Qaiser Jabeen

Ethnopharmacological evaluation of the anticonvulsant, sedative and antispasmodic activities of Lavandula stoechas L.

Lavandula stoechas L. (Lamiaceae) has been used for a long time in traditional medicine as an anticonvulsant and antispasmodic. The aqueous-methanolic extract of L. stoechas flowers (LS) was studied for its possible anticonvulsant and antispasmodic activities. When tested in mice, LS (600 mg/kg) significantly reduced the severity and increased the latency of convulsions induced by pentylene tetrazole (PTZ). LS likewise reduced PTZs lethality. LS up to a dose of 600 mg/kg was found devoid of any hypnotic effect in mice, however, animals were found to be dull, calm and relaxed. The sedative effect of the plant extract was confirmed, as it prolonged the pentobarbital sleeping time in mice similar to that of diazepam. In isolated rabbit jejunum preparations, LS caused a dose-dependent (0.1-1.0 mg/ml) relaxation of spontaneous contractions. LS also inhibited K(+)-induced contractions in a similar dose range, thereby suggesting calcium channel blockade. This effect was confirmed when pretreatment of the jejunum preparation with LS produced a dose-dependent shift of the Ca(2+) dose-response curve to the right, similar to the effect of verapamil, a standard calcium channel blocker. These data indicate that the plant extract exhibits anticonvulsant and antispasmodic activities. Its calcium channel blocking property may be mechanistically related to these activities. Its usefulness in folk medicine appears thus to be based on a sound mechanistic background.

Coriander fruit exhibits gut modulatory, blood pressure lowering and diuretic activities

AIM OF THE STUDY Coriander (Coriandrum sativum) is traditionally used for various gastrointestinal and cardiovascular disorders and this study was designed to rationalize its use in dyspepsia, abdominal colic, diarrhea, hypertension and as diuretic. MATERIALS AND METHODS Coriander crude extract (Cs.Cr) was evaluated through in vitro and in vivo techniques. RESULTS Cs.Cr caused atropine sensitive stimulatory effect in isolated guinea-pig ileum (0.1-10 mg/ml). In rabbit jejunum preparations, Cs.Cr evoked a similar contractile response but in the presence of atropine, it exhibited relaxation against both spontaneous and high K(+) (80 mM)-induced contractions as well as shifted the Ca(2+) concentration-response curves to right, similar to that caused by verapamil. Cs.Cr (1-30 mg/ml) caused fall in arterial blood pressure of anesthetized animals, partially blocked by atropine. Cs.Cr produced vasodilatation against phenylephrine and K(+) (80 mM)-induced contractions in rabbit aorta and cardio-depressant effect in guinea-pig atria. Cs.Cr produced diuresis in rats at 1-10mg/kg. Bio-assay-directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively. CONCLUSIONS These results indicate that coriander fruit exhibits gut stimulatory, inhibitory and hypotensive effects mediating possibly through cholinergic, Ca(2+) antagonist and the combination of these mechanisms respectively. Diuretic activity adds value to its use in hypertension.

Blood pressure lowering effect of olive is mediated through calcium channel blockade

Olive (Olea europea) is used in traditional medicine as a remedy for hypertension. The aqueous–methanolic crude extract of O. europea fruit (OeF.Cr) was studied in anaesthetized rats and its possible mechanism was elucidated using isolated cardiovascular preparations. Intravenous administration of OeF.Cr produced a dose-dependent (30–100 mg/kg) fall in arterial blood pressure in normotensive anaesthetized rats. This effect remained unaltered in atropinized animals. In the in vitro studies OeF.Cr (0.1–3.0 mg/ml) inhibited spontaneously beating guinea-pig atria. Moreover, it relaxed K+ and/or phenylephrine-induced contractions of rabbit aortic preparations over a dose range of 0.1–3.0 mg/ml, suggesting calcium channel blockade (CCB). The CCB effect was confirmed when pretreatment of the vascular preparations with OeF.Cr produced a dose-dependent rightward shift of the Ca2 +  dose–response curves, similar to verapamil. These results suggest that the blood pressure lowering effect of olive is mediated through CCB, justifying its use in hypertension.

Interdependent and independent multidimensional role of tumor microenvironment on hepatocellular carcinoma

HighlightsRole of tumor microenvironment on hepatocellular carcinoma is discussed.Detailed summary of implicated cytokines with related pathways is presented.Recent studies on the topic are analysed. Abstract The novelty of an effective therapeutic targeting for hepatocellular carcinoma (HCC) is based on improved understanding of each component of tumor microenvironment (TME) and its correspondent interactions at biological and molecular levels. In this context, new expansions for the treatment against TME and its communication with HCC are under exploration. Despite of the fact that blockage of growth factor receptors has become a treatment of choice in late phases of HCC in clinical practice, still a precise targeted treatment should address all the components of TME. Targeting one specific element out of cellular (cancer associated fibroblasts, endothelial cells, hepatic stellate cells, Kupffer cells and lymphocytes) or non‐cellular (extracellular matrix, growth factors, inflammatory cytokines, proteolytic enzymes) parts of TME may not be a successful remedy for the disease because of well‐designed hindrances of each component and their functional alternativeness. Meanwhile there are some elements of TME like epithelial‐mesenchymal transition and CAF, which are considerably important and need thorough investigations. Ascertaining the potential role of these elements, and a single or combinational drug therapy targeting these elements of TME simultaneously, may provide the appreciable considerations to eventually improve in clinical practices and may also minimize the chances of reoccurrence of HCC.

