Studies on antihypertensive and antispasmodic activities of Andropogon muricatus Retz.This article is one of a selection of papers published in this special issue (part 1 of 2) on the Safety and Efficacy of Natural Health Products.

2007 ◽  
Vol 85 (9) ◽  
pp. 911-917 ◽  
Author(s):  
Anwar H. Gilani ◽  
Abdul J. Shah ◽  
Khalid H. Janbaz ◽  
Shahida P. Ahmed ◽  
Muhammad N. Ghayur
Keyword(s):  
Calcium Channel ◽  
Rabbit Aorta ◽  
Natural Health Products ◽  
Response Curves ◽  
Medicinal Uses ◽  
Health Products ◽  
Rabbit Jejunum ◽  
The Right

The aqueous-methanolic crude extract of Andropogon muricatus (Am.Cr) was investigated pharmacologically to determine some of its medicinal uses in cardiovascular and gastrointestinal disorders. A series of in vivo and in vitro studies were conducted to evaluate dose-dependent effects of Am.Cr on mean arterial pressure (MAP), cardiac and vascular contractions, and to further investigate the potential mechanism of action. Intravenous administration of Am.Cr (10–50 mg/kg) caused a fall (18%–56%) in MAP in normotensive rats under anesthesia. When tested in isolated guinea pig atria, Am.Cr (0.03–5.0 mg/mL) exhibited a cardiodepressant effect on the rate and force of spontaneous contractions. In isolated rabbit aorta, Am.Cr caused inhibition of K+ (80 mmol/L)-induced contractions at a lower concentration than of phenylephrine. In isolated rabbit jejunum preparations, Am.Cr (0.01–0.10 mg/mL) caused relaxation of spontaneous and high K+ (80 mmol/L)-induced contractions, suggesting that the spasmolytic effect is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pretreatment of the tissue with Am.Cr (0.03–0.1 mg/mL) shifted the Ca2+ dose–response curves to the right, similar to that caused by verapamil. These data indicate that the blood pressure-lowering and spasmolytic effects of Am.Cr are mediated possibly through a calcium channel blocking activity. Phytochemical screening of Am.Cr revealed the presence of phenols, saponins, tannins, and terpenes, which may be responsible for the observed vasodilator, cardiodepressant, and antispasmodic activities. This study shows potential with respect to its medicinal use in cardiovascular and gut disorders.

scholarly journals Pharmacologically mechanistic basis for the traditional uses of Rumex acetosa in gut motility disorders and emesis

2015 ◽  
Vol 10 (3) ◽  
pp. 548 ◽  
Author(s):  
Musaddique Hussain ◽  
Shahid Masood Raza ◽  
Khalid Hussain Janbaz
Keyword(s):  
Rumex Acetosa ◽  
Response Curves ◽  
Motility Disorders ◽  
Traditional Uses ◽  
Antiemetic Activity ◽  
Rabbit Jejunum ◽  
Mechanistic Basis ◽  
The Right

<p class="Abstract"><em>In vitro</em> and<em> in vivo</em> studies were undertaken to evaluate the pharmacologically mechanistic background to validate the traditional uses of <em>Rumex acetosa</em> in the treatment of emesis and gastrointestinal motility disorders such as constipation and diarrhea. In rabbit jejunum preparation, methanolic extract of <em>R. acetosa</em> (0.01-1.0 mg/mL) caused a transient spasmogenic effect, followed by the spasmolytic effect (3-10 mg/mL). In presence of atropine, spasmogenic effect was blocked while spasmolytic effect was emerged, suggesting that spasmogenic effect was mediated through activation of muscarinic receptors. Extract inhibited the K<sup>+ </sup>(80 mM)-induced contraction, suggesting Ca<sup>2+</sup>-cha-nnel blockade, which was further confirmed when pretreatment of tissue with extract shifted the Ca<sup>2+ </sup>concentration-response curves to the right, similarly as verapamil.<em> R. acetosa</em> also exhibited the significant antiemetic activity (p&lt;0.05) against different emetogenic stimuli, when compared with chlorpromazine. This study confirms the presence of gut modulator (spasmogenic and spasmolytic) and antiemetic activates, validating its traditional uses.</p><p> </p>

scholarly journals Delphinidin and Its Glycosides’ War on Cancer: Preclinical Perspectives

