Anticancer efficacy of phenolics based structurally related compounds and their radical scavenging action

Cancer, one of the leading causes of death worldwide, is an abnormal cell proliferation that fails to respond to the normal signals. In an effort to eradicate the growing menace of cancer, a clear understanding of fundamental biology and molecular mechanism of carcinogenesis is essential for targeted therapies. Among the devised strategies in use for cancer treatment, the one that is of immense interest is the development of plant based novel anticancer agents. Due to their tremendous availability, biological activity and efficacy, the phytochemicals deemed a gibbous future in chemoprevention. In the present study, several phenolics based structurally related compounds of steroidal and non-steroidal skeleton were synthesized and tested for their modulatory effect on ornithine decarboxylase activity, an enzyme highly upregulated in cancer. Additionally, these compounds were also examined for radical scavenging extent to establish a correlation with the anticancer property. Our result suggests that the tested compounds possessed radical scavenging activity, for being the inherent property of the phenolics. 3-(3’,4’5’-trimethoxyphenyl)-4,5,6-trimethoxyindan-1-one oxime exhibited highest inhibition of enzyme activity (91%) followed by 1-(2,4-dibromophenyl)-3-[3-methoxyestra 1,3,5(10)-trien-17-acetate,2-yl]-2-propen-1-one (85%), 2-Hydroxy, 3-(3’,4’,5’-trimethoxy phenyl)-4,5,6-trimethoxy ind-2-en-1-one (80%), 1-(3,4-methylenedioxyphenyl)-3-(3,4,5-trimethoxyphenyl)-2-propen-1-one (74%) and 1-(3,-methoxy, 4-hydroxyphenyl)-3-[3-methoxyestra 1,3,5(10)-trien-17-acetate, 2-yl]-2-propen-1-one (67%). Furthermore, it was observed that 1-(3-Methoxy, 4- hydroxyphenyl)-3-[3-methoxyestra 1,3,5 (10)-trien-17-acetate, 2-yl]-2-propen-1-one showed the highest scavenging effect (67%) in nitric oxide assay, whereas 1-(3-methylphenyl)-3-[3-methoxy, 17-hydroxyestra 1,3,5(10)-trien, 2-yl]-2-propen-1-one showed maximum inhibition of radical formation in 2,2-diphenyl-1-picrylhydrazyl analysis. Most of these compounds possessed a 3,4,5-trimethoxyphenyl unit which might be inducing enzyme inhibition and scavenging radical formation. Further investigations are on the way to establish the structure-activity relationship, so that these compounds can be developed as anticancer agents

QSAR and Docking Studies of Gallic Acid Derivatives for Anticancer and Immunomodulatory Activity

Immuno-modulation is the process of alteration in immune response due to foreign intrusion of molecules inside the body. In the present communication QSAR and molecular docking studies for immuno-modulatory activity of derivatives of gallic acid were performed. Molecular docking studies showed higher binding affinity with INFα-2, IL-6, and IL-4 receptors. Binding site residues indicate hydrogen bonds formation with gallic acid derivative compounds G-3, G-4, G-5, G-6, G-7 and G-10. Further screening through quantitative structure activity relationship model establishes the immuno-modulatory activity of the compounds G-4, G-7, G-9, G-10, G-12 and G-13. Activity was predicted through a robust statistical model, developed by forward feed multiple linear regression method with leave-one-out approach. Relationship correlating measure (r2) and prediction accuracy (rCV2) of QSAR model were 0.99 and 0.96, respectively. QSAR studies indicate that dipole moment, steric energy, amide group count, λ max (UV-visible) and molar refractivity correlate well with their activities, while decrease in dipole moment, steric energy and molar refractivity have negative correlation. Moreover, on the basis of bioavailability, in-silico ADME and toxicity risk assessment screening, we concluded that compounds G-4, G-7, G-9, G-10, G-12 and G-13 have marked immuno-modulatory activity comparable to standard drugs

