IR@IIIM - Indian Institute of Integrative Medicine (CSIR)
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Chemoprevention with Aqueous Extract of Butea monosperma flowers results in normalization of nuclear morphometry and inhibition of a proliferation marker in liver tumors
No full textButea monosperma (Lam.) (family: Fabaceae) popularly known as 18Palas 19 or 18fire of forest 19 has been used traditionally as a hepatoprotective agent. This study evaluated the hepatoprotective and antitumorigenic properties of the aqueous extract and butanol fractions of B. monosperma flowers in animal models. Dried flowers of B. monosperma were extracted with water and fractionated further using n-butanol. The hepatoprotective activity of the aqueous extract was initially confirmed in a carbon tetrachloride-induced liver damage model of rats. Oral administration of the aqueous extract produced a strong hepatoprotective effect similar to silymarin and normalized the serum levels of ALT, AST, bilirubin and triglyceride in rats. However, it did not affect the levels of glutathione and malondialdehyde which are oxidative stress markers in liver. Intraperitoneal administration of the aqueous extract in the X15-myc oncomice not only maintained liver architecture and nuclear morphometry but also down-regulated the serum VEGF levels. Immunohistochemical staining of liver sections with anti-Ribosomal protein S27a antibody showed post-treatment abolition of this proliferation marker from the tumor tissue. The butanol fractions, however, did not show antitumorigenic activity. Thus, the aqueous extract of B. monosperma flowers is not only hepatoprotective but also antitumorigenic by preserving the nuclear morphometry of the liver. Copyrigh
In vitrocytotoxicityof extracts and fractions ofCalotropis procera(Ait.) roots against human cancer cell lines
No full textThis study was designed to determine the antiproliferative activity of three extracts (alcoholic, hydro-aqueous and aqueous) and their fractions from the root part of Calotropis procera using human oral (KB) and central nervous system (SNB-78) cancer cell lines as a model system. KB and SNB-78 cells were cultured in the presence of extracts and fractions at various concentrations (10, 30
and100 μg/ml) for 48 h, and the percentage of cell viability was evaluated by the sulforhodamine-B (SRB) assay. Our result indicates that out of the three extracts of C. procera (root), alcoholic extract had shown greater potential for growth inhibition followed by hydro-aqueous extract at three different concentration of 10 μg/ml, 30 μg/ml and 100 μg/ml in a dose-dependent manner, whereas
aqueous extract was found to be least active against both oral and CNS human cancer lines. On evaluation of the fractions prepared from alcoholic and hydro-aqueous extracts, it was observed that chloroform fraction from alcoholic extract was antiproliferative for oral (KB) cancer cell line and n-butanol fraction from alcoholic extract was antiproliferative for CNS cancer cell line than remaining fractions at three different concentration of 10 μg/ml, 30 μg/ml, 100 μg/ml in a dose-dependent manner. Thus, our result indicates that the root part of C. procera possess in vitro cytotoxicity against oral and CNS human cancer cell lines. Further investigations are required to obtain the clinically important lead molecules for the drug development
Natural antioxidants synergistically enhance the anticancer potential of AP9-cd, a novel lignan composition from Cedrus deodara in human leukemia HL-60 cells
No full textAntioxidants have been used as adjuvant with anticancer therapy to synergize the potential of the antineoplastic
therapeutics. Based on the fact, we have studied the effect of three natural antioxidants curcumin, silymarin and acteoside on AP9-cd (standardized lignan composition from Cedrus deodara) induced cytotoxicity in human leukemia HL-60 cells. The antioxidant potential of individual test compounds was first evaluated with ferric reducing antioxidant power (FRAP) test, which revealed that all
four molecules behave as antioxidants. The apoptotic potential of AP9-cd was significantly enhanced in
HL-60 cells in the presence of curcumin, silymarin and acteoside. It was confirmed by using various models
like MTT assay, DNA fragmentation, nuclei condensation, sub-Go DNA population, Annexin-V-FITC binding, ROS depletion and immunoblotting in HL-60 cells. AP9-cd and individual antioxidants alone at low doses (10�g and 10�M, respectively) have meager or no cytotoxicity in HL-60 cells, whereas in mutual combinations, there were 2–3 times enhancement in Annexin-V-FITC and sub-Go DNA population.
