The anti-inflammatory activity of curcumin (C), sodium curcuminate (NaC), diacetyl curcumin (DAC), triethyl curcumin (TEC), tetrahydro curcumin (THC) and ferulic acid (FA) was compared with that of phenylbutazone (PB) using the carrageenin-induced rat paw edema and cotton pellet granuloma tests. The rank order of potencies of curcumin analogues and PB in carrageenin-induced inflammation were NaC greater than THC greater than C greater than PB greater than TEC. The curcumin analogues de decreased carrageenin-induced paw edema at low doses, however, at higher doses this effect was partially reversed. FA and DAC were devoid of anti-inflammatory activity. Curcumin analogues were less effective in inhibiting the granulomatous tissue formation. Maximum activity was observed with TEC whereas C, NaC and PB were almost half as effective as TEC. C and NaC possess both anti-inflammatory and irritant properties as was evident from experiments in which drugs were incorporated into carrageenin and the cotton pellets for inducing inflammation. The anti-inflammatory action of NaC is not mediated through release of steroids from the adrenal cortex or inhibition of the biosynthesis of prostaglandins from arachidonic acid. The results of the present study support the rationale for the use of powdered rhizome of tumeric (contains 0.6% of curcumin) for conditions of sprain and inflammation.
Airway reactivity in spontaneously breathing unanaesthetized female guinea-pigs was significantly reduced as a consequence of maturation. Threshold doses to histamine (% w/v base) were 0.08% ± .01 and 0.27% ± .04 in immature (1 lOg + 2; 1 week old) and mature (837 g ± 29; 4 months old) animals, respectively. 2 The potency of 2-(2-thiazolyl) ethylamine in tracheal tissues from mature animals was significantly less than that in tissues from immature animals (5.06 ± .03 vs 5.26 ± .07). There was no change in the potency of this agonist in bronchial tissues (5.0 ± .09 vs 4.9 ± .13). 3 Diphenhydramine reduced tissue contractility in tracheal (30% at 0.1 1M; 50% at 3 iM) but not bronchial tissues. The antihistamine in concentrations ranging from 0.1 pM to 3 gM reduced the potency of histamine 2 to 50 fold in both tissues. 4 Schild plots were linear but slopes were significantly less than unity. pA2 values ± 95% fiducial limits derived from data from tracheal tissues of immature and mature animals using constrained Schild plots (unit slope) were 7.7 (7.6-7.7) and 7.1 (7.0-7.2), respectively (P< 0.05). pA2 values for diphenhydramine in bronchial tissues using constrained Schild plots were 7.8 (7.7-7.9) and 7.5 (7.3 -7.5), respectively (P< 0.05). 5 The data emphasize the unique nature of tracheal and bronchial tissues. We conclude that, with maturation, the characteristics of the histamine receptor change. We suggest that the remission of asthma which frequently occurs at puberty may be related to alteration in the properties of membrane receptors.
The synthesis and biological evaluation of 7,8-dihydroxy (2) and 7,8-methylenedioxy (3) analogues of 1-[(3,4,5-trimethyoxyphenyl)methyl]-2,3,4,5-tetradhyo-1H-2-b enzazepine on beta-adrenoceptor systems and human platelets were undertaken and compared with trimetoquinol (TMQ, 1). Whereas 1 is a potent beta-adrenoceptor agonist in guinea pig atria and trachea (pD2 = 8.2), analogue 2 was marginally effective at relaxing guinea pig tracheal smooth muscle (pD2 = 4.4) and inactive as an agonist on guinea pig atria. Analogues 2 and 3 were inhibitors of phospholipase C (PLC; from Clostridium perfringens) induced and secondary wave of ADP-induced aggregation responses and inactive against low-dose thrombin-induced or stable endoperoxide (U46619) induced human platelet aggregation. Against ADP-induced serotonin secretion, 3 was 9-fold more active than analogue 2. Further, the rank order of TMQ isomers and 3 as inhibitors of PLC-induced platelet aggregation, serotonin secretion, and phosphatidylinositol degradation was identical (3 greater than (S)-(-)-1 greater than (R)-(+)-1). The results suggest that these compounds are blocking the action of PLC by interfering with phosphatidylinositol turnover in platelet membranes. The inhibition of ADP-induced responses in human platelets by analogues 2 and 3 also suggests a site of inhibition at a level of arachidonic acid release. Thus, ring expansion of 1 as in the benzazepine analogues 2 and 3 has allowed us to develop selective inhibitors of platelet function that lack significant beta-adrenoceptor activity.
Musk(Kasturi), a dried prepucial secretion from male musk deer, has a wide range of activity in antagonizing the in vitro effects of-histamine, 5-hydroxy tryptamine, bradykinin, prostaglandin, acetylcholine and the Schultz-Dale reaction on the guinea-pig ileum. Musk also diminished in rats, the increased capillary perme ability induced by histamine and Russell's viper venom.
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