Determination of azelaic acid and potassium azeloycinate diglycinate in cosmetics by HPLC / 上海预防医学

ObjectiveAn HPLC method was established for the determination of azelaic acid and potassium azeloycinate diglycinate in cosmetics. MethodsThe samples were extracted with 60 mmol·L-1 sodium hydroxide water solution-methyl alcohol. After centrifugation and filtration， the analysis of azelaic acid and potassium azeloycinate diglycinate was performed with a SVEA C8（250 mm×4.6 mm， 5 μm） column， using 15 mmol‧L-1 potassium dihydrogen phosphate solution （pH=3.0） and acetonitrile for gradient elution at a flow rate of 1.0 mL·min-1.The analytes were detected with UV detector， and quantified by external standard curve. ResultsThe results showed a good linearity in the range of 5‒1 000 μg‧mL-1 with correlation coefficients （r） larger than 0.999. The detection limit of azelaic acid and potassium azeloycinate diglycinate （LOD） was 0.020% and 0.015%， respectively. The spiked recoveries were 87.66% to 108.96% with the relative standard deviation （RSD） of 0.6% to 3.3%. ConclusionThe method is simple， rapid and highly sensitive. It is suitable for the determination of azelaic acid and potassium azeloycinate diglycinate in cosmetics.

Preliminary discovery of quality marker (Q-marker) of Shenzhiling Oral Liquid based on “fingerprint-efficacy-pharmacokinetics” correlation / 中草药

Objective: To establish a research strategy for discovering quality marker (Q-marker) of Shenzhiling Oral Liquid based on the “fingerprint-efficacy-pharmacokinetics” correlation. Methods: HPLC fingerprints and acetylcholinesterase (AchE) inhibitory activities of 12 batches of Shenzhiling Oral Liquid were analyzed. The correlation analysis between the HPLC fingerprints and AchE inhibitory effects were carried out with orthogonal signal correction-partial least squares regression (OSC-PLSR) method. Combined with network pharmacology, efficacy-related components were determined. By identifying the compounds absorbed and exposed in vivo, pharmacologically active components were determined. Finally, Q-marker could be preliminarily discovered by the comprehensive analysis associated with the integration of efficacy-related components and pharmacologically active ingredients. Results: The results of OSC-PLSR analysis showed that three efficacy-related components were closely related to AchE inhibitory activities. According to mapping the targets of diseases, 61 efficacy-related components were determined. Eleven active compounds in plasma were identified by UHPLC-quadrupole-orbitrap-MS. The Q-markers of Shenzhiling Oral Liquid were liquiritin apioside, albiflorin and azelaic acid preliminarily determined by integrated and comprehensive analysis. Conclusion: The combination of fingerprint-efficacy relationship, network pharmacology and components absorbed in plasma could be an effective way for rapid analysis and discovery of Q-marker in Shenzhiling Oral Liquid, which will be of great significance both to improve the quality control and evaluation, and ensure the safety and effectiveness of traditional Chinese medicines.

Chemical constituets of Sparganium stoloniferum / 中草药

Objective: To study the chemical constituents of Sparganium stoloniferum. Methods: Column chromatographic techniques were applied to isolate the constituents. The chemical structures of the constituents were elucidated on the basis of physicochemical properties and spectral data. Results: Twelve compounds were isolated and identified as β-sitosterol palmitate (1), β-sitosterol (2), azelaic acid (3), docosanoic acid (4), 6,7,10-trihydroxy-8-octadecenoic acid (5), p-hydroxybenzaldehyde (6), sanleng diphenyl-acetypene (7), ferulic acid (8), 3,5-dihydroxy-4-methoxy-benzoic acid (9), 2,7-dihydroxy-xanthone (10), glycerol ferulate (11), and daucosterol (12). Conclusion: Compounds 3,4, and 9-11 are obtained from the plants of Sparganium L. for the first time.

A Study for Verification of Hair Growth Effect of Azelaic Acid and Vitamin B6

PURPOSE: Interest in the augmentation of hair growth for functional and aesthetic purpose has increased dramatically in recent years. Many hair growth products have been released, but most of these have not been proven scientifically. This study aims to measure the hair growth effect of azelaic acid and vitamin B6, which have been known as hair growth materials, in animal models. METHODS: Six weeks old C57BL/6 mice were used in this study and hair of mice were removed by topical treatment. The mice were divided into five experimental groups according to the testing material such as saline (negative control), propylene glycol(vehicle control), azelaic acid, vitamin B6 and azelaic acid plus vitamin B6 in combination. Hair growth was documented photographically and histologically, and then analysed by the high quality hair analysis program system. The quantity of endocrine factors, IGF-I and TGF-beta1 in the skin of mice was measured by PCR analysis. RESULTS: The topical treatment of azelaic acid and vitamin B6 in combination for 2 weeks to dorsal skin accelerated hair regrowth more than other groups. The azelaic acid and vitamin B6-combined treatment also promoted hair follicle elongation and thickness compared to the others. Histologic studies showed increased number of basal cells in azelaic acid and vitamin B6-combined treatment. Furthermore, the azelaic acid and vitamin B6-combined group significantly increased the expression of IGF-I but decreased the expression of TGF-beta1 in the skin of mice compared to other groups. CONCLUSION: These results suggest that azelaic acid and vitamin B6, when used together, have an additive effect and might be used as hair growth materials.

