6-SHOGAOL RICH GINGER OLEORESIN LOADED MIXED MICELLES ENHANCES IN VITRO CYTOTOXICITY ON MCF-7 CELLS AND IN VIVO ANTICANCER ACTIVITY AGAINST DAL CELLS

Objective: Ginger oleoresin (GO) plays an important role on the attenuation of complications associated to the cancer which is attributed to 6-shogaol (6-SGL). The major challenge in using 6-SGL for therapeutic applications is its poor aqueous solubility, low stability in GI and low bioavailability. Considering the potent anticancer nature of 6-SGL and its synergistic activity with other constituents in GO, there is a need to develop a suitable drug delivery system.Methods: Thus in the present study, 6-SGL rich GO (6-SRGO) was incorporated into mixed micelles using phospholipid (Soya Lecithin) as a carrier. The prepared 6-SRGO loaded mixed micelles (6-SRGO-LMM) were characterized physically and chemically using Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and further evaluated for stability study, in vitro release study, in vitro cytotoxicity study and in vivo anticancer activity in comparison with 6-SRGO.Results: The composition such as, drug content (86.27±1.56), encapsulation efficiency (81.55±1.05) and particle size (356.11±4.07) were optimized using 32 factorial design. FTIR and DSC study confirm that the 6-SGL from 6-SRGO was entrapped in the core of phospholipid by self-assembly method to form mixed micelles. The 6-SRGO-LMM exhibited significant in vitro (GI50-23.2 μg/ml) and in vivo anticancer activity in comparison with 6-SRGO.Conclusion: We have developed and investigated mixed micelles composed of phospholipids (soya lecithin S80) and SCH as an effective nanocarrier for the delivery of a natural lipophilic anticancer bioactive 6-SGL from 6-SRGO

STANDARDIZATION AND COMPARATIVE EVALUATION OF AYURVEDIC POLYHERBAL GHRITA FORMULATION WITH MODERN EXTRACTION TECHNIQUE FOR EXTRACTION EFFICIENCY USING REVERSED PHASE-HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY

Objective: Sarasvata ghrita (SG) is a polyherbal formulation in Ayurvedic Indian medicinal system, in which ghee is the main ingredient used for extraction. Ghee is 100% lipid, thus its regular use is limited, and there is a lack of quality control profile of SG. Thus, the objective of the study is to develop quality control method for standardization of SG and to analyze manufacturing process of SG and an effective method of extraction to extract phytoconstituents from herbs used in SG to overcome the limitation of SG.Methods: SG was processed as per the traditional method, whereas ethanolic extract (EE) and hydroalcoholic extract (HAE) were obtained by the conventional method and lipid-based extract (LE) was prepared by modern extraction method. SG and all extracts were standardized using newly developed high-performance liquid chromatography (LC) with respect to bebeerine, piperine, 6-shogaol, β-asarone, and chebulinic acid. All extracts were analyzed for pesticides, and heavy metal content by LC/mass spectrometry (MS/MS) and inductively coupled plasma/MS, respectively, screened for total polyphenols and flavonoids content, in vitro antioxidant potential, and for assessing its stability over time.Results: The better extraction was observed with maceration extraction using ethanol compared to ayurvedic method and LE method. All extracts were found to have a negligible amount of pesticide and heavy metals and found to be stable for 6 months under accelerated storage condition. Better polyphenols and flavonoid content and in vitro antioxidant potential were resulted in EE.Conclusion: EE showed a better potential in comparison with SG and LE

Comparative antioxidant potential of Withania somnifera based herbal formulation prepared by traditional and non-traditional fermentation processes

AbstractBackgroundAshwagandharishtha is a liquid polyherbal formulation traditionally prepared by fermentation process using the flowers of Woodfordia fruticosa. It contains roots of Withania somnifera as a major crude drug. Alcohol generated during the fermentation causes the extraction of water insoluble phytoconstituents. Yeasts present on the flowers are responsible for this fermentation.MethodsTotal nine formulations of ashwagandharishtha were prepared by fermentation process using traditional Woodfordia fruticosa flowers (ASG-WFS) and using yeasts isolated from the same flowers. During fermentation, kinetic of alcohol generation, sugar consumption, changes in pH and withanolides extraction were studied. All the formulations were tested for in vitro antioxidant potential by 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging, hydrogen peroxide scavenging and total reducing power assay. The results were compared with standard ascorbic acid.ResultsTraditional formulation (ASG-WFS) showed the highest activity (p < 0.001) relative to other formulations and standard ascorbic acid. ASG-WFS showed significant (DPPH) free radical scavenging (78.75%) and hydrogen peroxide scavenging (69.62%) at the concentration of 1000μg/mL and 100μg/mL, respectively.ConclusionTraditional process is the best process for preparing ashwagandharishtha to obtain significant antioxidant activity

Effect of pH and Gastrointestinal Enzymes on Stability of Psoralen, Bakuchicin and Bakuchiol using Simultaneous TLC Densitometric Method and Standardization of commercial formulations containing Psoralea cordyfollia Linn.