2021 ◽  
Vol 22 (21) ◽  
pp. 11500
Author(s):  
Anshul Sharma ◽  
Hyo-Kyoung Choi ◽  
Yeon-Kye Kim ◽  
Hae-Jeung Lee
Keyword(s):  
Molecular Mechanisms ◽  
Future Research ◽  
Natural Health Products ◽  
Cell Protection ◽  
Anticancer Properties ◽  
Dietary Antioxidant ◽  
Health Products ◽  
Antioxidant Supplements

Until now, several studies have looked at the issue of anthocyanin and cancer, namely the preventive and inhibitory effects of anthocyanins, as well as the underlying molecular processes. However, no targeted review is available regarding the anticarcinogenic effects of delphinidin and its glycosides on various cancers and their plausible molecular mechanisms. Considerable evidence shows significant anticancer properties of delphinidin-rich preparations and delphinidin alone both in vitro and in vivo. This review covers the in vitro and preclinical implications of delphinidin-mediated cell protection and cancer prevention; thus, we strongly recommend that delphinidin-rich preparations be further investigated as potential functional food, dietary antioxidant supplements, and natural health products targeting specific chronic diseases, including cancer. In addition to in vitro investigations, future research should focus on more animal and human studies to determine the true potential of delphinidin.

XP-828L (Dermylex), a new whey protein extract with potential benefit for mild to moderate psoriasisThis article is one of a selection of papers published in this special issue (part 1 of 2) on the Safety and Efficacy of Natural Health Products.

2007 ◽  
Vol 85 (9) ◽  
pp. 943-951 ◽  
Author(s):  
Réjean Drouin ◽  
Éric Lamiot ◽  
Kim Cantin ◽  
Sylvie F. Gauthier ◽  
Yves Pouliot ◽  
...  
Keyword(s):  
Whey Protein ◽  
Mechanism Of Action ◽  
Natural Health Products ◽  
Concomitant Treatment ◽  
Natural Health ◽  
Protein Extract ◽  
Murine Splenocytes ◽  
Health Products

Natural health products (NHPs) or complementary and alternative medicine (CAM) are commonly used to prevent disorders or support the usual treatments of many diseases. XP-828L, a whey protein extract, has demonstrated potential benefits for the treatment of mild to moderate psoriasis. The aim of this study was to analyze further clinical data that demonstrated the clinical benefits and safety of the XP-828L in patients with psoriasis and the potential mechanism of action of this product in vitro. Oral administration (2.5 g, twice a day, over 112 days) of XP-828L in 42 human subjects with mild to moderate psoriasis improved their PGA scores (physician’s global assessment). Moreover, no significant changes in haematology or hepatic and renal parameters were observed throughout the study period, indicating the safety of the product. In vitro experiments showed that XP-828L decreased the proliferation of concanavalin A (ConA)-stimulated murine splenocytes and their production of interleukin (IL)-2 and interferon (IFN)-γ. Although the in vivo mechanism of action of XP-828L remains unknown, XP-828L represents an NHP to be used as an alternative or concomitant treatment for mild to moderate psoriasis and potentially for other immune-mediated diseases.

ANG II- and TxA2-induced mesenteric vasoconstriction in rats is mediated by separate cell signaling pathways

1999 ◽  
Vol 277 (1) ◽  
pp. H1-H7 ◽  
Author(s):  
Johannes Bauer ◽  
Cécile Dau ◽  
Alessandro Cavarape ◽  
Franz Schaefer ◽  
Heimo Ehmke ◽  
...  
Keyword(s):  
Signaling Pathways ◽  
Dose Response ◽  
Ang Ii ◽  
Response Curves ◽  
Intracellular Ca ◽  
The Right ◽  
Activate Protein Kinase ◽  
Cell Signaling Pathways

