Pharmacokinetic Herb-Drug Interactions of Glipizide with Andrographis paniculata (Burm. f.) and Andrographolide in Normal and Diabetic Rats by Validated HPLC Method.

Co-administered medicinal herbs can modify a drug's pharmacokinetics (PK), effectiveness, and toxicity. Andrographis paniculata (Burm. f.) ethanolic extract (APE) and andrographolide (AND) (a potent CYP2C9 inducer/inhibitor) can alter the pharmacokinetic parameters of glipizide (GLZ). This study aimed to determine the potential pharmacokinetics of herb−drug interactions between GLZ and APE/AND in the plasma of normal and diabetic rats using the HPLC bioanalysis method. The glipizide bioanalytical method established with RP-HPLC/UV instrument was validated following the EMA guidelines. GLZ was administered alone and in combination with APE or AND to normal and diabetic rats. The GLZ pharmacokinetic parameters were estimated according to the correlation between concentration and sampling time using the PK solver program. A simple and rapid GLZ bioanalysis technique with a lower limit of quantitation of 25 ng/mL was developed and presented the following parameters: accuracy (error ≤ 15%), precision (CV ≤ 15%), selectivity, stability, and linearity (R2 = 0.998) at concentrations ranging 25−1500 ng/mL. APE administration significantly improved the Cmax and AUC0−t/AUC0−∞ GLZ values in normal and diabetic rats (p < 0.05). AND significantly reduced the bioavailability of GLZ in diabetic rats with small values of T 1/2, Cmax, and AUC0−t/AUC0−∞ (p < 0.05). This combination can be considered in administering medications because it can influence the pharmacological effects of GLZ.

Metabolite Fingerprinting Based on 1H-NMR Spectroscopy and Liquid Chromatography for the Authentication of Herbal Products.

Herbal medicines (HMs) are regarded as one of the traditional medicines in health care to prevent and treat some diseases. Some herbal components such as turmeric and ginger are used as HMs, therefore the identification and confirmation of herbal use are very necessary. In addition, the adulteration practice, mainly motivated to gain economical profits, may occur by substituting the high price of HMs with lower-priced ones or by addition of certain chemical constituents known as Bahan Kimia Obat (chemical drug ingredients) in Indonesia. Some analytical methods based on spectroscopic and chromatographic methods are developed for the authenticity and confirmation of the HMs used. Some approaches are explored during HMs authentication including single-component analysis, fingerprinting profiles, and metabolomics studies. The absence of reference standards for certain chemical markers has led to exploring the fingerprinting approach as a tool for the authentication of HMs. During fingerprinting-based spectroscopic and chromatographic methods, the data obtained were big, therefore the use of chemometrics is a must. This review highlights the application of fingerprinting profiles using variables of spectral and chromatogram data for authentication in HMs. Indeed, some chemometrics techniques, mainly pattern recognition either unsupervised or supervised, were applied for this purpose.

Metabolite Fingerprinting Using 1H-NMR Spectroscopy and Chemometrics for Classification of Three Curcuma Species from Different Origins.

Curcuma longa, Curcuma xanthorrhiza, and Curcuma manga have been widely used for herbal or traditional medicine purposes. It was reported that turmeric plants provided several biological activities such as antioxidant, anti-inflammatory, hepatoprotector, cardioprotector, and anticancer activities. Authentication of the Curcuma species is important to ensure its authenticity and to avoid adulteration practices. Plants from different origins will have different metabolite compositions because metabolites are affected by soil nutrition, climate, temperature, and humidity. 1H-NMR spectroscopy, principal component analysis (PCA), and orthogonal projections to latent structures-discriminant analysis (OPLS-DA) were used for authentication of C. longa, C. xanthorrhiza, and C. manga from seven different origins in Indonesia. From the 1H-NMR analysis it was obtained that 14 metabolites were responsible for generating classification model such as curcumin, demethoxycurcumin, alanine, methionine, threonine, lysine, alpha-glucose, beta-glucose, sucrose, alpha-fructose, beta-fructose, fumaric acid, tyrosine, and formate. Both PCA and OPLS-DA model demonstrated goodness of fit (R2 value more than 0.8) and good predictivity (Q2 value more than 0.45). All OPLS-DA models were validated by assessing the permutation test results with high value of original R2 and Q2. It can be concluded that metabolite fingerprinting using 1H-NMR spectroscopy and chemometrics provide a powerful tool for authentication of herbal and medicinal plants.

Self-nanoemulsifying Delivery of Andrographolide: Ameliorating Islet Beta Cells and Inhibiting Adipocyte Differentiation.

