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Painful menstrual cramps during or around the time of the monthly cycle are known as dysmenorrhea. The estimated global prevalence in women of reproductive age ranges from 45% to 95%. It has a significant negative impact on regular activities and productivity at work. However, despite the severe consequences on quality of life, primary dysmenorrhea (PD) is underdiagnosed. Dysmenorrhea has complex pathogenesis. It involves the release of prostaglandins and activation of the nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3) inflammasome and also includes the involvement of other mediators such as bradykinin, histamine and acetylcholine. Even though nonsteroidal anti-inflammatory drugs (NSAIDs) remain the most common type of pain medication, the question of which one should be the most preferred is still open to debate. The current review examines the existing evidence for the pathogenesis of PD and makes evidence based and clinical experience based recommendations for the use of mefenamic acid and its combination in the treatment of dysmenorrhea. Mefenamic acid alleviates PD by inhibiting endometrial prostaglandin formation, restoring normal uterine activity, and reducing the inflammatory response by inhibiting the NLRP3 inflammasome and reducing the release of cytokines such as interleukin (IL)-1?. It is also known to have bradykinin antagonist activity. Dicyclomine has a dual action of blocking the muscarinic action of acetylcholine in postganglionic parasympathetic effect or regions and acting directly on uterine smooth muscle by blocking bradykinin and histamine receptors to relieve spasms. According to the experts, mefenamic acid and dicyclomine act synergistically by acting on the different pathways of dysmenorrhea by blocking multifactorial agents attributed to the cause of dysmenorrhea. Hence, the combination of mefenamic acid and dicyclomine should be the preferred treatment option for dysmenorrhea.
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Background:Spasmolytics and NSAIDs are a therapy of choice in colic pain. However, the tolerability and effectiveness of this combination remains unexplored. The aim of this prospective, single-arm, open label, multicenter study was to evaluate the safety and effectiveness of Anafortan-N�(fixed-dose combination of camylofin dihydrochloride 50 mg + nimesulide 100 mg) in patients with acute colicky abdominal pain.Methods: In all, 295 patients with acute colicky abdominal pain and at least one episode of colicky pain in the last 24 hours were enrolled in this study. None of the patients were hospitalized. All patients were advised Anafortan-N畉ablets twice daily orally for 5 days. The safety of Anafortan-N畐as assessed by number and percentage of patients with adverse events (AEs) and change in the severity and frequency of AEs by the end of treatment. The tolerability was determined by number and percentage of patients who hadto discontinue the treatment due to AEs. The effectiveness was evaluated as percentage change in the mean intensity of pain score (based on a 100-mm visual analog scale) from baseline to end of treatment.Results: Overall, 14 (4.7%) patients reported 14 AEs, all of which were treatment-emergent and non-serious. Of the 14 AEs, 7 AEs were mild, 6 AEs were moderate, and 1 AE was severe. No serious adverse events (SAEs) were reported. No adjustment of the study medication was required in response to any of the AEs, and none of the AEs led to discontinuation of the study treatment. At end of treatment(EOT), the pain intensity significantly (p<0.0001) reduced to 1.7�49 with a mean change of -69.9�.42 from baseline, and the daily pain intensity significantly (p<0.0001) reduced to 0.1�38 with a mean change of -3.5�77 from baseline.Conclusions: Among Indian patients presenting with acute abdominal colicky pain, twice daily treatment with a FDC of camylofin dihydrochloride 50 mg and nimesulide 100 mg (Anafortan-N�) showed significant reduction in pain intensity with very few side effects, thereby confirming its safety, tolerability, and effectiveness in acute colicky abdominal pain.
