Optimization of prescription and quality evaluation of Jieyu Anshen Gel Plaster / 中草药

Objective: To optimize the formulation of Jieyu Anshen Gel Plaster (JAGP) and evaluate its quality. Methods: With the bonding strength and sensory evaluation scores as indicators, the formulation of JAGP was optimized by using orthogonal experiment design method. Then the content of methyl eugenol, elemicin, β-asarone and α-asarone in JAGP were determined by GC-MS and the in vitro transdermal properties were studied by modified Franz diffusion cells. Results: The optimized blank matrix formulation was as following: NP700 of 3%, glycerol of 36%, PVP K30 of 4% and aluminium glycinate of 0.08%. The containing ointment of prepared gel plaster was 217.4 mg/cm2 and the effective component of the total index in gel paste was 5.77 mg/paste. Then the accumulated transdermal permeation of methyl eugenol, elemicin, β-asarone and α-asarone was (81.798 6 ± 14.872 6), (72.110 2 ± 17.776 1), (146.390 6 ± 33.794 1), (5.522 6 ± 1.279 6) μg/cm2, respectively within 24 h, which were all consistent with the zero-order equation. Conclusion: The preparation of JAGP with good stability and drug-releasing properties conformed to the relevant quality requirement, And this study provides certain basis for the development of production.

Chemical Constituents from the Rhizome of Saururus chinensis / 中国药学杂志

OBJECTIVE: To study the chemical constituents from the rhizome of Saururus chinensis. METHODS: The chemical constituents from the rhizome of Saururus chinensis were extracted by supercritical CO2 extraction and isolated by various chromatographic methods, such as silica gel, MCI and pre-HPLC. Their structures were elucidated by physico-chemical constants and spectroscopic methods. RESULTS: Seventeen compounds were isolated and identified as aurantiamide acetate (1), echinuline (2), (-) -(7R, 8R) -7-O-acetylpolysphorin (3), elemicin (4), isoelemicin (5), 1, 4-bis (3, 4-dimethyoxyphenyl) -2, 3-dimethyl-1, 4-butanedione (6), saucerneol D (7), (2R) -3-(3', 4 ', 5'-trimethoxyphenyl) -1, 2 -propanediol (8), grandisin (9), rel-(7R, 8R, 7 'R, 8'R) -3', 4'- methylenedioxy-3, 4, 5, 5 '-tetramethoxy-7, 7 -epoxylignan(10), zanthopyranone (11), (±) -eritro-1-(3, 4, 5 -trimethoxy) -1, 2 -propanodiol (12), threo-3, 4, 5 -trimethoxy-7-hydroxy-1'-allyl-3', 5 '-dimethoxy-8. O. 4'-neolignan (13), (+) -(8R) -(2, 6 -dimethoxy-4-propenylphenoxy) -1-(3, 4, 5 -trimethoxyphenyl) propan-1-one (14), meso-dihydroguaiaretic acid(15), (-) -galbacin (16), and (-) - (7R, 8R) -7-O-acetylraphidecursinol B (17). CONCLUSION: Compound 6 is a new natural compound. Compounds 1 - 2, 4 - 6, 8 - 9 and 11 - 13 are isolated from this plant for the first time.

Inhibition of Proinflammatory Cytokine Generation in Lung Inflammation by the Leaves of Perilla frutescens and Its Constituents

This study was designed to find some potential natural products and/or constituents inhibiting proinflammatory cytokine generation in lung inflammation, since cytokines such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) are pivotal for provoking airway inflammation. In our preliminary screening procedure, the 70% ethanol extract of the leaves of Perilla frutescens (PFE) was found to clearly inhibit TNF-alpha production in the lung at 100 mg/kg, after intranasal lipopolysaccharide treatment of mice. Based on this result, ten constituents including phenylpropanoids (allyltetramethoxybenzene, caffeic acid, dillapiole, elemicin, myristicin, nothoapiole, rosmarinic acid methyl ester, rosmarinic acid) and monoterpenes (perilla aldehyde and perilla ketone) were successfully isolated from the extract. Among them, elemicin and myristicin were found for the first time to concentration-dependently inhibit IL-1beta-treated IL-6 production from lung alveolar epithelial cells (A549) at concentrations of 10-100 microM. These findings suggest that the phenylpropanoids including elemicin and myristicin have the potential to be new inhibitory agents against lung inflammation and they may contribute, at least in part, to the inhibitory activity of PFE on the lung inflammatory response.

Inhibition of Proinflammatory Cytokine Generation in Lung Inflammation by the Leaves of Perilla frutescens and Its Constituents

This study was designed to find some potential natural products and/or constituents inhibiting proinflammatory cytokine generation in lung inflammation, since cytokines such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) are pivotal for provoking airway inflammation. In our preliminary screening procedure, the 70% ethanol extract of the leaves of Perilla frutescens (PFE) was found to clearly inhibit TNF-alpha production in the lung at 100 mg/kg, after intranasal lipopolysaccharide treatment of mice. Based on this result, ten constituents including phenylpropanoids (allyltetramethoxybenzene, caffeic acid, dillapiole, elemicin, myristicin, nothoapiole, rosmarinic acid methyl ester, rosmarinic acid) and monoterpenes (perilla aldehyde and perilla ketone) were successfully isolated from the extract. Among them, elemicin and myristicin were found for the first time to concentration-dependently inhibit IL-1beta-treated IL-6 production from lung alveolar epithelial cells (A549) at concentrations of 10-100 microM. These findings suggest that the phenylpropanoids including elemicin and myristicin have the potential to be new inhibitory agents against lung inflammation and they may contribute, at least in part, to the inhibitory activity of PFE on the lung inflammatory response.