ABSTRACT
Dimedone derivatives (L1-L4) with methyl substitution at the ortho, para and meta positions were synthesized and their anti-radical, photoreactive and photostability activities were evaluated. All compounds are characterized by spectroscopic techniques and by single crystal X ray diffraction. UV exposure experiments on pBR322 showed inhibition of plasmid DNA fragmentation by UV radiation in a dose dependent manner. Radical scavenging assays and ESR spectra indicate that these compounds possess antiradical activities and do not photodegrade to form other side products as confirmed by chromatographic analysis. They are non-cytotoxic towards human keratinocyte HaCaT cell line indicates their potentiality in sunscreens.
Subject(s)
Cyclohexanones/pharmacology , Free Radical Scavengers/pharmacology , Keratinocytes/drug effects , Sunscreening Agents/pharmacology , Cell Line , Crystallography, X-Ray , Cyclohexanones/chemical synthesis , Cyclohexanones/chemistry , DNA Fragmentation/drug effects , DNA Fragmentation/radiation effects , Dose-Response Relationship, Drug , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/chemistry , Humans , Keratinocytes/radiation effects , Plasmids , Spectrum Analysis , Structure-Activity Relationship , Sunscreening Agents/chemical synthesis , Sunscreening Agents/chemistryABSTRACT
Breast cancer is one of the most common cancers among women in India and around the world. Despite recent advancement in the treatment of breast cancer, the results of chemotherapy to date remain unsatisfactory, prompting a need to identify natural agents that could target cancer efficiently with least side effects. Andrographolide (Andro) is one such molecule which has been shown to possess inhibitory effect on cancer cell growth. In this study, Andro, a natural diterpenoid lactone isolated from Andrographis paniculata has been shown to inhibit breast cancer cell proliferation, migration and arrest cell cycle at G2/M phase and induces apoptosis through caspase independent pathway. Our experimental evidences suggest that Andro attenuates endothelial cell motility and tumor-endothelial cell interaction. Moreover, Andro suppresses breast tumor growth in orthotopic NOD/SCID mice model. The anti-tumor activity of Andro in both in vitro and in vivo model was correlated with down regulation of PI3 kinase/Akt activation and inhibition of pro-angiogenic molecules such as OPN and VEGF expressions. Collectively, these results demonstrate that Andro may act as an effective anti-tumor and anti-angiogenic agent for the treatment of breast cancer.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Breast Neoplasms/drug therapy , Diterpenes/pharmacology , Down-Regulation/drug effects , Osteopontin/metabolism , Plant Extracts/pharmacology , Andrographis/chemistry , Animals , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/therapeutic use , Apoptosis/drug effects , Breast Neoplasms/pathology , Cell Line, Tumor , Cell Movement/drug effects , Cell Survival/drug effects , Coculture Techniques , Diterpenes/isolation & purification , Diterpenes/therapeutic use , Female , G2 Phase Cell Cycle Checkpoints/drug effects , Gene Expression/drug effects , Gene Expression Regulation, Neoplastic/drug effects , Human Umbilical Vein Endothelial Cells/drug effects , Human Umbilical Vein Endothelial Cells/physiology , Humans , Mice , Mice, Inbred NOD , Mice, SCID , Osteopontin/genetics , Phosphatidylinositol 3-Kinases/metabolism , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use , Proto-Oncogene Proteins c-akt/metabolism , Signal Transduction , Tumor Burden/drug effects , Tumor Microenvironment/drug effects , Xenograft Model Antitumor AssaysABSTRACT
Herbs have been used for medicinal purposes for centuries. According to recent investigations, they may help reduce the risk of chronic diseases, cardiovascular disease, and cancer due to antioxidant properties, which in turn can be attributed to the various phytoconstituents. With this intention, evaluation of antioxidant activity was performed. Methanol extract of aerial parts of Artemisia pallens Wall was screened for its antioxidant activity due to phenolic and flavonoid contents, by employing radical scavenging assays; 2,2 -diphenyl, 1-picryl hydrazyl (DPPH) and nitric oxide. Ascorbic acid was used as a standard. Quantitative determination of phenols and flavonoids were carried out using spectrophotometric method. Total flavonoid content was determined as quercetin equivalent and total phenolic content was determined as pyrocatechol equivalent using Folin-Ciocalteu reagent. Plant produces more phenolic compounds than flavonoids. IC(50) value of methanol extract for DPPH free radical scavenging activity was found to be 292.7 µg, whereas for nitric oxide it was 204.61 µg. The result obtained in the present study indicates that the aerial parts of this plant are a rich source of natural antioxidants.
ABSTRACT
In the title compound, C(18)H(16)O(6), the dimethoxy-phenyl ring is rotated by 61.8â (1)° from the plane of the benzopyran system. The mol-ecule is stabilized by an intra-molecular O-Hâ¯O hydrogen bond.
ABSTRACT
Using enantiopure 7-azabicyclo[2.2.1]heptane-2-ol, the synthesis of cis- as well as trans-2-aminocyclohexanols, dihydroconduramine E-1, and ent-conduramine F-1 has been described.