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Background: Skeletal muscle relaxants are structurally distinct drugs prescribed for reducing muscle spasms, pain, and hyperreflexia. Centrally acting skeletal muscle relaxants are manufactured by various pharmaceutical companies with variable price. The present study, aimed to analyze the cost variation of various brands of centrally acting skeletal muscle relaxants, so as to help the physician to choose the cost effective treatment.Methods: Current index of medical stores (CIMS) April 2018 and online literature were used as information guide to review the prices of drugs used in the treatment of musculo skeletal pain and spastic neurological disorders.Results: Among anti spasmodic group, thiocolchicoside 4 mg shows maximum price variation of 337.5%, whereas carisoprodol 350 mg shows the least variation of 0.1%. It is evident from antispastic group that baclofen 10 mg shows maximum price variation of 93.91% and 5 mg of Baclofen shows the least variation of 11.22%. It is observed that, among anti spastic group, a percentage prize variation of 93.91 for 10 mg and 11.22 for 5 mg baclofen. Largest % prize variation is seen in metaxalone + diclofenac sodium (400+50) mg as 525% and the least variation is observed in tolperisone+ paracetamol (150+325) mg as 3.88%.Conclusions: Centrally acting orally effective skeletal muscle relaxants are commonly prescribed for painful musculoskeletal and spastic neurological disorders. Physicians should give due importance for the cost of the drugs while selecting appropriate drug for musculo skeletal disorders.
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To explore the mechanistic basis behind smooth muscle relaxant prospective of Bismarckia nobilis in gastrointestinal, respiratory and cardiovascular ailments. The methanolic extract of B. nobilis and sub-fractions have been evaluated in vitro rabbit isolated tissues, in vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice. The B. nobilis extract relaxed spontaneous and K+(80 mM)- induced contractions in rabbit isolated jejunum preparations, CCh (1 µM) and K+ (80 mM)-induced contractions in tracheal and bladder preparations, PE (1 µM) and K+ (80 mM)-induced concentrations in aorta preparations, likewise verapamil. Spasmolytic activity of dichloromethane fraction is stronger as compared to aqueous fraction. In vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice further supported spasmolytic activity. B. nobilis extract possess anti-spasmodic, anti-diarrheal, airway relaxant and vasodilator activities possible mediated through calcium channel blocking mechanism, justifying therapeutic utility of B. nobilis in diarrhea, asthma and hypertension.
El objetivo de trabajo fue explorar el mecanismo de acción relacionado con el efecto relajante del músculo liso inducido por Bismarckia nobilis (B. nobilis) en enfermedades gastrointestinales, respiratorias y cardiovasculares. El extracto metanólico de B. nobilis y subfracciones fue evaluado in vitro en tejidos aislados de conejos. Además se evaluó diarrea in vivo inducida con aceite de ricino en ratas y la actividad de harina de carbón vegetal en ratones. El extracto de B. nobilis relajó tanto las contracciones espontáneas como las inducidas por K+(80 mM) en preparaciones de yeyuno aisladas de conejos, las contracciones inducidas por PE (1 µM) y K+(80 mM) inducidas en preparaciones de aorta; de manera similar a verapamilo. La actividad espasmolítica de la fracción de diclorometano es más potente en comparación con la fracción acuosa. La diarrea inducida in vivo por el aceite de ricino en ratas y la actividad de la harina de carbón vegetal en ratones apoyaron aún más la actividad espasmolítica. El extracto de B. nobilis posee actividades antiespasmódicas, antidiarreicas, relajantes de las vías respiratorias y vasodilatadoras, posibles a través del mecanismo de bloqueo de los canales de calcio, lo que justifica la utilidad terapéutica de B. nobilis en la diarrea, el asma y la hipertensión.