Purpose: Insulin resistance is a characteristic of non-insulin-dependent diabetes mellitus associated with obesity and caused by the failure of pancreatic beta cells to secrete sufficient amount of insulin. Andrographolide (AND) improves beta-cell reconstruction and inhibits fat-cell formation. This research aimed to improve the delivery of water-insoluble AND in self-nanoemulsifying (ASNE) formulation, tested in streptozotocin (STZ)-induced diabetic rats and 3T3-L1 preadipocyte cells. Methods: A conventional formulation of AND in suspension was used as a control. The experimental rats were orally administered with self-nanoemulsifying (SNE) and suspension of AND for 8 days. Measurements were performed to evaluate blood glucose levels in preprandial and postprandial conditions. Immunohistochemistry was used to assess the process of islet beta cell reconstruction. In vitro study was performed using cell viability and adipocyte differentiation assay to determine the delivery of AND in the formulation. Results: ASNE lowered blood glucose levels (day 4) faster than AND suspension (day 6). The histological testing showed that ASNE could regenerate pancreatic beta cells. Therefore, ASNE ameliorated pancreatic beta cells. The in vitro evaluation indicated the inhibition of adipocyte differentiation by both AND and ASNE, which occurred in a time-dependent manner. ASNE formulation had better delivery than AND. Conclusion: ASNE could improve the antidiabetic activity by lowering blood glucose levels, enhancing pancreatic beta cells, and inhibiting lipid formation in adipocyte cells.

Analysis of Lard in Lipstick Formulation Using FTIR Spectroscopy and Multivariate Calibration: A Comparison of Three Extraction Methods.

Analysis of lard extracted from lipstick formulation containing castor oil has been performed using FTIR spectroscopic method combined with multivariate calibration. Three different extraction methods were compared, namely saponification method followed by liquid/liquid extraction with hexane/dichlorometane/ethanol/water, saponification method followed by liquid/liquid extraction with dichloromethane/ethanol/water, and Bligh & Dyer method using chloroform/methanol/water as extracting solvent. Qualitative and quantitative analysis of lard were performed using principle component (PCA) and partial least square (PLS) analysis, respectively. The results showed that, in all samples prepared by the three extraction methods, PCA was capable of identifying lard at wavelength region of 1200-800 cm-1 with the best result was obtained by Bligh & Dyer method. Furthermore, PLS analysis at the same wavelength region used for qualification showed that Bligh and Dyer was the most suitable extraction method with the highest determination coefficient (R2) and the lowest root mean square error of calibration (RMSEC) as well as root mean square error of prediction (RMSEP) values.

Combination of low-concentration of novel phytoestrogen (8,9)-furanyl-pterocarpan-3-ol from Pachyrhizus erosus attenuated tamoxifen-associated growth inhibition on breast cancer T47D cells

Objective: To investigate the estrogenic effect of (8,9)-furanyl-pterocarpan-3-ol (FPC) on growth of human breast cancer T47D cells and the interactions between the FPC and tamoxifen (TAM), on the growth of estrogen receptor-dependent breast cancer T47D cells.Methods:T47D cells were treated with FPC alone (0.01-200 μmol/L) or in combination with TAM 20 nmol/L. The proliferation effect of FPC were conducted on T47D cells in vitro by MTT test. Furthermore, the expression of ERα or c-Myc were also determined by immunohistochemistry.Results:inhibitory effect on T47D cells, wheraes co-administered with low concentration (less than 1μmol/L) of FPC attenuated to promote cell proliferation. In contrast, the combination of TAM with higher doses (more than 20 μmol/L) of FPC showed growth inhibitory. This result was supported by immunocytochemistry studies that the administration of 20 nmol/L TAM down-regulated ER-αand c-Myc, but the combination of 20 nmol/L TAM and 1 μmol/L FPC robustly up-regulated expression of ER-α. Thus, the reduced growth inhibition of TAM 20 nmol/L by FPC 1 μmol/L on T47D cells may act via the modulation of ER-α.Conclusions:The findings indicate and suggest that FPC had estrogenic activity at low The results indicated that administration of an anti-estrogen TAM showed growth concentrations and anti-estrogenic effect that are likely to be regulated by c-Myc and estrogen receptors. We also confirm that low concentration of FPC attenuated the growth-inhibitory effects of TAM on mammary tumor prevention. Therefore, the present study suggests that caution is warranted regarding the consumption of dietary FPC by breast cancer patients while on TMA therapy.

Antidiabetic and antihiperlipidemic effect of Andrographis paniculata (Burm. f.) Nees and andrographolide in high-fructose-fat-fed rats.

OBJECTIVES: Andrographis paniculata (Burm. f.) Nees originates from India and grows widely in many areas in Southeast Asian countries. Andrographis paniculata (Burm. f.) Nees has shown an antidiabetic effect in type 1 DM rats. The present study investigates the purified extract of the plant and its active compound andrographolide for antidiabetic and antihyperlipidemic effects in high-fructose-fat-fed rats, a model of type 2 DM rats. MATERIALS AND METHODS: Hyperglycemia in rats was induced by high-fructose-fat diet containing 36% fructose, 15% lard, and 5% egg yolks in 0.36 g/200 gb.wt. 55 days. The rats were treated with the extract or test compound on the 50(th) day. Antidiabetic activity was measured by estimating mainly the pre- and postprandial blood glucose levels and other parameters such as cholesterol, LDL, triglyceride, and body weight. RESULTS: The purified extract and andrographolide significantly (P<0.05) decreased the levels of blood glucose, triglyceride, and LDL compared to controls. However, no changes were observed in serum cholesterol and rat body weight. Metformin also showed similar effects on these parameters. CONCLUSIONS: Andrographis paniculata (Burm. f.) Nees or its active compound andrographolide showed hypoglycemic and hypolipidemic effects in high-fat-fructose-fed rat.