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PubMed2003

Effect of 14-deoxyandrographolide on calcium-mediated rat uterine smooth muscle contractility.

In this study, the effect of 14-deoxyandrographolide (14-DAP) on calcium channel-dependent rat uterine smooth muscle contraction was evaluated. Using a tissue bath preparation, 14-DAP was able to reduce the contractile response to 0.3 and 3.0 mm of CaCl(2), with an IC(50) of 1.24 +/- 0.23 x 10(-5) m and 5.94 +/- 0.29 x 10(-5) m, respectively. 14-DAP shifted the CaCl(2) cumulative dose response curve to the right, increasing the EC(50) from 2.08 +/- 0.20 x 10(-4) m to 4.22 +/- 0.22 x 10(-4) m (5 micrometer 14-DAP) and 2.5 +/- 1.0 x 10(-3) m (50 micrometer 14-DAP). In order to determine if 14-DAP had any effect on intracellular calcium, the relaxant response to 14-DAP following contraction by oxytocin, PGF(2alpha) and vanadate in Ca(+2)-free solution was compared with that of isoproterenol and phenylbutazone. While isoproterenol and phenylbutazone relaxed the smooth muscle in a dose-dependent manner, 14-DAP did not have any effect on either the oxytocin, PGF(2alpha) or vanadate-induced smooth muscle contraction. Based on these data, it appears that 14-DAP is an uterine smooth muscle relaxant which produces a selective blockade of voltage operated calcium channels.

Andrographis↗
PubMed2004

Activation of alpha1A-adrenoceptor by andrographolide to increase glucose uptake in cultured myoblast C2C12 cells.

We investigated the mechanism of the plasma glucose lowering action of andrographolide, using radioactive glucose uptake into cultured myoblast C2C12 cells as the indicator. In C2C12 cells, andrographolide increased the radioactive glucose uptake in a concentration-dependent manner that was abolished by pretreatment with prazosin. Activation of alpha1-adrenoceptors by andrographolide was further indicated by the displacement of the [3H]prazosin binding in C2C12 cells. The alpha1A-adrenoceptor appears to have caused the displacement, because RS17053 abolished this andrographolide-stimulated glucose uptake at concentrations sufficient to block the alpha1A-adrenoceptor. Inhibition of phospholipase C (PLC) with U73312 concentration-dependently decreased under the action of andrographolide in C2C12 cells. This inhibition of glucose uptake by U73122 was specific because the inactive congener, U73343, failed to influence the action of andrographolide. Moreover, both chelerythrine and GF 109203X diminished the action of andrographolide at concentrations sufficient to inhibit protein kinase C (PKC). Our data suggest that an activation of alpha1A-AR by andrographolide in C2C12 cells may increase the glucose uptake via the PLC-PKC pathway.

Adrenergic alpha-Antagonists↗
PubMed2006

Oxidation studies on Andrographolide.

Jones oxidation of Andrographolide (1), gave mixture of three products (3-dehydroandrographolide (5), 3,19-bis dehydroandrographolide (6) and 19-dehydroandrographolide (7). Tritylation of andrographolide at C19-OH resulted to products 8 and diene 9, which can be converted to its acetate 10 and oxidation product 11.

Acetic Anhydrides↗
PubMed2004

[Effect of API 0134 on platelet membrane glycoprotein expression in patients with hyperlipemia].

OBJECTIVE: By observing the effect of API 0134, an active ingredient of green chiretta, on platelet membrane glycoprotein (GP) in patients with hyperlipemia to explore the mechanism of the anti-platelet aggregation effect of API. METHODS: The mean immunofluorescent intensity (MFI) of the platelet membrane glycoprotein GP II b/III a, GPIb, P-selectin (GMP-140) and von Willebrand's factor (vWF) in resting platelet, activated platelet (untreated or treated with API 0134 of different concentrations) were detected in 30 randomly selected patients with hyperlipemia, using immunofluorescent marker and flow cytometry. RESULTS: API of all concentrations (25 mg/L, 50 mg/L and 100 mg/L) could significantly decrease the MFI of GP II b/III a in a positive dose-dependent manner, as compared with that in activated platelet untreated with API; API of 50 mg/L and 100 mg/L could also reduce the MFI of GMP-140 and vWF in activated platelet (P < 0.01); but API of 100 mg/L showed insignificant influence on GPIb expression in activated platelet membrane. CONCLUSION: API 0134 exerts obvious anti-platelet GP II b/III a effect on activated platelets, middle or large dose of API also shows inhibiting effect on GMP-140 and vWF expression in platelet.

Aged↗
PubMed2006

[Effect of andrographolide on QS regulating virulence factors production in Pseudomonas aeruginosa].

OBJECTIVE: To investigate the effect of andrographolide on virulence factors production in Pseudomonas aeruginosa. METHOD: Growth rate, pyocyanin, proteolytic activity and elastase activity were measured with or without the presence of andrographolide. The effect of andrographolide on pyocyanin production, proteolytic activity and elastase activity in PAO-JP2 was investigated simultaneously. RESULT: The andrographolide did not affect the growth of PAO1 in planktonic culture. The production of pyocyanin, proteolytic activity and elastase activity were significanthy suppressed in P. aeruginosa cultures grown in the presence of andrographolide. However, these effects were not observed in PAO-JP2. CONCLUSION: The inhibiting effect of andrographolide on virulence factors production in P. aeruginosa may play a role in its anti-infection activity.

Andrographis↗