Suppressive effects of Mimosa pudica (L.) constituents on the production of LPS-induced pro-inflammatory mediators

The present study deals with the isolation of fourteen compounds from the active ethyl acetate (MPE) extract of M. pudica (L.) whole plant and their subsequent evaluation for the nitric oxide (NO), tumor necrosis factor alpha (TNF-α) and interleukin 1 beta (IL-1β) inhibitory activities in lipopolysaccharide (LPS) stimulated RAW 264.7 and J774A.1 cells. Among the tested compounds, L-mimosine (12; IC50= 19.23 to 21.15 μM), crocetin (4; IC50= 23.45 to 25.57 μM), crocin (14; IC50= 27.16 to 31.53 μM) and jasmonic acid (11; IC50= 21.32 to 29.42 μM) were identified as potent NO inhibitor when tested on the macrophages. Similarly, towards TNF-α and IL-1β inhibition, including these four compounds, and ethyl gallate (3), gallic acid (10) and caffeic acid (7) were found to be more active with half maximal concentration, 17.32 to 62.32 μM whereas the other compounds depicted moderate and mild effects (IC50= 59.32 to 95.01 μM). Also, at a dose of 40 mg/Kg, L-mimosine (12), jasmonic acid (11), crocin (14) and its de-esterified form, crocetin (4) were found to significantly (p < 0.05 and 0.001) reduce 60.7 %, 48.9 %, 48.4 % and 43.6 % respectively of TNF-α production in female Sprague Dawley rats. However, in case of IL-1β, with the same dose (40 mg/Kg), jasmonic acid (11) exhibited significant reduction with 54.2 % followed by crocin (14) (50.2 %) and crocetin (4) (39.8 %) while L-mimosine (12) was found to reduce only 16.3 %. Based on the results, it can be estimated that these compounds imparting greatly to anti-inflammatory effects of M. pudica in vitro as well as in vivo through reduction of LPS-induced pro-inflammatory mediators which affirm the ethno-pharmacological use of this plant for prevention of inflammatory-related disorders

Investigations on Leucas cephalotes (Roth.) Spreng. for inhibition of LPS-induced pro-inflammatory mediators in murine macrophages and in rat model

Silica gel column chromatography fractionation of the dichloromethane extract (LCD) of Leucas cephalotes (Roth.) Spreng. led to the isolation of five compounds namely β-sitosterol (1) + stigmasterol (2), lupeol (3), oleanolic acid (4) and laballenic acid (5). Also, gas chromatography-mass spectrometry (GC-MS) analysis of sub-fraction (LCD-F1) of this extract showed the presence of eleven (6-16) compounds. In addition to this, 3-5 and LCD-F1 were evaluated for lipopolysachharide (LPS)-induced nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in RAW 264.7 and J774A.1 cells. Results directed that 4 and 5 were found to inhibit these mediators at half maximal inhibitory concentration of 17.12 to 57.20 μM while IC50 for LCD-F1 was found to be 15.56 to 31.71 μg/mL. Furthermore, LCD at a dose of 50, 100 and 400 mg/Kg was found to reduce significantly LPS induced tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in female Sprague Dawley (SD) rats. All the results findings evoked that the anti-inflammatory effects of Leucas cephalotes is partially mediated through the suppression of pro-inflammatory mediators and hence can be utilized for the development of anti-inflammatory candidates

Inhibitors of pancreatic lipase

Obesity is a disorder of lipid metabolism and continues to be a global problem, ranking fifth for deaths worldwide. It also leads to diabetes, cardiovascular disorders, musculoskeletal disorders and some types of cancer. Obesity is regarded as the output of a long-term imbalance between energy intake and energy expenditure. Digestion and absorption of dietary lipids by pancreatic lipase, a major source of excess calorie intake, can be targeted for development of anti-obesity agents. Being the major factor of concern, food materials and edible plants are most widely studied for the anti-obesity activity, so that they can be incorporated in the routine diet. In this review, an attempt was made to present a current scenario of the bioactive compounds from plant and microbial origin that have been investigated for their pancreatic lipase inhibition. Compounds belonging to various classes of natural products such as alkaloids, carotenoids, glycosides, polyphenols, polysaccharides, saponins and terpenoids are well studied while lipophilic compounds from microbial sources are the most active against the pancreatic lipase. Few studies on the synthetic analogues, structurally similar to the triglycerides have been described in the review. Despite of tremendous research on the finding of potential pancreatic lipase inhibitor, very few compounds have entered the clinical studies and no new molecule after orlistat has been marketed. Along with HTS based screening, detailed structure-activity relationship studies on semi-synthetic and synthetic derivatives might also provide a direction for the development of potential lead(s) or pharmacophore for pancreatic lipase inhibition in order to treat and/or prevent obesity and related disorders

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