Studies in vitro have demonstrated that vasoconstrictor agents increase intracellular Ca2+ and activate protein kinase C (PKC) to elevate vascular tone. The aim of the present study was to determine the importance of these signaling pathways for angiotensin II (ANG II) and thromboxane A2(TxA2) in regulating mesenteric blood flow (MBF) in vivo. In anesthetized rats increasing doses of ANG II or the TxA2 agonist U-46619 were administered into the superior mesenteric artery to reduce MBF. Intra-arterial infusion of inhibitors served to examine the contribution of different pathways: 8-(diethylamino)octyl 3,4,5-trimethoxybenoate hydrochloride (TMB-8) to inhibit intracellular Ca2+ release, nifedipine to block transmembrane Ca2+ influx through the L-type Ca2+ channel, and staurosporine to inhibit PKC. Each of the inhibitors attenuated ANG II-induced reductions in MBF, and all dose-response curves were shifted to the right to an approximately threefold higher ANG II dose. Combinations of the inhibitors revealed that their effects were additive; together they abolished the vasoconstrictor action of ANG II completely. In contrast, the dose-response curve for U-46619 was not affected by any of the inhibitors infused either separately or together. The results demonstrate that a rise in intracellular Ca2+ and activation of PKC are major mediators of the vasoconstrictor effect of ANG II in mesenteric circulation, but they play a subordinate role, if any, for the effects of TxA2. Because TxA2 plays a major role only under pathological conditions, the uncontrolled vasoconstriction appears to be associated with the recruitment of novel signal transduction pathways.

Measuring the effect of avermectins and milbemycins on somatic muscle contraction of adult Haemonchus contortus and on motility of Ostertagia circumcincta in vitro

Parasitology ◽  
2014 ◽  
Vol 141 (7) ◽  
pp. 948-956 ◽  
Author(s):  
JANINA DEMELER ◽  
GEORG VON SAMSON-HIMMELSTJERNA ◽  
NICHOLAS C. SANGSTER
Keyword(s):  
Muscle Contraction ◽  
Haemonchus Contortus ◽  
Anthelmintic Resistance ◽  
Parasitic Nematodes ◽  
Response Curves ◽  
Drug Potency ◽  
The Right ◽  
Sites Of Action

SUMMARYThe mechanism of anthelmintic resistance against the widely used macrocyclic lactones (MLs) is still not fully understood. Pharyngeal, somatic body muscles and the ovijector have been proposed as putative sites of action as well as resistance. In the present study the effects of three avermectins and three milbemycins on adult parasitic nematodes were evaluated in vitro. The Muscle Transducer system was used to investigate the effects of MLs on muscle contraction in female Haemonchus contortus and effects on motility were measured in Ostertagia (Teladorsagia) circumcincta using the Micromotility Meter. Concentration-response curves for all substances in both systems shifted to the right in the resistant isolates. Resistance was present to ivermectin (IVM) and its components IVM B1a and IVM B1b, suggesting that both components are involved in the mode of action and resistance. No consistent patterns of potency and resistance of the substances were observed except that milbemycins generally showed lower resistance ratios (RRs) than IVM. IVM and IVM B1b were the most potent inhibitors of contraction and motility in both susceptible isolates and also showed the highest RR in both species. Low RRs for milbemycins recorded in vitro for highly resistant isolates in vivo suggest that other factors such as pharmacokinetics influence drug potency in vivo.

Reduction of intrinsic sinoatrial frequency and norepinephrine response of the exercised rat

1977 ◽  
Vol 55 (4) ◽  
pp. 813-820 ◽  
Author(s):  
Richard L. Hughson ◽  
John R. Sutton ◽  
J. Desmond Fitzgerald ◽  
Norman L. Jones
Keyword(s):  
Sinoatrial Node ◽  
Parasympathetic Nervous System ◽  
Control Group ◽  
Response Curves ◽  
Chronotropic Response ◽  
In Vitro Measurements ◽  
The Right

Physical training is associated with a reduction of intrinsic sinoatrial activity; the present study examined the role of the parasympathetic nervous system in this reduction. Six groups of rats were studied for 10 weeks: inactive control; treadmill exercised; parasympathetic receptor blockade with atropine; exercise plus atropine; parasympathetic receptor stimulation with carbachol; and exercise plus carbachol. In vivo ISF (cardiac frequency 20 min after injection of propranolol and atropine) was measured at 3-week intervals. At the end of 10 weeks the right atrium was excised, in vitro measurements were made of ISF, and chronotropic dose–response curves to acetylcholine and norepinephrine were established. In vivo, ISF was reduced with time, the greatest reduction being found in the exercise plus atropine group; the treadmill-exercised and the atropine-treated groups also had a greater reduction than the control group. In vitro, no differences were observed in acetylcholine responses. The maximum norepinephrine chronotropic response was reduced in the treadmill-exercised and the exercise plus atropine groups. The maximum norepinephrine-induced frequency correlated with the in vitro ISF (r = 0.75). Thus, ISF was reduced with training, but this effect was independent of parasympathetic activity. The properties of the sinoatrial node which set ISF also influenced the maximum norepinephrine response.