Subject(s)
Animals , Rabbits , Rats , Plant Extracts/pharmacology , Anti-Asthmatic Agents/pharmacology , Arecaceae , Antidiarrheals/pharmacology , Antihypertensive Agents/pharmacology , Aorta/drug effects , Asthma/metabolism , Trachea/drug effects , Calcium Channel Blockers/pharmacology , Diarrhea/metabolism , Methanol , Hypotension/metabolism , Jejunum/drug effects , Muscle Relaxation/drug effects , Muscle, Smooth/drug effectsABSTRACT
Camylofin dihydrochloride is an anti-spasmodic drug available in India and other Latin American and African countries, for the treatment of abdominal colic and for acceleration of labor. Although, the drug has been in use for over six decades, with multiple citations in academic text books of repute, treatment protocols, and multiple research publications, there is no consolidated published information on the pharmacology and clinical details of camylofin. This drug statement/monograph is an attempt to collate and present scientific information that will come in handy to practicing obstetricians and gynaecologists, as well as other primary care physicians, when treating cases of abdominal colic or managing prolonged labor. Approved clinical indications, clinical pharmacology, dosage, contraindications, precautions, drug interactions, adverse effects, overdose and clinical evidence in different indications are covered herein.
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Objective: To discover the mechanism behind ameliorative effects of Michelia champaca (M. champaca) in gastrointestinal, respiratory and cardiovascular disorders. Methods: Anti- spasmodic potential was evaluated by trying the M. champaca extract (aqueous:ethanolic) on rabbit aorta, trachea and jejunum in vitro. Isotonic and isometric transducers coupled with Power Lab data acquisition system was used to record the responses of isolated tissues. Results: M. champaca extract relaxed the spontaneous and high K
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Objective:To discover the mechanism behind ameliorative effects of Michelia champaca (M. champaca) in gastrointestinal, respiratory and cardiovascular disorders.Methods:Anti- spasmodic potential was evaluated by trying the M. champaca extract (aqueous:ethanolic) on rabbit aorta, trachea and jejunum in vitro. Isotonic and isometric transducers coupled with Power Lab data acquisition system was used to record the responses of isolated tissues.Results:M. champaca extract relaxed the spontaneous and high KConclusion:M. champaca possesses spasmolytic, airways relaxant and vasodilator actions mediated perhaps due to blocking of Ca
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BACKGROUND/AIMS: Gastric cancer evolves in the pathologic mucosal milieu, and its development is characterized by both the loss of acid-secreting parietal cells and mucosal cell metaplasia, called spasmolytic polypeptide-expressing metaplasia (SPEM). Cytokines, such as interleukin (IL)-10, IL-1β, and IL-6, play a key role in gastric carcinogenesis. However, changes in the cytokine profile of SPEM have not been evaluated. METHODS: To induce SPEM in mouse stomachs, C57BL/6 mice were intraperitoneally injected with tamoxifen and sacrificed at 3, 10, and 21 days after treatment. RNA-sequencing (RNA-seq) and a multiplex bead array were used to measure cytokines in the stomachs of tamoxifen-treated/control mice. RESULTS: The administration of tamoxifen led to the rapid development and histological normalization of SPEM 3 and 10 days after administration, respectively. RNA-seq revealed that the expression of IL-10 was decreased 3 days after tamoxifen administration. The multiplex assay identified a significant decline in IL-10 levels 3 days after tamoxifen treatment (58.38±34.44 pg/mL vs 94.09±4.98 pg/mL, p=0.031), which normalized at 10 and 21 days after tamoxifen treatment. Immunofluorescence staining confirmed that IL-10 expression was markedly decreased at the time of SPEM development and subsequently returned to normal, accompanied by a reversal in histologic changes. CONCLUSIONS: IL-10 may play a pivotal role in the tamoxifen-induced acute development of gastric SPEM.