Moreover, prominent DNA ladders were observed at low doses of AP9-cd in combinations with various antioxidants. The Hoechst staining of the nucleus also revealed the same results for the HL-60 cells treated with AP9-cd and different antioxidants. The molecular diagnostics revealed that the combinations induced a strong antioxidant effect which was correlated with the downregulation of NF-�B
expression in the nucleus. Out of the three antioxidants, curcumin was found to be more potent than acteoside and silymarin in terms of enhancing the apoptotic potential of AP9-cd. These results propose an important role of natural antioxidant as adjuvant to enhance the anticancer potential of AP9-cd and more likely other anti-neoplastic therapeutics
Evaluation of cassia occidentalis for in vitro cytotoxicity against human cancer cell lines and antibacterial activity
No full textObjective : To evaluate the in vitro cytotoxicity and antibacterial properties of Cassia occidentalis (whole plant) via alcoholic, hydro-alcoholic, and aqueous extracts against eight human cancer cell lines from six different tissues and four bacterial strains.
Material and Methods : In vitro cytotoxicity against the human cancer cells, cultured for 48h in presence of different concentrations C. occidentalis extracts and percentage of cell viability, was evaluated using the sulforhodamine-B (SRB) assay. The antibacterial activity was performed using the standard protocol against bacterial strains.
Results : It was observed that aqueous extract of C. occidentalis (whole plant) had more potential than hydro-alcoholic and alcoholic extracts against HCT-15, SW-620, PC-3, MCF-7, SiHa, and OVCAR-5 human cancer cell lines at 100, 30, and 10 μg/ml in a dose-dependent manner. The hydro-alcoholic extract showed potential against Bacillus subtillis.
Conclusion : The plant can be explored for the possible development of lead molecules for drug discovery
Protective Effect ofLabisia pumilaon Stress-Induced Behavioral, Biochemical, and Immunological Alterations
No full textThe aim of the present study was to investigate the antistress potential of LABISIA PUMILA aqueous extract (LPPM/A003) using a battery of tests widely employed in different stressful situations. Pretreatment of experimental animals with LPPM/A003 caused an increase in the swimming endurance and hypoxia time and also showed the recovery of physical stress-induced depletion of neuromuscular coordination and scopolamine induced memory deficit. LPPM/A003 at graded doses reversed the chronic restraint stress (RST), induced depletion of CD4 and CD8 T lymphocytes, NK cell population, and corresponding cytokines expression besides downregulating the stress-induced increase in plasma corticosterone, a major stress hormone. In addition, LPPM/A003 reversed the chronic stress-induced increase in adrenal gland weight, serum alanine aminotransferase (ALT), alkaline phosphatase (ALP), and hepatic lipid peroxidation (LP) levels and augmented the RST induced decrease in hepatic glutathione (GSH), thymus and spleen weight. Thus, we conclude that LPPM/A003 has the ability to reverse the alterations produced by various stressful stimuli and therefore restores homeostasis
Solvent free synthesis, anti-inflammatory and anticancer activity evaluation of tricyclic and tetracyclic benzimidazole derivatives
No full textHeterocyclic benzimidazole derivatives 3a–h, 5a–c and 7a–d have been synthesized by condensation of succinic acid (1) homophthalic acid (4) and 2,3-pyrazinedicarboxlic acid (6) with various substituted diamines under microwave irradiation in good yields. Structures assigned to 3a–h, 5a–c and 7a–d are fully supported by spectral data. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg po compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory
activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg po and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines
In vivo genotoxicity evaluation of a plant based antiarthritic and anticancer therapeutic agent Boswelic acids in rodents
No full textThe genotoxic potential of anti-inflammatory/anti-arthritic and anticancer plant based drug molecule Boswelic acids (BA) was studied by in vivo system. Systematic literature survey revealed that studies on the genotoxicity of BA are not available. Although reports on genotoxicity of Boswellia serrata dry extract and modified 3-O-acetyl-11-keto-b-boswelic acid are available and these studies were conducted in vitro systems. The earlier general toxicity study of BA has been conducted by us, revealed it to be non toxic. The genotoxicity was carried out in Wistar rats using different cytogenetic assay systemabnormalities
