No abstract available.
Fibroblasts* ; Glycyrrhetinic Acid* ; Humans*

In this study,a nano drug delivery system GA-DTX-NGO which could be used for liver tumor photothermal and chemotherapy was prepared and characterized,with docetaxel(DTX) as model drug,glycyrrhetinic acid(GA) as the target molecule,and nano graphene oxide(NGO) as the photosensitizer. Firstly,GA-NGO nanocomposites were synthesized by the amidation reaction,and then GA-DTX-NGO was prepared by ultrasonic dispersion method. The encapsulation efficiency and drug loading ratio were determined by high performance liquid chromatography(HPLC) and ultracentrifugation; the morphology was observed by transmission electron microscopy(TEM). The photothermal conversion test was carried out by laser irradiation at 808 nm and the drug release test in vitro was performed using reverse dialysis. Finally,the effect of GA-DTX-NGO on SMMC-7721 liver tumor cells proliferation was determined by using MTT assay. The results showed that GA-DTX-NGO had good water dispersibility,and TEM results showed a lamellar structure with about 200 nm in diameter. The encapsulation efficiency and drug loading ratio of GA-DTX-NGO were(98. 89 ± 0. 07) % and(64. 74±0. 26) %,respectively. GA-DTX-NGO had strong photothermal conversion performance under 808 nm of laser irradiation. The drug release test in vitro results showed GA-DTX-NGO had obvious sustained-release effects and temperature-dependent release characteristics. The results of cell assay showed that GA-DTX-NGO could effectively inhibit the proliferation of SMMC 7721 cells in a concentration-and time-dependent manner,and the inhibitory effect was enhanced after combination with the near-infrared therapy. In conclusion,the preparation process of GA-DTX-NGO nano drug delivery system is feasible,which could provide some theoretical basis for further study of photothermal and chemotherapy on liver tumor.
Antineoplastic Agents ; Drug Carriers ; Drug Delivery Systems ; Glycyrrhetinic Acid ; Graphite

PURPOSE: To compare axial length (AL) and keratometry (K) using optical low-coherence reflectometry (OLCR, Lenstar LS900(R), Haag-Streit, Bern, Switzerland) with current ocular biometry devices and evaluate the accuracy of intraocular lens (IOL) power calculation. METHODS: In this prospective, comparative observational study of eyes with cataracts, AL and K were measured using an OLCR device (Lenstar LS900(R), Haag-Streit), partial coherence interferometry (PCI, IOL Master(R), Carl Zeiss, Jena, Germany), A-scan (Eyecubed) and automated keratometry (KR-7100, Topcon, Tokyo, Japan). IOL power calculation was performed using the Sanders-Retzlaff-Kraff (SRK/T) formula. The IOL prediction error (PE) was calculated by subtracting the predicted IOL power from the postoperative (PO) IOL power (PO 4 weeks, PO 12 weeks). RESULTS: A total of 50 eyes of 39 patients with cataracts (mean age 67.12 +/- 8.51 years) were evaluated in this study. AL and K were not significantly different between the OLCR device and other devices (analysis of variance [ANOVA], p = 0.946, 0.062, respectively). The mean PE in IOL power calculation was -0.22 +/- 0.50D with the OLCR device, 0.08 +/- 0.45D with the PCI device and -0.01 +/- 0.48D with A-scan and automated keratometry (ANOVA, p = 0.006). The highest percentage of eyes with PE smaller than +/- 0.5D was IOL Master(R) followed by Eyecubed and then Lenstar LS900(R). The mean absolute PE was not statistically significant among the 3 devices (ANOVA, p = 0.684). CONCLUSIONS: Ocular biometry measurements were comparable between the OLCR device and the PCI ultrasound device. However, the IOL power prediction showed significant differences among the 3 devices. Therefore, the differences in application of these devices should be considered.
Biometry* ; Cataract ; Glycyrrhetinic Acid ; Humans ; Interferometry ; Lenses, Intraocular* ; Observational Study ; Prospective Studies ; Ultrasonography