Subject(s)
Animals , Mice , Carcinogenesis , Cytokines , Fluorescent Antibody Technique , Gastric Mucosa , Interleukin-10 , Interleukin-6 , Interleukins , Metaplasia , Rabeprazole , Stomach , Stomach Neoplasms , TamoxifenABSTRACT
The uterine tetanic contraction and uterine artery blood flow reduction are possible reasons for primary dysmenorrhea (PD). In the present study, we aimed to evaluate the uterine relaxant effect and the influence on uterine artery blood velocity of Ge-Gen Decoction (GGD), a well-known Chinese herbal formula. In female ICR mice, uterine contraction was induced by oxytocin exposure following estradiol benzoate pretreatment, and the uterine artery blood velocity was detected by Doppler ultrasound. Histopathological examination of the uterine tissue samples were performed by H&E staining. Ex vivo studies demonstrated that oxytocin, posterior pituitary, or acetylcholine induced contractions in isolated mouse uterus. GGD inhibited both spontaneous and stimulated contractions. In vivo study demonstrated that GGD significantly reduced oxytocin-induced writhing responses with a maximal inhibition of 87%. Further study demonstrated that GGD normalized oxytocin-induced abnormalities of prostaglandins F2 alpha (PGF2α) and Ca(2+) in mice. In addition, injection of oxytocin induced a decrease in uterine artery blood flow velocity. Pretreatment with GGD reversed the oxytocin response on blood flow velocity. Histopathological examination showed pretreatment with GGD alleviated inflammation and edema in the uterus when compared with the model group. Both ex vivo and in vivo results indicated that GGD possessed a significant spasmolytic effect on uterine tetanic contraction as well as improvement on uterine artery blood velocity which may involve PGF2α and Ca(2+) signaling, suggesting that GGD may have a clinic potential in PD therapy.
Subject(s)
Animals , Female , Humans , Mice , Blood Flow Velocity , Drugs, Chinese Herbal , Dysmenorrhea , Drug Therapy , Mice, Inbred ICR , Oxytocin , Uterine Contraction , UterusABSTRACT
Background: The herbal formulation consisting of Andrographis paniculata Nees., Cassia fistula L., Foeniculum vulgare Mill. and Cuminum cyminum L. is widely used by the local traditional practitioners in rural Northern Karnataka for spasmodic abdominal pain. Objective: The present study was undertaken to evaluate safety and spasmolytic effect of poly‑herbal formulation. Materials and Methods: Acute toxicity studies were carried out in Swiss mice, as per the Organization for Economic Co‑operation and Development (OECD) guidelines. The spasmolytic activity of the formulation was studied in isolated guinea pig ileum model using histamine and acetylcholine as agonists. The data were analyzed by one‑way ANOVA, followed by Dunnetts post‑hoc test and P ≤ 0.05 was considered as significant. Results: The formulation did not show any adverse toxic effects and found to be safe. It also showed significant (P < 0.05) relaxation in different agonist like histamine and acetylcholine‑induced contractions in guinea pig ileum. Conclusions: Antispasmodic activity of the herbal formulation can be attributed to its atropine‑like activity. The present findings, therefore, support its utility in spasmodic abdominal pain.
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Recent studies have shown the spasmolytic activity of p-menthane monoterpenes (+)-pulegone and 4-terpinyl acetate (4-T) in guinea pig ileum. Since the action mechanism of these monoterpenes in intestinal smooth muscle is unknown, the present study was conducted to characterize their relaxant mechanism in isolated guinea pig ileum. We tested the involvement of voltage-dependent calcium and potassium channels and muscarinic antagonism. Both the monoterpenes caused a shift in the calcium curve to the right with reduction in the maximum effect. Pretreatment with tetraethylammonium chloride partially inhibited relaxation produced by both 4-T and (+)-pulegone. Both compounds caused a shift in the bethanechol curve to the right with reduction in the maximum effect. The results of this study indicate that the mechanisms of action of the smooth muscle relaxant monoterpenes (+)-pulegone and 4-T possibly involve the partial blockade of calcium channels, the activation of potassium channels, and the non-competitive antagonism of muscarinic receptors.