viz. chromosomal aberrations; sperm morphology, micronuclei and comet assays. Six groups of animals, each comprised of five rats, were taken for each study. Group1-4 received BA at 125,250, 500 and 1000mg/kg p.o., respectively prepared as 2% gum acacia suspension, fifth group received a
positive control cyclophosphamide (CP) 40 mg/kg p.o. or metronedazole (MTZ) 130 mg/kg p.o. or mercuric chloride (HgCl2) 0.864 mg/kg p.o. (as per the experiment requirement) whereas the sixth group kept as vehicle control. The results on the bases of the data obtained revealed that BA is quite safe as it did not show any genotoxicity at any dose level up to 1000mg/kg. The positive controls used in different experiments showed highly significant abnormal cytogenetic changes in comparison to the control group
Production dynamics of Withaferin A inWithania somnifera(L.) Dunal complex
No full textWithaferin A (WA) is an important withanolide holding promise in cancer treatment and as a relatively safe radiosensitive/chemotherapeutic agent, which is
present in traces in all parts of Withania somnifera except the leaves, where as it is reported to be present in only two non-Indian chemotypes (South African chemotype/Israel chemotype 1). The present studies have marked its presence in all Indian populations (wild/cultivated), as well as two identified Indian chemotypes (AGB002 and AGB025). The quantitative dynamics of WA production in Indian populations and interchemotypic hybrids developed at
our institute have been studied, and the results were compared with five previously reported chemotypes from Israel, South Africa and India. An analysis on inheritance characteristics based on presence/absence of WA in hybrid plants and their respective parents is given for future studies on the chemogenetics of this complex species in greater detail. Further, the production potential of WA in vitro propagated plants of elite varieties developed at our institute is discussed, in view of maintaining chemotypic fidelity and stability from a production point of view.
Also, evidence-based clues suggesting the leaves as the site of the synthesis of WA is provided
Sub-acute toxicity evaluation of an aqueous extract of Labisia pumila, a Malaysian herb
No full textLabisia pumila (Myrsinaceae), is a popular herb among the women in Malaysia known locally as ‘‘Kacipn Fatimah”. Recently many nutraceutical products containing the powdered or extracted parts of the plant have become available for women’s health care. However no evaluation of the effect of the repeated dosing of any herbal product of this plant had been undertaken prior to a 28-day sub-acute study presented in this report. The results showed that a dose of 50 mg/kg of an aqueous extract of L. pumila corresponded to no-adverse-effect-level (NOAEL), whereas higher doses were associated with some toxicity concerns
Anticancer activity of an essential oil from Cymbopogon flexuosus
No full textThe essential oil froma lemon grass variety of Cymbopogon flexuosuswas studied for its in vitro cytotoxicity against twelve human cancer cell lines. The in vivo anticancer activity of the oil was also studied using both solid and ascitic Ehrlich and Sarcoma-180 tumor models in mice. In addition, the morphological changes in tumor cells were studied to ascertain the mechanism of cell death. The in vitro cytotoxicity studies showed dose-dependent effects against various human cancer cell lines. The IC50 values of oil ranged from 4.2 to 79�g/ml depending upon the cell line. In 502713 (colon) and IMR-32 (neuroblastoma)
cell lines, the oil showed highest cytotoxicity with IC50 value of 4.2 and 4.7�g/ml, respectively. Intraperitoneal
administration of the oil significantly inhibited both ascitic and solid forms of Ehrlich and Sarcoma-180 tumors in a dose-dependent manner. The tumor growth inhibition at 200 mg/kg (i.p.) of the oil observed with both ascitic and solid tumor forms of Ehrlich Ascites carcinoma was 97.34 and 57.83 respectively. In case of Sarcoma-180, the growth inhibition at similar dose of oil was 94.07 and 36.97%
in ascitic and solid forms respectively. Morphological studies of the oil treated HL-60 cells revealed loss
of surface projections, chromatin condensation and apoptosis. The mitochondria showed apparent loss
of cristae in the cells undergoing apoptosis. The morphological studies of Sarcoma-180 solid tumor cells
from animals treated with the oil revealed condensation and fragmentation of nuclei typical of apoptosis.
Morphological studies of ascites cells from animals treated with the oil too revealed the changes typical of apoptosis. Our results indicate that the oil has a promising anticancer activity and causes loss in tumor cell viability by activating the apoptotic process as identified by electron microscopy