Development of Ayurveda - Tradition to trend.

ETHNOPHARMACOLOGICAL RELEVANCE: Ayurveda entails a scientific tradition of harmonious living and its origin can be traced from ancient knowledge in Rigveda and Atharvaveda. Ayurveda is a traditional healthcare system of Indian medicine since ancient times. Several Ayurvedic medicines have been exploiting for treatment and management of various diseases in human beings. The several drugs have been developed and practiced from Ayurveda since ancient time to modern practice as 'tradition to trend'. The potential of Ayurvedic medicine needs to be explored further with modern scientific validation approaches for better therapeutic leads. AIM OF THE STUDY: The present study was aimed to explore the various aspects of Ayurveda and inspired drug discovery approaches for its promotion and development. MATERIALS AND METHODS: We have reviewed all the literature related to the history and application of Ayurvedic herbs. Various aspects for the quality control, standardization, chemo-profiling, and metabolite fingerprinting for quality evaluation of Ayurvedic drugs. The development of Ayurvedic drugs is gaining momentum with the perspectives of safety, efficacy and quality for promotion and management of human health. Scientific documentation, process validation and several others significant parameters are key points, which can ensure the quality, safety and effectiveness of Ayurvedic drugs. RESULTS: The present review highlights on the major goal of Ayurveda and their significant role in healthcare system. Ayurveda deals with several classical formulations including arka, asavas, aristas, churna, taila, vati, gutika, bhasma etc. There are several lead molecules that have been developed from the Ayurvedic herbs, which have various significant therapeutic activities. Chemo-profiling of Ayurvedic drug is essential in order to assess the quality of products. It deals with bioactive compound quantification, spurious and allied drug determination, chromatographic fingerprinting, standardization, stability and quality consistency of Ayurvedic products. CONCLUSIONS: Scientific validation and the documentation of Ayurvedic drugs are very essential for its quality evaluation and global acceptance. Therapeutic efficacy of Ayurvedic herbs may be enhanced with high quality, which can be achieved by identity, purity, safety, drug content, physical and biological properties. Ayurvedic medicines need be explored with the modern scientific approaches for its validation. Therefore, an attempt has been made in the present review to highlight the crucial aspects that need to be considered for the promotion and development of Ayurvedic medicine.

CYP450 mediated inhibition potential of Swertia chirata: An herb from Indian traditional medicine.

ETHNOPHARMACOLOGICAL RELEVANCE: An Ayurvedic herb, Swertia chirata (SC) have been used in treating various ailments such as hyperglycemia, leishmania, liver infections, inflammation, abdominal pain, bacterial infection, malaria etc. in Indian Systems of Medicine (ISM). AIM OF THE STUDY: Study was designed to investigate the inhibition potential of the standardized SC extract along with its bioactive molecule ursolic acid on hepatic drug metabolizing isozymes (CYP3A4 and CYP2D6) and further some heavy metals were also analysed of the plant material. MATERIALS AND METHODS: The hydro-alcoholic extract was standardized with standard ursolic acid by reverse phase-high performance liquid chromatography (RP-HPLC) method and the heavy metals content were analyzed through atomic absorption spectroscopy (AAS). The effect of extract on rat liver microsome (RLM) and individual CYP isozymes (CYP3A4 and CYP2D6) was investigated through CYP450-CO complex assay and fluorescence microplate assay respectively. RESULTS: The content of ursolic acid was found to be 2.66% (w/w) in the SC extract and heavy metal contents along with trace elements were within the prescribed limits as per WHO guidelines. The inhibitory potential of SC extract on RLM was found to be 23.64±1.80%. CYP3A4 and CYP2D6 inhibitory effect of SC and ursolic acid (IC50: 197.49±2.68, 211.45±3.54 and IC50: 229.25±2.52, 212.66±1.26 µg/mL) was less as compared to that known inhibitors, ketoconazole and quinidine respectively. CONCLUSIONS: The current study revealed that S. chirata has less inhibition potential with two major drug metabolizing isozymes CYP3A4 and CYP2D6. SC extract and ursolic acid showed significantly (P<0.001) less inhibitory potential on RLM. The Ayurvedic herb (SC) has shown less inhibitory activity in a concentration dependent manner against the tested two CYP450 enzymes. The tested heavy metals and trace elements present SC was within limit. Therefore, the traditional use of S. chirata may be safe in respect of both tested isozymes.

Interaction potential of Trigonella foenum graceum through cytochrome P450 mediated inhibition.

OBJECTIVE: The seeds of Trigonella foenum-graecum (TFG) (family: Leguminosae) are widely consumed both as a spice in food and Traditional Medicine in India. The present study was undertaken to evaluate the inhibitory effect of standardized extract of TFG and its major constituent trigonelline (TG) on rat liver microsome (RLM) and cytochrome P450 (CYP450) drug metabolizing isozymes (CYP3A4 and CYP2D6), which may indicate the possibility of a probable unwanted interaction. MATERIALS AND METHODS: Reverse phase-high performance liquid chromatography method was developed to standardize the hydroalcoholic seed extract with standard TG. The inhibitory potential of the extract and TG was evaluated on RLM and CYP isozymes using CYP450-carbon monoxide (CYP450-CO) complex assay and fluorescence assay, respectively. RESULTS: The content of TG in TFG was found to be 3.38% (w/w). The CYP-CO complex assay showed 23.32% inhibition on RLM. Fluorescence study revealed that the extract and the biomarker had some inhibition on CYP450 isozymes e.g. CYP3A4 and CYP2D6 (IC50 values of the extract: 102.65 ± 2.63-142.23 ± 2.61 µg/ml and TG: 168.73 ± 4.03-180.90 ± 2.49 µg/ml) which was very less compared to positive controls ketoconazole and quinidine. Inhibition potential of TFG was little higher than TG but very less compared to positive controls. CONCLUSIONS: From the present study, we may conclude that the TFG or TG has very less potential to inhibit the CYP isozymes (CYP3A4, CYP2D6), so administration of this plant extract or its biomarker TG may be safe.

Soya phospholipid complex of mangiferin enhances its hepatoprotectivity by improving its bioavailability and pharmacokinetics.

BACKGROUND: Mangiferin is a xanthonoid present in Mangifera indica. It has been reported for a variety of pharmacological activities, including hepatoprotection. However, the major disadvantage of mangiferin is its reduced biological activity due to poor absorption, low bioavailability and rapid elimination from the body after administration. The aim of this study was to prepare a phospholipid complex of mangiferin to overcome these limitations and to investigate the impact of the complex on hepatoprotective activity and bioavailability. RESULTS: The results showed that the complex has an enhanced hepatoprotective and in vivo antioxidant activity as compared to pure mangiferin at the same dose level (30 and 60 mg kg⁻¹). The complex restored the levels of serum hepatic marker enzymes and liver antioxidant enzymes with respect to carbon tetrachloride-treated animals. The complex also increased the bioavailability of mangiferin in rat serum by 9.75-fold compared to pure mangiferin at the same dose level and enhanced the elimination half-life (t(1/2 el)) from 1.71 ± 0.12 h⁻¹ to 3.52 ± 0.27 h⁻¹. CONCLUSION: The results suggested that the complexation of mangiferin with soya phospholipid enhanced the hepatoprotection and in vivo antioxidant activity, which may be due to the improved bioavailability and pharmacokinetics of mangiferin in rat serum.