OBJECTIVES: In this study, the destabilizing effect of glycyrrhetinic acid on pre-formed biofilms of Streptococcus mutans (S. mutans) was observed. METHODS: Alamar blue assay was used to determine the toxicity of glycyrrhetinic acid on pre-formed biofilms of S. mutans. Four different concentrations (0, 3.75, 7.5, 15 µg/ml) of glycyrrhetinic acid were tested. Changes in the biofilm architecture after exposure to glycyrrhetinic acid were analyzed by scanning electron microscopy (SEM). Moreover, the role of glycyrrhetinic acid in enhancing the antimicrobial activity of cetylpyridinium chloride (CPC), an antimicrobial agent commonly used in oral health care products, was evaluated. RESULTS: Glycyrrhetinic acid concentration of up to 15 µg/ml had little cytotoxic effect but significantly changed the biofilm architecture. SEM analysis revealed destabilized biofilm structure after the preformed biofilms were exposed to glycyrrhetinic acid. Supplementing 2.5 µg/ml CPC with 15 µg/ml glycyrrhetinic acid significantly enhanced the bactericidal effect of CPC on the pre-formed biofilms than that in the non-supplemented CPC treated control. This indicates that glycyrrhetinic acid enhanced the antimicrobial activity of CPC by modifying the structure, thus facilitating the penetration of CPC into the biofilm. CONCLUSIONS: Glycyrrhetinic acid could be a potential agent to effectively control S. mutans biofilms responsible for dental caries.
Biofilms* ; Cetylpyridinium ; Dental Caries ; Glycyrrhetinic Acid* ; Microscopy, Electron, Scanning ; Oral Health ; Streptococcus mutans* ; Streptococcus*

A study on the microbial transformation of glycyrrhetinic acid (GA) was conducted by a fungus, Cunninghamella blakesleeana CGMCC 3.970 systematically. After incubation with the cell cultures of C. blakesleeana CGMCC 3.970 at 25 degrees C for 7 days on a rotary shaker operating at 135 r x min(-1), GA was converted into one major product and five minor products. The products were extracted and purified by solvent extraction, macroporous adsorbent resin, silica gel column chromatography, and semi-preparative RP-HPLC chromatography. Their structures were identified as 3-oxo-15α-hydroxy-18β-glycyrrhetinic acid(1), 3-oxo-15β-hydroxy-18β-glycyrrhetinic acid (2), 7β,15α-dihydroxy-18β-glycyrrhetinic acid (3), 3-oxo-7β, 15α-dihydroxy-18β-glycyrrhetinic acid (4), 7β-hydroxy-18β-glycyrrhetinic acid(5) and 15α-hydroxy-18β-glycyrrhetinic acid(6) by the analyses of MS, 1H-NMR and 13C-NMR spectroscopic data respectively. Among them, 2 was a new compound. These results suggest that C. blakesleeana CGMCC 3.970 has the capability of selective ketonization and hydroxylation for GA. [Key words] glycyrrhetinic acid; Cunninghamella blakesleeana CGMCC 3. 970; microbial transformation
Biotransformation ; Cunninghamella ; metabolism ; Glycyrrhetinic Acid ; analogs & derivatives ; chemistry ; metabolism ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

Glycyrrhetinic acid is a major active ingredient in licorice, a famous traditional Chinese medicine. Many studies on its anti-tumor activities and low toxicity to normal cells have attracted a great deal of attention. Reports indicated that glycyrrhetinic acid inhibited the growth of tumor cells through inducing apoptosis, differentiation and the block of cell cycle, suppressing tumor metastasis, reversing the multidrug resistance. Glycyrrhetinic acid also presented synergistic effects combined with chemotherapeutics and could inhibit the carcinogenesis induced by carcinogen. With further studies on mechanism of anticancer actions, glycyrrhetinic acid is being expected to have a good prospect of development and application for cancer therapy.
Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Cell Cycle ; drug effects ; Glycyrrhetinic Acid ; pharmacology ; Humans ; Neoplasm Invasiveness

OBJECTIVETo determine glycyrrhetinic acid concentration in rat plasma and concentration of calcium (Ca), copper (Cu), iron (Fe), potassium (K), magnesium (Mg) and sodium (Na) in rat serum after oral administration by LC-MS/MS and the flame atomic absorption method, and analyze the effect of glycyrrhetinic acid on the six elements in serum.

