Standardization of a Polyherbal <i>Ayurvedic </i>Formulation: <i>Ayaskrti</i>

589-593The present study deals with standardization of ayaskrti, known to be effective in adhmana (flatulence with gargling sound), pandu (anaemia), sula (pain), parsvasula (intercostals neuralgia and pleurodynia), diabetes, piles, lithnotriptic, anorexia, worms, malabsorption, diarrhoea and obesity. Formulation has been standardized by following modern scientific quality control procedures for the finished product according to the Ayurvedic pharmacopoeia such as organoleptic study, physic-chemical analysis and high performance thin layer chromatoghaphy (HPTLC). The obtained values of physical and chemical parameters can be adopted to lay down new standards for analysis of ayaskrti to check batch to batch variation. Quantitative evaluation of gallic acid in ayaskrti by HPTLC found to be in the range of 8.10 to 8.29 g/ml

Natural products drug discovery research in India: Status and appraisal

199-207Discovery of a new drug is time consuming and laborious process. Natural products have long been a thriving source for the discovery of new drugs due to their chemical diversity and ability to act on various biological targets. The phytochemical exploration of indigeneous flora has contributed to some extent in this race for the discovery of new drugs. The traditional Indian systems of medicine has been a part of our lifestyle since ages and the classical texts like Ayurveda and Charak Samhita have served as materia medica for this purpose. This review focuses on the contributions made from India in the drug discovery and development process and provides future directions in the area

A review on biological sources, chemistry and pharmacological activities of pinostrobin

<p>Pinostrobin, a dietary bioflavonoid discovered more than 6 decades ago in the heart-wood of pine (<i>Pinus strobus</i>), has depicted many pharmacological activities including anti-viral, anti-oxidant, anti-leukaemic, anti-inflammatory and anti-aromatase activities. It is an inhibitor of sodium channel and Ca²⁺ signalling pathways and also inhibits intestinal smooth muscle contractions. In spite of the fact that pinostrobin has an application as functional foods, till-to-date no comprehensive review on pinostrobin has been carried out. Hence, the present review deals with the biological sources, chemistry and pharmacological activities of pinostrobin.</p

Fate of Embelin in Pippalyadi Yoga, an Ayurvedic oral contraceptive: Structure of Embelin-borax complex and evaluation of anti-fertility activity

320-325In the present communication, is reported the existence of embelin 1 as embelin-borax complex 3 in a stoichiometry of 1:2 in an Ayurvedic formulation Pippalyadi Yoga. The structure of the complex is established on the basis of spectral data and it is concluded that both the phenolic oxygens as well as carbonyl groups of embelin are involved in complex formation. Embelin-borax complex is stable under basic conditions; however, it is sensitive to acidic conditions and breaks up to yield embelin and borax on treatment with mild acids. Anti-fertility activity of formulation and individual constituents was evaluated at cellular and hormonal level in Sprague Dawley female albino rats. Pippalyadi Yoga showed better activity than any of the individual constituents in the formulation including the complex

<i><span style="font-size:15.0pt;font-family:"Times New Roman","serif";mso-fareast-font-family: "Times New Roman";color:black;mso-ansi-language:EN-US;mso-fareast-language: EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">Kalyanaka ghrita</span></i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">: an example of intertextuality among the<span style="font-size:15.0pt; font-family:"Times New Roman","serif";mso-fareast-font-family:"Times New Roman"; color:black;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">Bower </span></i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">manuscript,<span style="font-size:15.0pt; font-family:"Times New Roman","serif";mso-fareast-font-family:"Times New Roman"; color:black;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">Charak samhita</span></i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">, <i>Susruta samhita</i>,<span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <i><span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">Astangahrdayam samhita</span></i><span style="font-size:15.0pt;font-family:"Times New Roman","serif";mso-fareast-font-family: "Times New Roman";color:black;mso-ansi-language:EN-US;mso-fareast-language: EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">and<span style="font-size:15.0pt; font-family:"Times New Roman","serif";mso-fareast-font-family:"Times New Roman"; color:black;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <i style="mso-bidi-font-style:normal"><span style="font-size:15.0pt; font-family:"Times New Roman","serif";mso-fareast-font-family:"Times New Roman"; color:black;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: AR-SA;mso-bidi-font-weight:bold" lang="EN-US">Ayurvedic</span></i><span style="font-size:15.0pt;font-family:"Times New Roman","serif";mso-fareast-font-family: "Times New Roman";color:black;mso-ansi-language:EN-US;mso-fareast-language: EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> Formulary of India<span style="font-size:15.0pt; font-family:"Times New Roman","serif";mso-fareast-font-family:"Times New Roman"; color:black;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: AR-SA;mso-bidi-font-weight:bold" lang="EN-US"> <span style="font-size:15.0pt;font-family:"Times New Roman","serif"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA;mso-bidi-font-weight:bold" lang="EN-US">(AFI)</span></span></span></span></span></span></span></span></span></span></span></span>

