade and therefore may provided scientific basis to validate the folkloric uses of the plant in the management of gastrointestinal, respiratory and cardiovascular ailments. The observed antioxidant activity as well as the lipoxygenase inhibitory activity may validate its traditional use in pain and inflammations.

Review: probiotics and their beneficial effects against various diseases.

Joint FAO/WHO expert's consultation report defines probiotics as: Live microorganisms which when administered in adequate amounts confer a health benefit on the host. Most commonly used probiotics are Lactic acid bacteria (LAB) and bifidobacteria. There are other examples of species used as probiotics (certain yeasts and bacilli). Probiotic supplements are popular now a days. From the beginning of 2000, research on probiotics has increased remarkably. Probiotics are now day's widely studied for their beneficial effects in treatment of many prevailing diseases. Here we reviewed the beneficiary effects of probiotics in some diseases.

Risk for oral cancer from smokeless tobacco.

Tobacco products which are used in a way other than smoking are known as smokeless tobacco. The most common smokeless tobaccos are chewing tobacco, naswar, snuff, snus, gutka, and topical tobacco paste. Any product which contains tobacco is not safe for human health. There are more than twenty-five compounds in smokeless tobacco which have cancer causing activity. Use of smokeless tobacco has been linked with risk of oral cancer. Smokeless tobacco contains tobacco-specific nitrosamines (TSNAs), polonium, formaldehyde, cadmium, lead, and benzo[a]pyrene, which are carcinogenic agents. Although there is presence of some compounds, carotenoids and phenolic compounds, that have cancer inhibiting properties, they are in low concentrations. Dry snuff use is linked with higher relative risks, while the use of other smokeless tobacco is of intermediate risk. Moist snuff and chewing tobacco have a very low risk for oral cancer. Therefore, from this review article, it was concluded that smokeless tobacco has risk for oral cancer - either low, medium or high depending on the balance between cancer causing agents and cancer inhibiting agents.

Spasmolytic, bronchodilator and vasorelaxant activity of methanolic extract of Tephrosia purpurea.

The methanolic extract of the whole plant of Tephrosia pupurea, Linn. was subjected to find out its possible therapeutic utility to validate its folkloric use in native systems of medicine. The extract on application to spontaneous contractions in isolated rabbit jejunum preparations exerted a concentration dependent (0.003-3.0 mg/mL) relaxant effect. The extract also caused concentration dependent relaxation of K+(80 mM)-induced spastic contractions. These findings were further supported by the observations that the extract caused a concentration dependent right ward shift of the Ca2+ response curves in manner similar to that of verapamil. The extract exhibited a relaxant effect on carbachol and high K+ (80 mM)-induced contractions of isolated rabbit tracheal preparations in a manner similar to verapamil. The observed non-specific bronchodilator response is possibly mediated through Ca2+ channel blockade. Moreover, the extract also exhibited a dose dependent relaxant effect on phenylephrine (1 microM) and K+(80 mM)-induced contractions in a manner similar to verapamil. On the basis of the above-mentioned findings, it can be concluded that the use of Tephrosia purpurea, in gastrointestinal spasm, asthma and hypertension is likely to be mediated through calcium channel blockage.

Tuberculosis: burning issues: multidrug resistance and HIV-coinfection.

Tuberculosis is an infection of respiratory tract and Mycobacterium tuberculosis is the causative agent. Multidrug resistance and HIV-coinfection are the burning issues for tuberculosis. The management of drug resistance to tuberculosis is the necessity of the day so by taking effective and controlled measures and giving high doses of 2nd line drugs, we can minimize the death rate in TB. For the HIV-related TB infection, it is necessary to treat TB infection first so that effectiveness of antiretroviral therapy may not be altered and the transmission of M. tuberculosis to other healthy individuals of community could be prevented. All HIV positive individuals who are at a greater risk of acquiring TB infection, either due to suppressed immune system or unhealthy circumstances, must be investigated and if indicated must be treated effectively at immediate basis so that latent TB infection may not progress to active TB.

Pharmacological Evaluation of Prosopis cineraria (L.) Druce in Gastrointestinal, Respiratory, and Vascular Disorders.

In this paper, a crude methanolic extract from the stem bark of Prosopis cineraria, a plant native of Pakistan, was tested for its possible presence of spasmolytic, bronchodilator, and vasodilator activities in an attempt to validate some of its folkloric uses. Moreover, attempts were made to provide plausible explanations of the observed biological activities. The extract caused relaxation of the spontaneous as well as K(+) (80 mM)-induced contractions at tissue bath concentrations of 3-10 mg/mL in isolated rabbit jejunum preparations, probably mediated through blockade of Ca(+2) channels. This finding was further confirmed by the shifting of the Ca(+2) concentration response curves to the rightward in a manner similar to verapamil used as a standard Ca(+2) channel blocker. The extract also exhibited nonspecific relaxant effect on carbachol (1 µM)- and K(+) (80 mM)-induced contractions in isolated rabbit tracheal preparations. The same effect was recorded for phenylephrine (11 µM) and K(+) (80 mM)-induced contractions in isolated rabbit aortic preparations in a manner similar to verapamil. These observations confirm that observed bronchodilator and vasodilator activities were possibly mediated through blockade of Ca(+2) channels. The above-mentioned observations validate the traditional use of the plant in the treatment of respiratory and gastrointestinal ailments.