RESULTA similar variation trend between the concentration of glycyrrhetinic acid in plasma and that of Na, Cu elements in serum after oral administration of glycyrrhetinic acid was observed. Glycyrrhetinic acid in plasma at 2 h after administration reached the peak. Meanwhile, the concentration of Na and Cu at 4 h after the administration of glycyrrhetinic acid exhibited a significant increase (P < 0.05). Moreover, an increasing glycyrrhetinic acid dosage could result in the accumulation of Cu and Na in rat serum. Compared with the control group, the concentration of Cu and Na in the the glycyrrhetinic acid administration group with doses of 200 and 400 mg x kg(-1) revealed a significant increase (P < 0.05). However, glycyrrhetinic acid did not exhibit the great impact on the concentration of other elements in serum.

CONCLUSIONThis study focuses on the effect of oral administration of glycyrrhetinic acid on six metal elements in rat serum and provides an experimental basis for the adverse effect of glycyrrhetinic acid in clinical-applications.

Administration, Oral ; Animals ; Female ; Glycyrrhetinic Acid ; administration & dosage ; pharmacology ; Male ; Metals ; blood ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo develop a HPLC for the determination of plasma concentration of glycyrrhetic acid (GA) and study the pharmacokinetics of GA in rats.

METHODTo sample blood from rat which were injected GA by 1.0 mg x kg(-1) at 0.08, 0.17, 0.25, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6 h and use HPLC to determine the concentration of GA in it, the pharmaeokinetie parameters were accessed by DAS 1.0.

RESULTThe calibration curve was linear (r = 0.999 7) within the range of 50-2 000 ng x mL(-1) for GA in plasma. The average recovery was (105.2 +/- 2.23)%, (102.5 +/- 2.95)%, (98.4 +/- 2.32)%. The within-day and between-day derivation (RSD) were less than 4%. GA was fitted to a two compartment open pharmaeokinetie model in rats. The mainly pharmaeokinetie parameters were: t1/2alpha = (0.153 +/- 0.023) h, t1/2beta = (2.365 +/- 0.866) h, C(max) = (2.074 +/- 0.100) mg x L(-1), CL = (0.715 +/- 0.082) L x h(-1) x kg(-1), V(d) = (2.427 +/- 0.872) L x kg(-1), AUC(0-6 h) = (1.302 +/- 0.151) mg x h(-1) x L(-1).

CONCLUSIONThe method can be used to determine the concentration and to investigate the pharmacokinetics of GA in rat. GA was disposed extensively and rapidly in rats.

Animals ; Calibration ; Chromatography, High Pressure Liquid ; Glycyrrhetinic Acid ; pharmacokinetics ; Male ; Rats ; Reproducibility of Results ; Sensitivity and Specificity

Cell Line, Tumor ; Cell Proliferation ; Colorectal Neoplasms ; Glycyrrhetinic Acid/pharmacology* ; Humans

The optimal prescription of tanshinone Ⅱ_A(TSN)-glycyrrhetinic acid(GA) solid lipid nanoparticles(GT-SLNs) was explored and evaluated in vivo and in vitro, and its effect on acne after oral administration was investigated. The preparation processing and prescription were optimized and verified by single factor and response surface methodology. The in vitro release of GA and TSN in GT-SLNs was determined by ultra-performance liquid chromatography(UPLC). The effect of GT-SLNs on acne was investigated by the levels of sex hormones in mice, ear swelling model, and tissue changes in sebaceous glands, and the pharmacokinetics was evaluated. The 24-hour cumulative release rates of GA and TSN in SLNs were 65.87%±5.63% and 36.13%±2.31% respectively. After oral administration of GT-SLNs and the mixture of GA and TSN(GT-Mix), the AUC_(0-t) and AUC_(0-∞) of TSN in GT-SLNs were 1.98 times and 4.77 times those in the GT-Mix group, respectively, and the peak concentration of TSN in the GT-SLNs group was 17.2 times that in the GT-Mix group. After intragastric administration of GT-SLNs, the serum levels of testosterone(T) and the ratio of testosterone to estradiol(T/E2) in the GT-SLNs group significantly declined, and the sebaceous glands of mice were atrophied to a certain extent. The results demonstrated that obtained GT-SLNs with good encapsulation efficiency and uniform particle size could promote the release of GA and TSN. GT-SLNs displayed therapeutic efficacy on acne manifested by androgen increase, abnormal sebaceous gland secretion, and inflammatory damage.
Abietanes ; Acne Vulgaris/drug therapy* ; Animals ; Drug Carriers ; Glycyrrhetinic Acid ; Liposomes ; Mice ; Nanoparticles ; Particle Size ; Testosterone