Endothelium-dependent vasorelaxation evoked by desmopressin and involvement of nitric oxide in rat aorta

1993 ◽  
Vol 264 (2) ◽  
pp. E203-E207 ◽  
Author(s):  
K. Yamada ◽  
M. Nakayama ◽  
H. Nakano ◽  
N. Mimura ◽  
S. Yoshida
Keyword(s):  
Nitric Oxide ◽  
Specific Inhibitor ◽  
Rat Aorta ◽  
Receptor Antagonists ◽  
Response Curves ◽  
V2 Vasopressin Receptor ◽  
In Vitro Effects ◽  
The Right

It is known that in vivo administration of desmopressin (DDAVP; a selective V2-vasopressin receptor agonist) results in prostacyclin-independent vasodilation. The in vitro effects of DDAVP and its mechanisms were examined using rat aortic strips. DDAVP from a concentration of 1 x 10(-9) M caused a concentration-dependent relaxation of the aorta precontracted with norepinephrine (10(-7) M) with intact endothelium. However, no relaxation was induced in aorta with the endothelium removed. The DDAVP-induced relaxation was not influenced by the presence of indomethacin but was inhibited by L-NG-monomethyl-L-arginine (L-NMMA), a specific inhibitor of nitric oxide (NO) synthesis. The inhibition by L-NMMA was reversed by the addition of L-arginine but not D-arginine. Further, the endothelium-dependent relaxation due to DDAVP was potentiated by superoxide dismutase, a scavenger of superoxide anions, and was inhibited by hemoglobin. DDAVP induced an increase in guanosine 3',5'-cyclic monophosphate levels in the aorta with endothelium but not in aorta without endothelium, and this was suppressed by L-NMMA and hemoglobin. The suppression by L-NMMA was also partially reversed by L-arginine but not by D-arginine. Two selective V2-receptor antagonists had no effect on the DDAVP-induced vasorelaxation. Selective V1-receptor antagonists (a peptidic and a nonpeptidic) caused a concentration-dependent but nonparallel shift to the right of the concentration-response curves to DDAVP. However, DDAVP did not affect the tension of the strip with or without endothelium in nonprecontracted aorta.(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals Antispasmodic and Antidiarrheal Activities ofValeriana hardwickiiWall. Rhizome Are Putatively Mediated through Calcium Channel Blockade

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Samra Bashir ◽  
Raafia Memon ◽  
Anwar H. Gilani
Keyword(s):  
Calcium Channel ◽  
Castor Oil ◽  
Channel Blockade ◽  
Response Curves ◽  
Calcium Channel Blockade ◽  
Traditional Use ◽  
Medicinal Uses ◽  
Rabbit Jejunum ◽  
Spontaneous Contractions ◽  
Dose Dependent

Valeriana hardwickiiis indigenous to Pakistan, Burma and Ceylon, where it is traditionally being used as an antispasmodic and antidiarrheal, besides its culinary use as spice. The aim of this paper was to provide pharmacological validation to these medicinal uses. The crude aqueous-methanolic extract ofValeriana hardwickiirhizome (Vh.Cr) was studied on isolated rabbit jejunum and castor oil-induced diarrhea in mice for spasmolytic and antidiarrheal properties, respectively. Vh.Cr caused concentration-dependent (0.01–1 mg/mL) relaxation of spontaneous contractions in isolated rabbit jejunum and inhibited K+-induced contractions (0.01–0.3 mg/mL), similar to verapamil, suggestive of calcium channel blockade (CCB). The CCB effect was confirmed when pretreatment of the jejunum preparations with Vh.Cr produced a concentration-dependent (0.03–0.1 mg/mL) rightward shift in the Ca++concentration-response curves, as caused by verapamil. Vh.Cr exhibited dose-dependent (100–300 mg/kg) protection against castor oil-induced diarrhea in mice. Loperamide, a standard antidiarrheal drug, similarly prevented the diarrhea. These data indicate the presence of CCB effect in the extract ofValeriana hardwickiirhizome, possibly mediating its antispasmodic and antidiarrheal activities and provide a scientific base for its traditional use in hyperactive gut disorders.