Spasmolytic, bronchodilatory and antioxidant activities of Erythrina superosa Roxb.

The present study was undertaken to explore the possible antioxidant, spasmolytic, bronchodilator and antioxidant activities of Erythrina suberosa Roxb. flowers. The crude aqueous methanolic extract of Erythrina suberosa Roxb. flowers (Es.Cr), on application to isolated rabbit jejunum preparations, caused concentration dependent relaxation of the spontaneous contractions as well as inhibition of K(+) (80 mM)-induced contractions, suggested that Es.Cr exhibited spasmolytic activity may possibly be mediated through Ca(2+) channel blocking effect. This was confirmed further as Es.Cr treatment of the isolated rabbit jejunum preparations resulted in a rightward shift in the Ca(2+) concentration-response curves in a manner similar to verapamil, a standard calcium channel blocker. Similarly, Es.Cr on application to isolated rabbit tracheal preparations; caused the concentration dependent relaxation of the carbachol (1 microM) and K(+) (80 mM)-induced contractions indicating its bronchodilator activity in a manner similar to verapamil. The crude methanolic extract of Erythrina suberosa exhibited antioxidant activity as manifested by strong scavenging activity on DPPH free radicals, whereas weaker scavenging activity was shown on NO free radicals in comparison with standard antioxidant quercetin, which is equally potent against both free radicals. It is concluded from this study that the crude aqueous methanolic extract of the flowers of Erythrina suberosa Roxb. possesses the antioxidant, spasmolytic and bronchodilator activities likely to be mediated through Ca(2+) channel blocking mechanism.

Analgesic effect of ketamine and morphine after tonsillectomy in children.

A comparative double blind study of Ketamine and Morphine was conducted on eighty children following tonsillectomy to assess the analgesic, respiratory rate depressant and emesis. Children (6-12 years) were divided into two groups randomly (n=40). General anesthesia was induced followed by 0.1mg/kg morphine (I/M) and 0.5mg/kg ketamine (I/M) to Group I and Group II respectively before the initiation of surgical procedure. Pain scores (face score and CHEOPS score) were estimated for children at thirty, sixty, one hundred and twenty and two hundred and forty minutes following surgery. Comparison of CHEOPS score estimation reflected that pain scores were statistically significant (P < 0.05) in Group I receiving Morphine as compared to Group II who received Ketamine. The analgesic effect of ketamine and morphine showed statistically insignificant results (P >0.05) in case of face score. Moreover, respiratory rate in Group I had shown statistical association (p<0.05) as compared to the ketamine at 60 and 120 minutes. Furthermore, incidence of vomiting was more in Group I (0.05) as compared to Group II. It can be concluded from the study that ketamine may be used as a suitable substitute to that of morphine in children undergoing tonsillectomy.

Novel drugs from marine microorganisms.

Marine microorganisms have expected mounting consideration on the basis of bioactive metabolites and propose an exclusive prospect to both enhance the amount of aquatic natural foodstuffs in clinical trials as well as speed up their progress. This review focuses particularly on those molecules, originated from marine microorganisms, presently in the medical pipeline that have been recognized or highly expected to be identified based on growing incidental evidence. Particularly karlotoxin class compounds, isolated from dinoflagellate Karlodinium veneficum, offer chances to create new molecules for control of cancer and high serum cholesterol levels.

Ethnopharmacological basis for folkloric claims of Anagallis arvensis Linn. (Scarlet Pimpernel) as prokinetic, spasmolytic and hypotensive in province of Punjab, Pakistan.