519-524This critical and careful study aimed to gather information on the common formulation(s) found in the following ancient medical texts: the<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black;letter-spacing: -.1pt" lang="EN-US"> <span style="font-size: 9.0pt;color:black;letter-spacing:-.1pt;mso-bidi-font-style:italic" lang="EN-US">Bower Manuscript<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black;letter-spacing: -.1pt" lang="EN-US"> (Bower Ms.),<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Charak Samhita (CS),<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Susruta Samhita<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black;letter-spacing: -.1pt" lang="EN-US"> (SS),<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Astangahrdayam Samhita (AHS) and Ayurvedic Formulary of India<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> (AFI). We found that only one formulation,<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Kalyanaka ghrita, had the same formula in all the texts.<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Kalyanaka ghrita was prepared according to the formula provided in the AFI and in the ancient classical texts. The prepared<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black; letter-spacing:-.1pt" lang="EN-US"> ghrita was examined by high performance thin layer chromatography and then compared with commercial<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Triphala Churna<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black;letter-spacing: -.1pt" lang="EN-US"> with respect to chemical markers. We identified a connection among the<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> Bower Ms.,<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> CS,<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> SS,<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> AHS<span style="font-size:8.0pt;mso-bidi-font-size: 9.0pt;color:black;letter-spacing:-.1pt" lang="EN-US"> and AFI.<span style="font-size:8.0pt;mso-bidi-font-size:9.0pt;color:black; letter-spacing:-.1pt" lang="EN-US"> </span

Activity-guided investigation of <i>Carissa carandas</i> (L.) roots for anti-inflammatory constituents

<div><p>The present study was structured to investigate the anti-inflammatory potential of the extracts, fractions and compounds isolated from <i>Carissa carandas</i> (L.) roots. Bioassay guided fractionation of methanol extract based on inhibitory potential towards proinflammatory mediators (TNF-α, IL-1β and nitric oxide (NO)) led to the identification of stigmasterol (<b>1</b>), lupeol (<b>2</b>), oleanolic acid (<b>3</b>), carissone (<b>4</b>) and scopoletin (<b>5</b>) as potential anti-inflammatory agents. Carissone (<b>4</b>) (IC₅₀ = 20.1 ± 2.69 μg/mL) and scopoletin (<b>5</b>) (IC₅₀ = 24.6 ± 1.36 μg/mL) exhibited significant inhibition of NO production comparable to specific NO inhibitor (L-NAME; IC₅₀ = 19.82 ± 1.64 μg/mL) without affecting the cell viability. Also, <b>4</b> and <b>5</b> at a concentration of 30 μM were found to inhibit 41.88–53.44% of TNF-α and IL-1β. To the best of our knowledge, this is the first report displaying the anti-inflammatory effects of <i>C. carandas</i> (L.) roots, partially mediated by inhibition of TNF-α, IL-1β and NO.</p></div

Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity

265-268Aryl hydrazine and hydrazide analogues were synthesized based on p-tolyl hydrazine, isolated as a breakdown product of a secondary metabolite from the mushroom, Agaricus bisporus, and tested to be highly active molecule than 5-fluorouracil in in vitro anticancer studies. The synthesized analogues were tested for anticancer activity using NCI protocol. Anolgues 12 and 15 emerged as molecules with significant in vitro anticancer activity. Molecular docking study revealed the binding orientations of aryl hydrazines and hydrazides analogues in the active sites of thymidylate synthase

Online antioxidant activity and ultra-performance LC-electrospray ionisation-quadrupole time-of-fight mass spectrometry for chemical fingerprinting of Indian polyherbal formulations

<div><p>A HPLC–DAD–DPPH method was developed for evaluating the 1, 1-diphenyl-2-picryl hydrazyl free radical scavenging activity of ethylacetate extracts of different polyherbal formulations (draksarista, draksava, lohasava and arvindasava) by using RP-18e column. The ethylacetate extract from polyherbal, ‘draksarista’ exhibited maximum free radical scavenging activity (99.9 ± 0.38%) followed by draksava (99.8 ± 0.34%), lohasava (98.5 ± 0.30%) and arvindasava (42.3 ± 0.34%) at 100 μg mL^− 1. Simultaneously, ultra-performance liquid chromatography coupled with electrospray ionisation-quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOF-MS) was used to study chemical composition of the ethylacetate extracts of formulations. The characteristic electrospray mass ionisation reveals the dominance of polyphenols and their glycosides in the four polyherbal formulations.</p></div

Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols

Plants are an important source of a variety of bioactive compounds with different modes of action. Anti-HIV agents from plant sources can be useful in developing novel therapies for inhibiting HIV infection. Based on the reported anti-HIV activity of plant derived phloroglucinols, several new dimeric phloroglucinols were synthesized in the present study by varying substitution on aromatic ring and at methylene bridge. Some of the synthesized compounds have shown good HIV inhibitory activity in a human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL4.3 virus isolate. Structure–activity studies indicate that phenyl, 4-benzyloxy-1-phenyl and cyclohexyl substitution at methylene bridge gave compounds with better anti-HIV activity. Compounds 22 and 24 showed highest anti-HIV activity with an IC50 of 0.28 μM and 2.71 μM, respectively, former was more active than the positive standard AZT in cell based assay