Estudios recientes han demostrado la actividad espasmolítica de los monoterpenos p-mentano de (+)-pulegona y acetato de 4-terpinilo (4-T) en el íleon de cobayo. Dado que el mecanismo de acción de estos monoterpenos en el músculo liso intestinal es desconocido, el presente estudio se llevó a cabo para caracterizar su mecanismo relajante en íleon aislado de conejillo de indias. Hemos probado la participación de tanto los canales calcio dependiente de voltaje como los canales de potasio y antagonistas muscarínicos. Ambos monoterpenos causaron un desplazamiento en la curva de calcio a la derecha con la reducción en el efecto máximo. El tratamiento previo con cloruro de tetraetilamonio inhibe parcialmente la relajación producida por tanto 4-T y (+)-pulegona. Ambos compuestos causaron un cambio en la curva de betanecol a la derecha con la reducción en el efecto máximo. Los resultados de este estudio indican que los mecanismos de acción de los monoterpenos relajantes del músculo liso (+)-pulegona y 4-T posiblemente implican el bloqueo parcial de los canales de calcio, la activación de los canales de potasio, y el antagonismo no competitivo de los receptores muscarínicos.
Subject(s)
Animals , Guinea Pigs , Ileum , Monoterpenes/pharmacology , Monoterpenes/chemistry , Plant Leaves , Parasympatholytics/pharmacology , Oils, Volatile/pharmacology , Muscarinic Antagonists/pharmacology , Ion Channels , Muscle, Smooth , Muscle RelaxationABSTRACT
Aims: Berberis lycium (Sumbal) is abundantly available in the northern areas of Pakistan and extensively used in local practice for the treatment of several human diseases. The objective of this study was to explore pharmacological basis for its use in gastrointestinal disorders. Materials and Methods: Crude aqueous (Bl.Aq) and methanolic (Bl.Meth) extracts of B. lycium were studied on isolated gut preparations of rabbit (jejunum) and guinea pig (ileum) by using in-vitro techniques. Tissues were mounted in tissue organ baths assembly containing physiological salt (Tyrode's) solution, maintained at 37ºC and aerated with carbogen, to assess the spasmogenic and spasmolytic effect and to find out the possible underlying mechanisms. Responses were measured on BioScience Powerlab data acquisition system by using isotonic transducers. Results: Phytochemical analysis indicates the presence of alkaloids, tannins and saponins in Bl.Aq and Bl.Meth. when tested on spontaneously contracting isolated rabbit jejunum, showed a dose-dependent spasmogenic effect at lower concentration (0.01-0.1 mg/mL) and (0.01-0.03 mg/mL), which was followed by spasmolytic effect at higher concentration (0.3-1.0 mg/mL) and (0.1-0.3 mg/mL) respectively. Pretreatment of the tissue with atropine (0.1 μM) partially suppressed the contractile effect. Bl.Aq and Bl.Meth caused complete inhibition of high K+ (80 mM)–induced contraction at 0.3 mg/mL and 0.1 mg/mL respectively and also produced a dose-dependent (0.01-0.03 mg/mL) rightward shift in the Ca++ concentration-response curve, similar to verapamil. When tested in bolus protocol on isolated guinea pig ileum, Bl.Aq and Bl.Meth caused a dosedependent spasmogenic effect at 0.01-0.1 mg/mL. Pretreatment of tissue with atropine (0.1 μM) partially suppress the contractile effect. Conclusions: Results indicate that spasmogenic effect was partially mediated through cholinergic activity and spasmolytic effect was mediated through calcium channel blocking activity (CCB), explain its traditional uses in diarrhea, intestinal cramps and other gastrointestinal intestinal disorders.