Antidiabetic Potentials of Various Ethno-Medicinal Plants of Rajasthan

Diabetes Mellitus is a syndrome of disordered metabolism, due to a combination of hereditary and environmental causes, resulting in abnormally high blood sugar levels (hyperglycemia), caused by defects in either insulin secretion or insulin action in the body. Diabetes epidemic is underway. Currently available therapeutic options for non-insulin-dependent diabetes mellitus such as dietary modification, oral hypoglycemics and insulin have a lot potentials to cure diabetes. Now-a-days natural products and herbal medicines have been recommended for the treatment of diabetes. The present paper is an attempt to list of the plants and their preparations used for cure of diabetes with Ethnomedicinal backgrounds with the list of plants experimental or clinically listed from Rajasthan (arid zone) with antidiabetic potentials. The review also include the various preparations which can safely used to cure diabetes in the form of daily diet as plant potentials for future generations. The studies are a move towards awareness towards changing our diet system with potential input of Ethnomedicinal knowledge to cure the incidence of diabetes

PHARMACOGNOSTICAL STUDIES AND PRELIMINARY PHYTOCHEMICAL INVESTIGATION ON THE BARK OF BAUHINIA VARIEGATA (CAESALPINIACEAEA)

Bauhinia variegata (Family - Caesalpiniaceaea) is a medium-sized, deciduous tree, found throughout India, ascending to an altitude up to 1800m in Himalayas. The objective of the study was to develop various standardization parameters for the evaluation of Bark of this plant. Microscopy, powder characteristics of bark were observed and results were recorded. Physicochemical analysis such as extractive value includes petroleum ether, ethanol, ethyl acetate and aqueous soluble extractive values of 2.88, 6.86, 2.96, and 8.88% w/w respectively; extracts were analysed by chemical test and showed presence of flavonoids, tannins, steroids and triterpenoids etc. The preliminary phytochemical investigation indicated presence of tannins, carbohydrates, flavenoieds and steroids. The results obtained from standardization of bark established the macro and microscopical parameters, physicochemical parameters, TLC profiles that characterize the genuine plant drug (B.variegata) so these parameters are useful for quick identification of drug and are particularly useful in the case of powdered materials

Desorption of artemisinin extracts of CIM-Arogya by supercritical carbon dioxide

Artemisinin is a drug for chloroquine resistant malaria and cerebral malaria treatments. In the recent past, there was an acute shortage of this drug and hence World Health Organization made a strategy to fulfil the Artemisinin demand. In this study, artemisinin was extracted by supercritical Carbon Dioxide (SFCO2) from CIM-Arogya, a variety of Artemisia annua, in temperature and pressure ranges of 313.1-333.1 K and 15\u201325 MPa. Artemisinin global yield isotherms were determined obtaining a maximum yield of 3.65 wt%. Artemisinin extracts were also obtained by hexane Soxhlet extraction: then, the crude extracts were purified using SFCO2, after adsorption on silica gel. Different desorption runs were performed with a 6 ml/min CO2 flow rate, in temperature and pressure ranges of 313.1\u2013333.1 K and 15\u201325 MPa. At different time intervals, extracts were collected and analysed: their yields varied from 2.75% to 4.34% function of the experimental conditions. Desorption trials were also correlated with different models

Biotransformation of artemisinin mediated through fungal strains for obtaining derivatives with novel activities

Artemisinin, a sesquiterpene lactone, is the active antimalarial constituent of Artemisia annua. Several fungal strains Saccharomyces cerevisiae, Aspergillus flavus, Aspergillus niger and Picchia pastoris were used to biotransform artemisinin. Among these strains, A. flavus was the only microorganism capable of transforming artemisinin to deoxyartemisinin in higher yields than the previous reports. The structure of deoxyartemisinin was elucidated by spectroscopy. Deoxyartemisinin showed antibacterial activity against Staphylococcus aureus, S. epidermidis and S. mutans at a minimum inhibitory concentration (MIC) of 1 mg/mL compared to artemisinin whose MIC was >2 mg/mL