In vitro and in vivo biological approach to validate folkloric claims of Trianthema triquetra Rottler & Willd

2021 ◽  
Vol 50 (1) ◽  
pp. 21-28
Author(s):  
Fatima Saqib ◽  
Mehwish Shaukat ◽  
Sana Javad ◽  
Muhammad Riaz ◽  
Zahid Khan ◽  
...  
Keyword(s):  
Calcium Channels ◽  
Analgesic Activity ◽  
Rabbit Aorta ◽  
Lipoxygenase Activity ◽  
Traditional Practices ◽  
Response Curves ◽  
In Vivo Testing ◽  
Dose Dependent

Trianthema triquetra Rottler & Willd (Tt.Cr) is used in traditional practices as a remedy for various ailments. Hence current research was commenced to authenticate the folkloric uses. To discover spasmolytic potential, Tt.Cr was applied to isolate jejunum, while isolated tracheal and aorta tissues were used to determine the tissue relaxing properties of the extract. Anti-lipoxygenase activity was determined in vitro using Baicalein as standard. In vivo testing was carried to examine the potentiality of the herb to treat pyrexia and pain. Tt.Cr showed dose-dependent (0.01 - 3.0 mg/ml) spasmolytic effects in jejunum tissues and relaxed K+ (80 mM)-induced spasm and triggered rightwards shift of Ca+2 concentration-response curves. Carbachol (1μM)- together with K+ (80 mM) - induced tracheal spasm was also relaxed by Tt.Cr (0.01 to 1.0 mg/ml). Additionally, Tt.Cr (0.01 - 1.0 mg/ml) relaxed phenylephrine (1 μM) and K+ (80 mM) - treated constricted rabbit aorta. Tt.Cr (0.5 mM) inhibited lipoxygenase enzyme. Tt.Cr (80 mg/kg) settled pyrexia in rabbits comparable to aspirin and prolonged tail deflection time in mice (100 mg/kg) hence proving analgesic activity. The Tt.Cr demonstrated antispasmodic, bronchodilation and vasodilation properties probably by blocking calcium channels. These outcomes generate logic behind ancient application of herb for numerous ailments such as asthma, cough, heart problems and spasm.

scholarly journals Pharmacological basis for the folkloric uses of Buxus wallichiana in gastrointestinal, respiratory and vascular disorders

2015 ◽  
Vol 10 (2) ◽  
pp. 260 ◽  
Author(s):  
Musaddique Hussain ◽  
Shahid Masood Raza ◽  
Khalid Hussain Janbaz
Keyword(s):  
Crude Extract ◽  
Rabbit Aorta ◽  
Channel Blockade ◽  
Response Curves ◽  
Vascular Disorders ◽  
The Right ◽  
Dose Dependent ◽  
Higher Doses ◽  
Pharmacological Basis

<p><em>In vitro</em> study was carried out to explore the pharmacological basis of crude extract of <em>Buxus wallichiana </em>for its folkloric uses in gastrointestinal, respiratory and vascular disorders. In jejunum preparations, crude extract (0.03 ± 1.0 mg/mL) caused a transient spasmogenic effect followed by the spasmolytic effect at higher doses (3.0–10 mg/mL). In atropinized jejunum preparation, crude extract inhibited the spontaneous and K<sup>+ </sup>(80 mM)-induced contraction, suggesting that spasmolytic effect is mediated through the Ca<sup>+2</sup>-channel blockade. The Ca<sup>+2</sup>-channel blockade effect was confirmed when pretreatment of tissue with extract produced a dose-dependent shift in Ca<sup>+2 </sup>concentration-response curves to the right, similarly as verapamil. Furthermore, crude extract exhibited non-specific relaxant effect on carbachol- (1 µM) and K<sup>+ </sup>(80 mM)-induced tracheal contractions, suggesting the coexistence of anticholi-nergic and Ca<sup>+2</sup>-antagonistic properties. Moreover, it relaxed the K<sup>+ </sup>(80 mM)- and phenylephrine (1 µM)-induced contraction in rabbit aorta, suggesting the Ca<sup>+2</sup>-channel blockade. These findings may validate the folkloric uses of <em>B. wallichiana</em> in constipation, bronchitis, asthma and hypertension.</p>

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