Effect of cleistanthin A and B on adrenergic and cholinergic receptors

Parasuraman, Subramani; Raveendran, R

doi:10.4103/0973-1296.84239

Cited by 18 publications

(25 citation statements)

References 10 publications

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“…It was reported in a study conducted on isolated rat heart that both cleistanthins A and B had no effect on beta 1-adrenoceptors. 7 This suggests that the blockade of phenylephrine induced relaxation could be due to alpha 1-adrenoceptor antagonism. From the present study, it is evident that cleistanthins A and B effectively blocked the phenylephrine induced relaxation and this effect could be attributed to blockade of alpha 1-adrenoceptors.…”

Section: Conflict Of Interestmentioning

confidence: 99%

“…This finding is in agreement with the effect of cleistanthins A and B on rat vas deferens where both the compounds prevented the phenylephrine induced contractions. 7 We have collected all the blood samples under general anaesthesia and any undue stress induced endogenous epinephrine release was avoided. We have estimated the plasma insulin levels using an ultra-sensitive rat ELISA kit that can detect insulin levels up to ng/ml precise when compared to conventional radio-immuno assay technique.…”

Section: Conflict Of Interestmentioning

confidence: 99%

“…6 Subsequent study with cleistanthin A and B on guinea pig vas deferens confirmed the blockade of phenylephrine induced contractions. 7 Phenylephrine shows selective agonism to alpha 1-adrenoceptor and the fact that cleistanthins A and B block the contractions induced by phenylephrine indicates that cleistanthins A and B have alpha 1-adrenoceptor blocking property. However, to the best of our knowledge, the specificity of the compounds with respect to alpha 1 and 2-adrenoceptors has not been reported.…”

Section: Introductionmentioning

confidence: 99%

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Action of Cleistanthins A and B on Alpha Adrenoceptors in Rats

Lakshmanan¹,

Bobby²,

Raveendran³

2016

JYP

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Objectives: Cleistanthins A and B (CAB), active phytochemicals present in Cleistanthus collinus, have been proven to have alpha 1-adrenoceptor blocking property. However action on alpha 2-adrenoceptor is not studied. We aimed to study the action of CAB on alpha 2-adrenoceptor by measuring platelet aggregation, insulin and blood glucose levels with yohimbine as a standard comparator control and alpha 1-adrenoceptor by measuring the blockade of relaxation induced by phenylephrine in the jejunum of Wistar albino rats. Materials and methods: Forty eight adult male Wistar rats were divided into eight drug groups of six each, namely control (CMC 0.5%), yohimbine 2 mg/kg, 10, 30 and 100 mg/kg doses of cleistanthin A and cleistanthin B. Blood samples were drawn at baseline, after 5 h and after high-epinephrine dose (5 mg/kg) from the retro-orbital sinus and used for estimation of platelet aggregation and plasma insulin levels. Blood glucose levels were estimated at six different time points. Degree of jejunal relaxation was studied by relaxing the acetylcholine pre-contracted jejunum with phenylephrine. Results: All groups, except control and cleistanthin A 10 mg/kg group, significantly inhibited the platelet aggregation when compared to the respective baseline values (p<0.05). No significant difference was observed between different drug groups in plasma insulin and blood glucose levels. With regard to phenylephrine induced jejunal relaxation, the median IC 50 for all three doses of cleistanthin A and cleistanthin B 100 mg/kg differ significantly from that of control (CMC 0.5%). Conclusion: CAB block both alpha 1 and 2-adrenoceptorand hence are non-selective alpha-adrenoceptor blockers.

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Section: Conflict Of Interestmentioning

confidence: 99%

Section: Conflict Of Interestmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Action of Cleistanthins A and B on Alpha Adrenoceptors in Rats

Lakshmanan¹,

Bobby²,

Raveendran³

2016

JYP

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“…[ 23 ] Parasuraman and Raveendran reported that cleistanthins A and B had an alpha-adrenergic receptor blocking property in isolated guinea pig vas deferens. [ 24 ] It was suggested that cleistanthins A and B reduce BP, and it could be due to their alpha-adrenergic receptor blocking property. [ 22 ] The effect of cleistanthins, A and B on BP in repeated doses, was not studied, and their antihypertensive effect was not evaluated using animal models of hypertension.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the antihypertensive activity and alpha adrenergic receptor interaction of cleistanthins A and B

Priyadharsini¹,

Parasuraman²,

Raveendran³

2014

J Basic Clin Pharma

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Hypertension was induced in male Sprague Dawley rats with twice weekly administration of deoxycorticosterone acetate (DOCA) salt (20 mg/kg s.c) for 4 weeks. They were divided into eight groups of six animals each viz., hypertensive control, standard (prazosin 1 mg/kg), cleistanthin A 12.5, 25, 50 mg/kg and cleistanthin B 12.5, 25 mg/kg, and 50 mg/kg. One more group served as normal control. The hypertension was induced in 4 weeks, and the animals were given assigned treatment in 5th week. The alteration in blood pressure (BP) was recorded weekly using a rodent noninvasive blood pressure system. At the end of the experiment alpha-adrenergic receptor response of drugs like adrenaline, nor adrenaline, dopamine (doses 1 μg and 2 μg) was recorded invasively. Two-way repeated measures ANOVA followed by Bonferroni post-hoc test was used to analyze the data. The systolic BP and diastolic BP of test groups rose to a higher level after DOCA administration and fell to the normal range (P < 0.05) following the administration of cleistanthins A and B. There were no differences in the weekly heart rate among the groups. In the test group animals pretreated with prazosin and cleistanthins, adrenaline, noradrenaline and dopamine failed to raise the mean arterial pressure and the end-diastolic pressure from baseline (P > 0.05) cleistanthins A and B exert a significant antihypertensive effect through alpha-adrenergic receptor blockade similar to prazosin.

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“…Cleistanthus has been shown to contain bioactive lignan compounds such as cleistanthins A and B (from Cleistanthus collinus); these were found to be cytotoxic against several tumor cell lines [7,8]. Also, cleistanthins A and B inhibited the actions of the alpha adrenergic receptor and the nicotinic cholinergic receptor [9]. In Vietnam, 14 species of Cleistanthus have been identified and, importantly, some of them were used in traditional medicine [10].…”

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Cytotoxic Aryltetralin Lignans from Fruits of Cleistanthus indochinensis

et al. 2014

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Eight new aryltetralin lignans, cleisindosides A-F (1-6), picroburseranin (7), and 7-hydroxypicropolygamain (8), were isolated from the fruits of Cleistanthus indochinensis (Euphorbiaceae). The structures of the isolates were established on the basis of their one- and two-dimensional NMR spectral data, as well as their mass spectrometric data. Compound 7 was found to have potent cytotoxicity against oral epidermoid carcinoma cells with an IC50 value of 0.062 µM, whereas glycosylation to 3 (IC50 7.5 µM) and stereochemical changes to 8 (IC50 10.8 µM) led to marked decreases in biological activity. Thus, it was determined that the C-7 and C-8' positions are critical for the biological activity of the lignans from this plant.

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Effect of cleistanthin A and B on adrenergic and cholinergic receptors

Cited by 18 publications

References 10 publications

Action of Cleistanthins A and B on Alpha Adrenoceptors in Rats

Action of Cleistanthins A and B on Alpha Adrenoceptors in Rats

Evaluation of the antihypertensive activity and alpha adrenergic receptor interaction of cleistanthins A and B

Cytotoxic Aryltetralin Lignans from Fruits of Cleistanthus indochinensis

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