Psoralea corylifolia is used for treatmet of skin diseases such as psoriasis, vitiligo. Psoralen is responsible for its effectiveness against psoriasis. Bakuchicin and Bakuchiol are DNA polymerase and topoisomerase II inhibitors. To study the effect of pH and gastrointestinal (GI) enzymes on Psoralen, Bakuchicin and Bakuchiol from Psoralea corylifolia Linn using a simple, sensitive, accurate and robust high performance thin layer chromatographic (HPTLC) method. The method was performed on silica gel 60 F254with n- Hexane : Ethyl acetate ( 7.5 : 2.5 v/v)&nbsp; as the mobile phase. Densitometric scanning at 285 nm for Psoralen, Bakuchicin and Bakuchiol was used. The method was validated as per the guidelines of International Conference on Harmonization (ICH). In addition the applicability of the method was tested for the standardization of both mono and polyherbal formulations containing the above markers. The Rf values of 0.37, 0.48 and 0.63 were obtained for Psoralen, Bakuchicin and Bakuchiol respectively. The linearity range of 20-120 ng spot-1,&nbsp; 20-120 ng spot-1 and 80-280 ng spot-1&nbsp; with good correlation coefficients of r2 = 0.998, 0.998 and 0.999 were obtained for Psoralen, Bakuchicin and Bakuchiol&nbsp; respectively. The method was applied for the in vitro stability studies of above markers in simulated gastric and intestinal fluids to study the effect of pH and GI enzymes. Psoralen was found to be most stable in the simulated physiological fluids whereas other two compounds showed instability. The method was found to be precise, robust and suitable for the routine quality control analysis of plant extracts and polyherbal formulations. Keywords: Psoralea corylifolia Linn, Leguminoceae, HPTLC, Enzymatic stabilit

An experimental study of cathodic protection for chloride contaminated reinforced concrete

Cathodic protection (CP) is being increasingly used on reinforced concrete structures to protect steel reinforcing bars from corrosion in aggressive conditions. Due to the complexity of environmental conditions, the design specifications in national and international standards are still open to discussion to achieve both sufficient and efficient protection for reinforced concrete structures in engineering practices. This paper reports an experimental research to investigate the influence of chloride content on concrete resistivity, rebar corrosion rate and the performance of CP operation using different current densities. It aims to understand the correlation between the chloride content and concrete resistivity together with the CP current requirement, and to investigate the precision of the CP design criteria in standards

Trapping of Intermediates with Substrate Analog HBOCaA in the Polymerizations Catalyzer by Class III Polyhydroxybutyrate (PHB) Synthase from Allochromatium Vinosum

Polyhydroxybutyrate (PHB) synthases (PhaCs) catalyze the formation of biodegradable PHB polymers that are considered as an ideal alternative to petroleum-based plastics. To provide strong evidence for the preferred mechanistic model involving covalent and noncovalent intermediates, a substrate analog HBOCoA was synthesized chemoenzymatically. Substitution of sulfur in the native substrate HBCoA with an oxygen in HBOCoA enabled detection of (HB)nOCoA (n = 2–6) intermediates when the polymerization was catalyzed by wild-type (wt-)PhaECAv at 5.84 hr−1. This extremely slow rate is due to thermodynamically unfavorable steps that involve formation of enzyme-bound PHB species (thioesters) from corresponding CoA oxoesters. Synthesized standards (HB)nOCoA (n = 2–3) were found to undergo both reacylation and hydrolysis catalyzed by the synthase. Distribution of the hydrolysis products highlights the importance of the penultimate ester group as previously suggested. Importantly, the reaction between primed synthase [3H]-sT-PhaECAv and HBOCoA yielded [3H]-sTet-O-CoA at a rate constant faster than 17.4 s−1, which represents the first example that a substrate analog undergoes PHB chain elongation at a rate close to that of the native substrate (65.0 s−1). Therefore, for the first time with a wt-synthase, strong evidence was obtained to support our favored PHB chain elongation model

Micropropagation and conservation of selected endangered anticancer medicinal plants from the Western Ghats of India

Globally, cancer is a constant battle which severely affects the human population. The major limitations of the anticancer drugs are the deleterious side effects on the quality of life. Plants play a vital role in curing many diseases with minimal or no side effects. Phytocompounds derived from various medicinal plants serve as the best source of drugs to treat cancer. The global demand for phytomedicines is mostly reached by the medicinal herbs from the tropical nations of the world even though many plant species are threatened with extinction. India is one of the mega diverse countries of the world due to its ecological habitats, latitudinal variation, and diverse climatic range. Western Ghats of India is one of the most important depositories of endemic herbs. It is found along the stretch of south western part of India and constitutes rain forest with more than 4000 diverse medicinal plant species. In recent times, many of these therapeutically valued herbs have become endangered and are being included under the red-listed plant category in this region. Due to a sharp rise in the demand for plant-based products, this rich collection is diminishing at an alarming rate that eventually triggered dangerous to biodiversity. Thus, conservation of the endangered medicinal plants has become a matter of importance. The conservation by using only in situ approaches may not be sufficient enough to safeguard such a huge bio-resource of endangered medicinal plants. Hence, the use of biotechnological methods would be vital to complement the ex vitro protection programs and help to reestablish endangered plant species. In this backdrop, the key tools of biotechnology that could assist plant conservation were developed in terms of in vitro regeneration, seed banking, DNA storage, pollen storage, germplasm storage, gene bank (field gene banking), tissue bank, and cryopreservation. In this chapter, an attempt has been made to critically review major endangered medicinal plants that possess anticancer compounds and their conservation aspects by integrating various biotechnological tool