ETHNOPHARMACOLOGICAL RELEVANCE: The conventional naturopaths of Punjab Province (Pakistan) have trivial usage of Anagallis arvensis Linn.(Primulaceae) for cure of diarrhea, constipation, asthma as well as hypertension. AIM: Present research was focused to discover comprehensive mechanism of spasmogenic, spasmolytic, bronchorelaxant and hypotensive folkloric usage of Anagallis arvensis Linn.. METHODOLOGY: The crude extract of Anagallis arvensis Linn. (Aa.Cr) & its (aqueous & organic) portions tested in-vitro on isolated jejunum, ileum, trachea, aorta, paired atria preparations as well as in-vivo in mice & normotensive anaesthetized rats. The responses have been noted by transducers (isotonic & isometric) coupled to Power Lab. RESULT: Anagallis arvensis Linn. (Aa.Cr; crude aqueous-alcoholic extract) produced contractile action at low concentrations but relaxant action was observed by increasing concentrations on spontaneous contractions of isolated jejunum of rabbit. But, pre-treatment of tissue with atropine prior extract caused suppression of contractile effect indicating presence of cholinergic muscarinic response of Aa.Cr. It also triggered relaxation of high Potassium -stimulated contractions of jejunum with subsequent non-parallel right move in Ca++ CRCs. Moreover, Aa.Cr relaxed carbachol - & high Potassium - stimulated contractions in trachea of rabbit but observed relaxant effect was powerful against CCh (1 µM)- stimulated contractions with rightside parallel move of CCh-curves succeeded by non-parallel move, like Dicyclomine, having dual activities. The Aa.Cr also showed relaxant result on Phenylephrine and High Potassium -prompted contractions in endothelium intact aorta. The fractionation revealed segregations of contractile & relaxant effects in relevant aqueous & organic portions. The Intravenous administration of Aa.Cr to ketamine-diazepam anaesthetized normo-tensive albino rats resulted in decreased MABP, SBP & DBP. The Aa.Cr applied negative (-) inotropic & chronotropic action on paired atria. The Aa.Cr also exhibited anti-diarrheal action in mice against castor oil prompted diarrhea and also mitigated distance covered by charcoal meal in gastrointestinal tract in a manner comparable with loperamide. CONCLUSION: These results revealed presence of CCB and selective muscarinic agonist activity in Aa.Cr, hence validating folkloric practice of Anagallis arvensis Linn. in diarrhea, constipation, asthma & hypertension.

Antiplatelet Aggregation, Cardiotonic, Anti-Inflammatory, Antioxidant, and Calcium Channel Antagonistic Potentials of Nepeta ruderalis Buch.

The objective of this study was to authenticate the ethnobotanical claims of the Nepeta ruderalis Buch.-Ham. (N. ruderalis) extract in the traditional system of medicine. Crude extract was prepared via a simple maceration process. DPPH free radical scavenging and carrageenan-induced rat paw edema models were used to monitor antioxidant and anti-inflammatory responses of the N. ruderalis extract. Furthermore, it was tested for antiplatelet aggregation, cardioprotective, and calcium channel antagonistic activities via standard documented protocols. The N. ruderalis extract exhibited 80.82% antioxidant activity (IC50 = 207.51 ± 4.36 µg) while the anti-inflammatory response was significant (p < 0.05 to p < 0.01) at 50 mg/kg (45.58%) and 100 mg/kg (60.90%) doses. Moreover, it was found to inhibit platelet aggregation (IC50 = 1.06 and 0.91 mg/mL) and, in addition, to increase the force of contraction at the concentration of 3.0-10 mg/mL with a decrease in the heart rate on isolated paired atria (EC50 = 11.78 mg/mL). Relaxant activity was observed on the isolated rabbit jejunum (EC50 = 0.96 mg/mL) and trachea (EC50 = 0.89 mg/mL). However, in a cumulative way, an 80-millimolar potassium-induced contraction was evaluated (EC50 = 1.31 mg/mL). The N. ruderalis extract exhibited antioxidant, anti-inflammatory, platelet aggregating, cardiotonic, and calcium channel antagonistic activities, therefore proving scientifically its effectiveness in the traditional system of medicine.

Ethnopharmacological studies on antispasmodic and antiplatelet activities of Ficus carica.

ETHNOPHARMACOLOGICAL RELEVANCE: The ripe dried fruit of Ficus carica Linn. (Moraceae) commonly known as "Fig" has medicinal value in traditional system of medicine for its use in gastrointestinal and inflammatory disorders. AIM OF THE STUDY: To rationalize the medicinal use of Fig (Ficus carica) in gastrointestinal and inflammatory disorders. MATERIALS AND METHODS: The aqueous-ethanolic extract of Ficus carica (Fc.Cr) was studied for antispasmodic effect on the isolated rabbit jejunum preparations and for antiplatelet effect using ex vivo model of human platelets. RESULTS: Fc.Cr tested positive for alkaloids, flavonoids, coumarins, saponins, sterols and terpenes. When tested in isolated rabbit jejunum, Fc.Cr (0.1-3.0mg/mL) produced relaxation of spontaneous and low K(+) (25 mM)-induced contractions with negligible effect on high K(+) (80 mM) similar to that caused by cromakalim. Pretreatment of the tissue with glibenclamide caused rightward shift in the curves of low K(+)-induced contractions. Similarly, cromakalim inhibited the contractions induced by low K(+), but not of high K(+), while verapamil equally inhibited the contractions of K(+) at both concentrations. Fc.Cr (0.6 and 0.12 mg/mL) inhibited the adenosine 5'-diphosphate and adrenaline-induced human platelet aggregation. CONCLUSION: This study showed the presence of spasmolytic activity in the ripe dried fruit of Ficus carica possibly mediated through the activation of K(+)(ATP) channels along with antiplatelet activity which provides sound pharmacological basis for its medicinal use in the gut motility and inflammatory disorders.