Effects of azelaic acid and tretinoin cream in the treatment of facial post-burn hyperpigmentation / 医学研究生学报

Objective:To investigate the method for treating facial post-burn hyperpigmentation. Methods: Forty-two patients with facial post-burn hyperpigmentation were randomly divided into two groups.Twenty-four subjects applied 15% Azelaic Acid cream combined with 0.025% Tretinoin cream daily to face,and eighteen subjects applied vehicle cream.At base line and six weeks of treatment,each subject's facial hyperpigmentation was assessed by area and colorimetric evaluations.Results:The facial post-burn hyperpigmentation of the Azelaic Acid and Tretinoin-treated subjects were significantly lighter after six weeks of therapy than those of the vehicle-treated subjects(?~(2)=10.94,P

The effect of azelaic acid and retinoic acid on epidermal melanocytes in UVB-irradiated black mice / 대한피부과학회지

Increased melanin pigmentation following ultraviolet irradiat.ion is due to increasing tyrosinase activity and multiplicatian of functioning melanocytes. After UV-irradiation, the size of melanocytes increases, and melanocyte dendrites elongatc, and branch. In this experiment, we induced the activation of melanocyts in the epidermis of C57BL black mice by ultraviolet-B(UVB) irradiation and observcd ihe effect of azelaic acid and retinoic acid on the UVB activated epidermal melanocytes. Sixty C57BL black mice were irradiated by UVB 100mJ/cm daily for 10 days, and then azeiaic acid and retinoic acid were topically applied daily for 7 weeks. For the estimation of morphologic change of epidermal melanocytes, light microscopic observation with split DOPA stain was performed at the end of the 1st, 3rd, 5th and 7th week of topical application. The results are summerized as follows : 1. The number, size and circumference of DOPA-positive epidermal melanocytes were significantly decreased in 20% azelaic acid applied group and 30% azelaic acid and 0.05% retinoic acid applied group. 2. In 20% azelaic;i.cid and 0.05% retinoic acid applied group, the number, size and circumference of DOPA-positive epidermal melanocytes were nore significantly decreased than in 20% azelaic acid applied group. In summary, the present study suggets that azelaic acid act as a depigmenting agent on epidermal melanocyte; and such depigmenting effect of azelaic acid was increased by addition of retinoic acid.

Effects of azelaic acid on melanocytes / 대한피부과학회지

The authors investigsted the effects of azelaic acid on human melanoma cells (G 361 melanoma cell line) and cultured normal melanocytes obtained from the prepuce of newborn. The results were as follows : 1. The proliferation of melanoma cells was decreased, but not in a dose-and time- ependent fashion. The cell population of melanoma cells after 2, 4, and 6 days of culture was decreased to 3.80 x 10(5)cells/well, 4.55 x 10(5)cells/well, and 4.30 X 10(5)cells/ well, respectively, in the presence of 10(-2)M azelaic acid. The proliferation of mormal elanocytes of normal melanocytes was decreased in a dose-dependent, but not in a time-dependent fashion. The cell population of normal melanocytes after 2, 4, and 6 days of culture was significantly decreased to 6.38 x 10(5)+/-1.37 x 10(5) cells/well, 5.33 x 10(5)+/-0.73x10(5) cells/well, and 7.20x10(5)+/-1,11 x10(5)cells/well, respectively, in the presence of 10(-2) M azelaic acid(p0.05) and 6953+/-1217 CPM (p<0.05) after 4 and 6 days of culture in the prensence of 10(-2) Mazelaic acid, 3. There was no difference in melanin content per well at various concentrations in either group, but the melanin content per individual melanocyte of the melanoma cells was increased to 0.0303 ng/cell, 0.0253 ng/cell, and 0.0377 ng/cell, respectively, and that of normal melanocytes was signifieantly increased to 0.0754+/-0.0215 ng/cell, 0.0719+/-0.0144 ng/cell(p<0.05), and 0.1089+/-0.0185 ng/cell(p<0.05), respectively, after 2, 4, and 6 days of culture in the presence of 10(-2) M azelaic acid.