Traditional knowledge for dairy animals in Una district of Himachal Pradesh

662-668Traditional knowledge (TK), also known as indigenous knowledge (IK) or local knowledge (LK) generally refers to the matured long-standing traditions and practices of certain regional, indigenous, or local communities. India stands at number 1 in milk production as dairy master across the world. However, due to large number of animal population, distant/remote location, shortage of veterinary staff, some time, veterinary aids are not available to the farmers. In such instances, it is the traditional knowledge of the people which guides them to mitigate the sufferings of the animals. In this article, some of the ITKs are described based on oral communication with the people

Traditional knowledge for dairy animals in Una district of Himachal Pradesh

Traditional knowledge (TK), also known as indigenous knowledge (IK) or local knowledge (LK) generally refers to the matured long-standing traditions and practices of certain regional, indigenous, or local communities. India stands at number 1 in milk production as dairy master across the world. However, due to large number of animal population, distant/remote location, shortage of veterinary staff, some time, veterinary aids are not available to the farmers. In such instances, it is the traditional knowledge of the people which guides them to mitigate the sufferings of the animals. In this article, some of the ITKs are described based on oral communication with the people

Bioactive isochromenone isolated from Aspergillus fumigatus, endophytic fungus from Bacopa monnieri

Fungal endophytes are a significant reservoir of novel bioactive secondary metabolites. Present communication describes isolation and structure determination of isochromenone, from endophytic microorganism Aspergillus fumigatus hosted in Bacopa monnieri plant. Further, its biological evaluation revealed it as antioxidant and antitubercular. The methanol extract of A. fumigatus inhibits the growth of the virulent strain of Mycobacterium tuberculosis H37RV with minimum inhibitory concentration 500 μg/mL. This is the first report of isolation of isochromenone from A. fumigatus.</em

In vitro production of steroidal saponin, total phenols and antioxidant activity in callus suspension culture of Paris polyphylla Smith: an important Himalayan medicinal plant

Paris polyphylla Smith (Melanthiaceae) family, which is native to the Himalayan region, has received a lot of attention recently due to its extensive history of usage in traditional medicine. The production of steroidal saponin from callus suspension cultures of P. polyphylla was observed in the current study. The current study attempted to develop a P. polyphylla plant callus suspension culture through optimization of cultivation technique for callus suspension, quantification of total phenolic components and estimation of the extract’s antioxidant activity. A light-yellow callus was formed within six weeks of cultivating rhizomes on Murashige and Skoog (MS) media supplemented with Thidiazuron (TDZ). Furthermore, the effect of TDZ, Methyl Jasmonate (MeJA), and Yeast Extract (YE) on callus growth, steroidal saponin (dioscin and diosgenin), total phenolic content, total flavonoids, total tannin, and total antioxidant activity was also measured. The medium containing 0.5 μM TDZ depicted the maximum callus biomass (2.98 g fresh weight). Significantly high phenolic and tannin content was observed in the MS medium containing 50 μM MeJA, whereas, no significant increase was observed in total tannin production in any treatment. Three in vitro assays, DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2′-azino-bis (3-ethylbenzothiazoline- 6-sulfonic acid)) and FRAP (ferric ion reducing antioxidant potential) and FC (Folin-Ciocalteu), were used to assess antioxidant potential of callus. Maximum antioxidant analysis reported in 1.0 μM TDZ (6.89 mM AAE/100 g) containing medium followed by 50 μM MeJA (6.44 mM AAE/100 g). The HPLC analysis showed a high presence of dioscin and diosgenin (5.43% and 21.09%, respectively) compared to the wild sample (2.56% and 15.05%, respectively). According to the results, callus produced on media supplemented with 50 μM MeJA have significant phenolic contents and elevated antioxidant activity; nevertheless, callus growth was greater in the presence of 0.5 μM TDZ. The findings of the current study have commercial implications since greater biomass production will result in active phytochemicals that the pharmaceutical and nutraceutical sectors are in need desperately