Anti-diabetic and spasmolytic potential of Farsetia hamiltonii Royle from Cholistan desert.

ETHNOPHARMACOLOGICAL RELEVANCE Folk herbal practitioners of the Cholistan desert claim Farsetia hamiltonii Royle (Brassicaceae) to treat diabetes, oxidative damages, diarrhea, fever, and abdominal cramps. The aim of this study was to scientifically find the potential of Farsetia hamiltonii in treating diabetes and gastrointestinal diseases. MATERIALS AND METHODS In vivo anti-diabetic activity of Farsetia hamiltonii was studied on alloxan induced diabetic rats to justify its traditional use. The in vitro antispasmodic activity on isolated tissues of rabbit jejunum was also evaluated. In addition, several enzyme inhibition studies (lipoxygenase, tyrosinase, acetylcholinesterase (AchE), carbonic II anhydrase and phosphodiesterase I) and antioxidant activity of plant extracts were also conducted. RESULTS In vivo experiments, Farsetia hamiltonii methanol extract (300 mg/kg) significantly lowered the fasting blood glucose (107.6 ± 1.249 mg/dL up to 4th day) comparable to positive control (Glibenclamide) throughout the study period. The in vitro antispasmodic activity on isolated tissues of rabbit jejunum on methanol extract showed concentration dependent (0.01-0.3 mg/ml) relaxation of spontaneous contractions with EC₅₀ value 0.011 µM and high K(+) (80 mM) induced contraction (0.01-0.1 mg/ml) with EC₅₀ value 0.066 mg/ml. Farsetia hamiltonii DCM and methanol extracts exhibited some antilipoxygenase activities while tyrosinase, acetylcholinesterase (AchE), carbonic II anhydrase, phosphodiesterase I, and antioxidant activity of plant extracts were not significant. CONCLUSIONS Our results validate the traditional use of Farsetia hamiltonii for the traditional therapeutic potential in treating diabetes and gastrointestinal diseases.

Immunostimulant activities of the aqueous methanolic extract of Leptadenia pyrotechnica, a plant from Cholistan desert

ETHNOPHARMACOLOGICAL RELEVANCE Leptadenia pyrotechnica (Forssk.) Decne (Asclepiadaceae) is a well-renowned medicinal shrub, used by herbal practitioners for various ailments including allergic rhinitis, productive cough, abortion, diabetes, stomach disorders, fever, kidney disorders, stones and cancer AIM OF THE STUDY On the basis of folkloric uses, L. pyrotechnica was selected from the wide medicinal flora of the Cholistan desert of Pakistan, for the exploration of immunomodulatory potential. MATERIALS AND METHODS Aqueous methanolic (30:70) extract of aerial parts of L. pyrotechnica (Lp. Cr) was prepared by 3 days thrice maceration and subsequent evaporation under reduced pressure. In-vivo experiments were performed in Wistar albino rats including neutrophil adhesion test, haemagglutinating antibody (HA) titre, delayed-type hypersensitivity response, phagocytic activity and cyclophosphamide-induced myelosuppression. RESULTS Lp. Cr produced a significant increase in phagocytic index in dose-dependent fashion (3.56, 4.18 and 5.42 at 30, 100 and 300mg/kg, respectively) as well as an augmented response in the delayed-type hypersensitivity reaction and HA titre induced by sheep erythrocytes. Lp. Cr also showed improved adhesion of neutrophils with nylon pellets (15.28, 27.85 and 38.42% at the doses of 30, 100 and 300mg/kg) and prevented myelosuppression in cyclophosphamide-treated rats as evidenced from the hematological parameters. The results of treatment were compared with normal and standard control groups throughout the study and the effects by Lp. Cr (300mg/kg) were found to be comparable with Levamisole. CONCLUSIONS The results indicated that L. pyrotechnica possesses immunostimulatory activity and justify its traditional use for the control and management of diseases in which the immune system needs to be stimulated like infectious diseases.

Evaluation of prunes for hypotensive, angiotensin converting enzyme (ACE) inhibitory and diuretic activities in rats

Prunes are dried fruits of several species of Prunus, including that of Prunus domestica Linn (Rosaceae) and are used for the treatment of hypertension in traditional systems of medicine in India and Pakistan. We investigated the blood pressure lowering, angiotensin converting enzyme (ACE) inhibitory and diuretic activities of the aqueous-methanolic crude extract of dried fruits of P. domestica (Pd.Cr.) in rats. Intravenous administration of the Pd Cr decreased mean arterial blood pressure, systolic blood pressure (SBP) and diastolic blood pressure (DBP) of the ketamine-diazepam anesthetized normotensive rats dose-dependently, at the dose range of 1 to 30 mg/kg. In vitro, the extract was fond to have serum ACE inhibitory activity, with IC50 value of 1.102 mg/ml. The extract did not increase urine output in rats. The study concludes that the crude extract of prunes has hypotensive and ACE inhibitory activities, which provides scientific justification for its traditional uses as cardioprotective and antihypertensive remedy.