Vishākhapatnam, India
Vishākhapatnam, India

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PubMed | University of Insubria, Vassar College, Natsol Laboratories Private Ltd and University of Camerino
Type: | Journal: Journal of inorganic biochemistry | Year: 2016

The antitumor activity of ruthenium(II) arene (p-cymene, benzene, hexamethylbenzene) derivatives containing modified curcumin ligands (HCurcI=(1E,4Z,6E)-5-hydroxy-1,7-bis(3,4-dimethoxyphenyl)hepta-1,4,6-trien-3-one and HCurcII=(1E,4Z,6E)-5-hydroxy-1,7-bis(4-methoxyphenyl)hepta-1,4,6-trien-3-one) is described. These have been characterized by IR, ESI-MS and NMR spectroscopy. The X-ray crystal structure of HCurcI has been determined and compared with its related Ru complex. Four complexes have been evaluated against five tumor cell lines, whose best activities [IC


PubMed | Acharya Nagarjuna University, Natsol Laboratories Private Ltd and Andhra University
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2016

A series of 20 hispolons/dihydrohispolons were synthesized and characterized by spectral data. These compounds were subjected to in vitro antitubercular activity screening against Mycobacterium tuberculosis (H37Rv) strain. The synthesized compounds showed varied antitubercular activity ranging from 100 to 1.6g/mL. Among the screened compounds, four compounds (H1, H2, H3 and H15) have shown moderate activity with MIC 25g/mL. Potent activities were observed for the dihydrohispolon derivative H14 (MIC 1.6g/mL) followed by H13 (6.25g/mL) and H17 (12.5g/mL), H19 (3.125g/ML). Docking simulations gave good insights on the possible interactions between the tested compounds and -keto acyl synthase enzyme (mtbFabH). Drug-inhibitor combination studies showed no synergism with the drugs targeting mycolic acid biosynthesis (isoniazid, ethambutol and thiolactomycin, a specific inhibitor of KAS-B enzyme) but showed significant synergism with other drugs including rifampicin and ciprofloxacin ascertaining the drug target for hispolons as inhibition of mycolic acid biosynthesis, probably via mtbFabH.


Balaji N.V.,Natsol Laboratories Private Ltd | Ramani M.V.,Natsol Laboratories Private Ltd | Viana A.G.,Tuskegee University | Sanglard L.P.,Tuskegee University | And 8 more authors.
Bioorganic and Medicinal Chemistry | Year: 2015

Phytochemicals play an important role in cancer therapy. Hispolon and 26 of its analogs (9 known and 17 new) were synthesized and evaluated for their antiproliferative activities in a panel of six independent human cancer cell lines using the in vitro cell-based MTT assay. Among the hispolon analogs tested, compound VA-2, the most potent overall, produced its most significant effect in the colon cancer cell lines HCT-116 (IC50 1.4 ± 1.3 μM) and S1 (IC50 1.8 ± 0.9 μM) compared to its activity in the normal HEK293/pcDNA3.1 cell line (IC50 15.8 ± 3.7 μM; p <0.01 for each comparison). Based on our results, VA-2 was about 9- to 11-times more potent in colon cancer cells and 2- to 3-times more potent in prostate cancer cells compared to HEK293/pcDNA3.1 cells. Morphological analysis of VA-2 showed significant reduction of cell number, while the cells' sizes were also markedly increased and were obvious at 68 h of treatment with 1 μM in HCT-116 (colon) and PC-3 (prostate) cancer cells. A known analog, compound VA-4, prepared by simple modifications on the aromatic functional groups of hispolon, inhibited prostate and colon cancer cell lines with IC50 values <10 μM. In addition, hispolon isoxazole and pyrazole analogs, VA-7 and VA-15 (known), respectively, have shown significant activity with the mean IC50 values in the range 3.3-10.7 μM in all the cancer cell lines tested. Activity varied among the analogs in which aromatic functional groups and β-diketone functional groups are modified. But the activity of analogs VA-16 to VA-27 was completely lost when the side chain double-bond was hydrogenated indicating the crucial role of this functionality for anticancer activity. Furthermore, many of the compounds synthesized were not substrates for the ABCB1-transporter, the most common cause of multidrug resistance in anti-cancer drugs, suggesting they may be more effective anticancer agents. ©2015 Elsevier Ltd. All rights reserved.


Rambabu A.,Acharya Nagarjuna University | Kumari K.J.,Acharya Nagarjuna University | Baby Ramana M.,Acharya Nagarjuna University | Ramani M.V.,Natsol Laboratories Private Ltd | And 2 more authors.
Asian Journal of Chemistry | Year: 2016

Apigenin and luteolin are the antioxidant flavonoids found in foods such as parsley, artichoke, basil and celery. Both of these compounds have shown the ability to protect cells against cancer and also to inhibit DNA oxidative damage. These flavonoids are part of many nutraceutical formulations available in the market. There is a need for the development of cost effective methodologies to produce them in large quantities. The synthetic process developed for both these compounds is general and can be applied for other flavonoids also. An industrially applicable high pure product, cost effective synthesis and general synthetic method has been developed and presented.


Trademark
Natsol Laboratories Private Ltd | Date: 2011-11-18

dietetic food or beverages adapted for medical use containing flavonols, dietary supplements containing flavonols.


PubMed | University of Mississippi, Tuskegee University, Biopharmatech Consulting Inc. and Natsol Laboratories Private Ltd
Type: Journal Article | Journal: Bioorganic & medicinal chemistry | Year: 2015

Phytochemicals play an important role in cancer therapy. Hispolon and 26 of its analogs (9 known and 17 new) were synthesized and evaluated for their antiproliferative activities in a panel of six independent human cancer cell lines using the in vitro cell-based MTT assay. Among the hispolon analogs tested, compound VA-2, the most potent overall, produced its most significant effect in the colon cancer cell lines HCT-116 (IC 1.4 1.3 M) and S1 (IC 1.8 0.9 M) compared to its activity in the normal HEK293/pcDNA3.1 cell line (IC 15.83.7 M; p<0.01 for each comparison). Based on our results, VA-2 was about 9- to 11-times more potent in colon cancer cells and 2- to 3-times more potent in prostate cancer cells compared to HEK293/pcDNA3.1 cells. Morphological analysis of VA-2 showed significant reduction of cell number, while the cells sizes were also markedly increased and were obvious at 68 h of treatment with 1 M in HCT-116 (colon) and PC-3 (prostate) cancer cells. A known analog, compound VA-4, prepared by simple modifications on the aromatic functional groups of hispolon, inhibited prostate and colon cancer cell lines with IC values <10 M. In addition, hispolon isoxazole and pyrazole analogs, VA-7 and VA-15 (known), respectively, have shown significant activity with the mean ICv values in the range 3.3-10.7 M in all the cancer cell lines tested. Activity varied among the analogs in which aromatic functional groups and -diketone functional groups are modified. But the activity of analogs VA-16 to VA-27 was completely lost when the side chain double-bond was hydrogenated indicating the crucial role of this functionality for anticancer activity. Furthermore, many of the compounds synthesized were not substrates for the ABCB1-transporter, the most common cause of multidrug resistance in anti-cancer drugs, suggesting they may be more effective anticancer agents.

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