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O lapachol, alfa e beta-lapachona são o naftoquinonas obtidas de espécies de Tabebuia, apresentam propriedades antiinflamatória, antibacteriana, anticâncer e tripanossomicida. O objetivo deste trabalho foi investigar um possível efeito espasmolítico destas naftoquinonas em íleo de cobaia, uma vez que, outras naftoquinonas inibem a atividade contrátil de músculos lisos. O lapachol, alfa e beta-lapachona inibiram as contrações fásicas induzidas tanto por carbacol (CI50 = 1,5 ± 0,2 x 10-4; 7,3 ± 0,9 x 10-5 e 3,2 ± 0,5 x 10-5 M, respectivamente) quanto por histamina (CI50 = 3,6± 0,5; 3,6 ± 0,7 e 3,3 ± 0,6 x 10-5 M, respectivamente). Estes compostos também relaxaram o íleo pré-contraído com KCl (CE50 = 1,2 ± 0,4; 4,3 ± 0,8 e 2,7 ± 0,2 x 10-5 M, respectivamente); carbacol (CE50 = 2,6 ± 0,7; 3,5 ± 0,5 e 2,2 ± 0,7 x 10-5 M, respectivamente) ou histamina (CE50 = 3,0 ± 0,8; 1,1 ± 0,3 e 3,3 ± 0,6 x 10-5 M, respectivamente) de maneira dependente de concentração. Este efeito é provavelmente devido à inibição do influxo de Ca2+ através dos canais de Ca2+ dependentes de voltagem (CaV). Beta-lapachona antagonizou (pD'2 = 5,73 ± 0,12; "slope" = 1,51 ± 0,05) as contrações induzidas por CaCl2 em meio despolarizante nominalmente sem Ca2+. O achado de que a beta-lapachona inibiu as contrações tônicas induzidas por S-(-)-Bay K8644 (CE50 = 1,4 ± 0,1 x 10-5 M) é sugestivo que o CaV envolvido é o do tipo L. Em conclusão lapachol, alfa e beta-lapachona apresentam atividade espasmolítica não seletiva em íleo de cobaia, e beta-lapachona exerce este efeito pelo bloqueio dos canais CaV tipo L.
Lapachol, alpha and beta-lapachone are naphthoquinones extracted from species of Tabebuia that have shown antiinflammatory, antibacterial, anticancer and trypanosomicidal properties. The aim of this work was to investigate the spasmolytic effect of these naphthoquinones on the guinea-pig ileum, since other naphthoquinones are known to depress the contractile activity of smooth muscles. Lapachol, alpha and beta-lapachone inhibited the phasic contractions induced by both carbachol (IC50 = 1.5 ± 0.2 x 10-4; 7.3 ± 0.9 x 10-5 and 3.2 ± 0.5 x 10-5 M, respectively) and histamine (IC50 = 3.6± 0.5; 3.6 ± 0.7 and 3.3 ± 0.6 x 10-5 M, respectively). These compounds also relaxed the ileum pre-contracted with KCl (EC50 = 1.2 ± 0.4; 4.3 ± 0.8 and 2.7 ± 0.2 x 10-5 M, respectively); carbachol (EC50 = 2.6 ± 0.7; 3.5 ± 0.5 and 2.2 ± 0.7 x 10-5 M, respectively) or histamine (EC50 = 3.0 ± 0.8; 1.1 ± 0.3 and 3.3 ± 0.6 x 10-5 M, respectively) in a concentration-dependent manner. This effect is probably due to inhibition of calcium influx through voltage-gated calcium channels (Ca v). Beta-lapachone antagonized (pD'2 = 5.73 ± 0.12; slope = 1.51 ± 0.05) CaCl2-induced contractions in depolarizing medium nominally without Ca2+. The finding that Beta-lapachone inhibited the tonic contractions induced by S-(-)-Bay K8644 (EC50 = 1.4 ± 0.1 x 10-5 M) is suggestive that the L-type CaV is involved. In conclusion, lapachol, alpha and beta-lapachone showed non-selective spasmolytic activity in guinea-pig ileum, and beta-lapachone exerts this effect by to blockade of L-type CaV channels.
