Objective. Hydroalcoholic extract of Picrorhiza kurroa and its fractions were subjected to in vitro screening for cytotoxicity; further best active fraction (BAF) obtained was tested against Ehrlich ascites carcinoma (EAC) model in Balb/c mice after its quality control analysis. Methods. Cytotoxicities of all the fractions and mother extract of P. kurroa were determined, using MTT assay on breast cancer (MCF-7, MDA-MB 231) and cervical cancer (HeLa, SiHa) cell lines. Metabolic fingerprinting was developed using HPTLC with quantification of biomarkers (cucurbitacins B and E; betulinic acid; picrosides 1 and 2; and apocynin) in BAF. The EAC tumor-bearing mice were used for in vivo anticancer activity after oral administration (50 mg Kg−1) for 10 days. Results. Cytotoxicity assay of mother extract and its fractions over breast cancer and cervix cancer cell lines showed that dichloromethane (DCM) fraction was most cytotoxic (IC50 36.0–51.0 µg mL−1 at 72 h). Oral administration of DCM fraction showed significant reduction in tumor regression parameters, viable tumor cell count and restoration of hematological parameters may be due to presence of cucurbitacins B and E; betulinic acid; picrosides 1 and 2; and apocynin, as compared to the untreated mice of the control group. Conclusion. The DCM fraction of P. kurroa displayed potent anticancer activity and can be further explored for the development of a potential candidate for cancer therapy.

An attempt has been made to develop and validate a simultaneous HPLC method for novel approach of drug release via oil-in-water (o/w) nanoemulsion formulation and Habb-e-Khardal Unani tablet containing piperine and guggul sterones E and Z as main ingredients. Nanoemulsion was prepared by titration method using sefsol-218 as an oily phase, cremophor-EL as a surfactant, transcutol as a co-surfactant and distilled water as an aqueous phase. The formulation was optimized on the basis of thermodynamic stability and dispersibilty test. The nanoformulation was evaluated for particle size, surface morphology, electrical conductivity and viscosity determination. The in vitro dissolution was carried out by dialysis bag method. Drugs were quantified using an HPLC method developed in-house with a C(18) column as stationary phase and acetonitrile and water as mobile phase at λ(max) of 240 nm. The optimized formulation showed higher drug release, lower droplet size and less viscosity as compared with the conventional Habb-e-Khardal Unani tablet. The present study illustrated the potential of nanoemulsion dosage form in improving biopharmaceutic performance of piperine and guggul sterone. The HPLC method was also found to be quite sufficient for the routine quality control of formulations containing piperine and guggul sterone E and Z as ingredients and also for in vitro drug release studies.

1. The metabolism of dexrazoxane (ICRF-187) and its optical isomer levrazoxane (ICRF-186) by the isolated rat hepatocyte was studied by hplc. 2. 4-Chlorobenzenesulphonamide, which is a strong inhibitor of dihydropyrimidine amidohydrolase (DHPase), caused 82% inhibition of the loss of dexrazoxane from the hepatocyte suspension. 3. Dexrazoxane was metabolized at an initial rate by isolated hepatocytes that was 1.8 times faster than levrazoxane. This ratio is close to that found for purified DHPase, suggesting that DHPase present in the hepatocyte catalyses the ring-opening hydrolysis of these drugs. 4. The ratios of the rates at which each of the one-ring open intermediates of dexrazoxane and levrazoxane were produced in the hepatocyte suspension are also consistent with DHPase being primarily responsible for the metabolism of dexrazoxane and levrazoxane. 5. Thus, the DHPase-catalysed formation of the one-ring opened intermediates enhances the rate at which the presumably active metal-ion binding forms of dexrazoxane are produced in the hepatocyte. 6. The DHPase content of the hepatocyte was estimated to be 1.2 nmol/kg of total hepatocyte mass, or equivalently 5700 molecules of DHPase per hepatocyte.

The study investigated the growth-inhibiting and apoptosis mediating effects of B. serrata extract as monotherapy and combination therapy with DOX against hepatocellular carcinoma cell lines. Boswellic acid rich fraction of B. serrata extract was prepared. MTT assay on HepG2 and Hep3B cells was carried out using B. serrata alone and in combination with DOX. Further, caspase-3 activity, TNF-α level, and IL-6 level were estimated. Isobolographic analysis was carried out to evaluate the effect of combination therapy. Additionally, protective effect of B. serrata extract on DOX induced hepatic toxicity was also evaluated in Wistar rats. B. serrata extract inhibited growth of HepG2 (IC50 value of 21.21 ± 0.92 μg/mL) as well as HepG2 (IC50 value of 18.65 ± 0.71 μg/mL). DOX inhibited growth in HepG2 and Hep3B cells with an IC50 of 1.06 ± 0.04 μg/mL and 1.92 ± 0.09 μg/mL. Isobolographic analysis showed combination index (CI) of DOX and B. serrata extract of 0.53 ± 0.03 to 0.79 ± 0.02 suggesting synergistic behavior against the two cell lines. B. serrata extract also caused dose dependent increase in caspase-3 activity, TNF-α level, and IL-6 level which was higher (P < 0.001) with DOX (1 μM) and B. serrata extract (20 μg/mL) combination. B. serrata extract also protected Wistar rats against DOX induced hepatic toxicity.

A simple, economic, selective, precise and robust method has been developed and validated for the analysis of glabridin in crude drugs and polyherbal formulations. Reversed-phase chromatography is performed on a C18 column with water and acetonitrile as mobile phase in gradient elution method at a flow rate of 1 mL/min. Detection is performed at 230 nm and a sharp peak is obtained for glabridin at a retention time of 14.9 + + + + + 0.02 min. Linear regression analysis data for the calibration plot showed a good linear relationship between response and concentration in the range of 1-500 mg/mL; the regression coefficient is 0.9992 and the linear regression equation is y 5 26.683x-142.17. The method is validated for accuracy, precision, reproducibility, robustness and detection and quantification limits, in accordance with International Conference on Harmonization guidelines. Statistical analysis proved that the method is precise, reproducible, selective and accurate for the analysis of glabridin. The proposed, developed and validated high-performance liquid chromatography method for the quantification of glabridin can be used for the quality control and standardization of licorice (Glycyrrhiza glabra Linn.) and different herbal formulations in which licorice is present as a constituent.