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Na última década, o gênero Hypericum ganhou repercussão mundial devido à utilização de Hypericum perforatum para obtenção de medicamentos antidepressivos. Por esta razão, a maioria dos estudos com outras espécies do gênero centra-se nesta atividade. Porém, um dos usos populares de espécies de Hypericum nativas do sul do Brasil é no tratamento de problemas gastrintestinais, inclusive como antiespasmódico. Neste trabalho, foi avaliado o efeito de uma das espécies de Hypericum nativas do Rio Grande do Sul, H. caprifoliatum, sobre as contrações induzidas por agonistas em íleo isolado de cobaio. Foi investigado o efeito de um extrato ciclo-hexano purificado (isento de clorofila e ceras), nas concentrações de 1, 3, 10 e 30 mg/mL, sobre curvas cumulativas de acetilcolina, histamina, potássio e serotonina (10-7 a 10-4 M). Na concentração de 30 mg/mL o extrato inibiu totalmente as contrações induzidas por todos os agonistas. Na concentração de 10 mg/mL, o extrato apresentou efeito antagonista não-competitivo de serotonina, reduzindo a contração máxima induzida por serotonina em cerca de 50 por cento. A resposta contrátil aos outros mediadores não foi alterada. Estes resultados indicam que espécies de Hypericum do sul do Brasil podem ser uma perspectiva interessante na busca de moléculas com atividade sobre a motilidade gastrintestinal.
In the last decade the genus Hypericum has achieved worldwide recognition due to the therapeutic value of H. perforatum as an antidepressant drug. Consequently this activity is the most investigated one. However, species native to Brazil have other folk uses such as for the treatment of digestive disorders, including cramps. In this study we evaluated the effect of a purified cyclohexane extract (chlorophyll and waxes free) (1,3,10 and 30 mg/mL) of H. caprifoliatum, a specie native to South Brazil, on isolated guinea pig ileum contractions induced by different mediators: serotonin, histamine, acetylcholine and potassium chloride (10-7 - 10-4 M). At 30 mg/mL all contractile responses were abolished. At 10 mg/mL only serotonin responses were altered: the extract reduced the maximal effect in 50 percent, which represents a non-competitive antagonism. At 1 and 3 mg/mL the extract was unable to modify all mediators response. These results point to native species of Hypericum as an interesting perspective in searching new molecules active on gastrointestinal motility.
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Hypericum , Ileum , Parasympatholytics , SerotoninABSTRACT
OBJECTIVE:To explore the spasmolytic effect of baked Radix Vladimiriae on in vitro intestinal muscle in rabbits. METHODS:Magnus in vitro intestinal muscle accumulative dose method was adopted to observe the dose-effect relationship of petroleum ether parts of baked Radix Vladimiriae with in vitro intestinal muscle of rabbits and its impact on the spasm of rabbit intestinal muscle induced by acetylcholine, histamine phosphate and Bacl2. RESULTS:There was a certain dose-effect relationship between petroleum ether parts of baked Radix Vladimiriae and spasmolytic mechanism of rabbit in vitro intestine. It showed the effect of acetylcholine, histamine phosphate and Bacl2. CONCLUSION:The inhibition effect of petroleum ether parts of baked Radix Vladimiriae on normal in vitro intestinal muscle increase as long as dose increase. The inhibition mechanism may be associated with acetylcholine competing with histamine to block M receptor and H1 receptor as well as to inhibit excitability of intestinal muscle.
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Solanum megalonyx Sendtn. (Solanaceae) é conhecida popularmente por "jurubeba" no Nordeste do Brasil e se apresenta na forma de arbusto. Várias espécies de Solanum apresentam efeito espasmolítico em órgãos isolados. Assim, objetivou-se investigar e comparar o efeito dos extratos metanólico (SM-MeOH) e acetato de etila (SM-AcOEt), obtidos das partes aéreas de S. megalonyx, em íleo isolado de cobaia. SM-MeOH e SM-AcOEt antagonizaram (n = 5) as contrações fásicas induzidas por 1 mM de acetilcolina (logCI50 = 3,2 ± 0,1 e 1,8 ± 0,6 mg/mL, respectivamente) ou de histamina (logCI50 = 2,8 ± 0,5 e 1,7 ± 0,3 mg/mL, respectivamente). SM-MeOH e SM-AcOEt também relaxaram (n = 5) o íleo pré-contraído por 40 mM de KCl (logCE50 = 1,9 ± 0,09 e 1,9 ± 0,1 mg/mL, respectivamente), por 1 mM de histamina (logCE50 = 1,9 ± 0,07 e 1,7 ± 0,08 mg/mL, respectivamente) ou de acetilcolina (logCE50 = 1,9 ± 0,02 e 1,7 ± 0,09 mg/mL, respectivamente) de maneira dependente de concentração e equipotente. Demonstra-se pela primeira vez que S. megalonyx apresenta efeito espasmolítico não seletivo em íleo isolado de cobaia, sugerindo que os extratos podem estar agindo em um passo comum da via de sinalização dos agentes contráteis testados.
Solanum megalonyx Sendtn. (Solanaceae) is known popularly as "jurubeba" in Northeastern Brazil where it can be found as a shrub. Several species of Solanum present spasmolytic effect in several tissues, thus this study was aimed to investigate and compare the effect of the methanol extract (SMMeOH) and ethyl acetate extract (SM-AcOEt), obtained from aerial parts of Solanum megalonyx Sendtn., in guinea-pig ileum. In this work, both SM-MeOH and SM-AcOEt antagonized the phasic contraction induced by acetylcholine 1 mM (logIC50 = 3.2 ± 0.1 and 1.8 ± 0.6 mg/mL) and histamine 1 mM (logIC50 = 2.8 ± 0.5 and 1.7 ± 0.3 mg/mL, respectively) (n = 5), without statistical differences between these values. In another set of experiments, SM-MeOH and SM-AcOEt also relaxed the isolated guinea-pig ileum pre-contracted by KCl 40 mM (logEC50 = 1.9 ± 0.09 and 1.9 ± 0.1 mg/mL, respectively), histamine 1 mM (logEC50 = 1.9 ± 0.07 mg/mL and 1.7 ± 0.08 mg/mL, respectively) or acetylcholine (logEC50 = 1.9 ± 0.02 mg/mL and 1.7 ± 0.09 mg/mL, respectively) (n = 5) in a concentration-dependent and equipotent manner. This study demonstrates for the first time that aerial parts of S. megalonyx present a non-selective spasmolytic effect in guinea-pig ileum, suggesting that the extracts could be acting in a common step of the pathway signaling that leads to contraction induced by the contractile agents tested.
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OBJECTIVE:To study the litholytic,bacteriostatic and spasmolytic effects of Baoganxiaoshi capsule(BXC) in vitro.METHODS:Observed the effects of BXC on human bile pigmental and cholesterol gallstone, bacteria, duodenum smooth muscle of rabbits in vitro.RESULTS:The litholytic concentration of 7.568,15.135 and 30.270g(crude drug)/ml solutions of BXC on human bile pigmental gallstone were 5.4mg,8.3 mg and 14.7 mg respectively,and on human bile cholesterol gallstone were 2.9mg,5.1 mg and 7.1 mg respectively.So BXC have the litholytic function of bile pigmental and cholesterol gallstone.It can strongly inhibit or sterilize staphylococcus aureus, enterococcus, diphtherial bacillus, hemo1ytic streptococcus, and the MICs were 23.65mg(crude drug)/ml ,23.65mg(crude drug)/ml,23.65mg(crude drug)/ml and 47.297mg(crude drug)/ml respectively, and all of the MBCs were 47.297mg(crude drug)/ml.It can inhibit or sterilize coliform,salmonella and pneumococcus, and all of the MICs were 378.375mg(crude drug)/ml, and all of the MBCs were 756.75mg(crude drug)/ml.5.3 414mg(crude drug)/ml solutions of BXC could obviously inhibit the average tension amplified,the frequency accelerated,and the activity increaced,on the duodenum smooth muscle induced by ach(P