Pectic polysaccharides from dietary sources such as Decalepis hamiltonii--swallow root (SRPP), Hemidesmus indicus (HPP), Nigella sativa--black cumin (BCPP), Andrographis serpyllifolia-(APP), Zingiber officinale--ginger (GRPP) and, citrus pectin (CPP) were examined for galectin inhibitory activity. Inhibition of (a) galectin-3 of MDA-MB-231 cells induced hemagglutination of red blood cells; (b) galectin-3 mediated interaction between normal/metastatic human buccal cells (NBC)/(MBC) and; (c) invasion of MDA-MB-231 and MBC in the invasive chamber was assessed. Results indicated that SRPP inhibited hemagglutination at Minimum Inhibitory Concentration (MIC) of 1.86 microg ml(-1) equivalent of carbohydrate as apposed to those of BCPP (130 microg ml(-1)), APP (40 microg ml(-1)), HPP (40 microg ml(-1)) and CPP (25 microg ml(-1)). GRPP even at concentration >1-6 mg ml(-1) did not inhibit agglutination. Also SRPP showed approximately 15 and 2 fold potent anti hemagglutination activity relative to that of galectin-3 specific sugars-galactose (MIC-27.1 microg ml(-1)) and lactose (MIC-4.16 microg ml(-1)) respectively. Further, SRPP at 10 microg ml(-1) inhibited agglutination of NBC by galectin-3 of MDA-MB-231 cells. Modified swallow root pectic polysaccharide (MSRPP) of 50 kDa retained anti hemagglutination activity (MIC of 1.03 microg ml(-1)) and inhibited MDA-MB-231 and MBC invasion by 73 and 50% with an IC(50) of 136 and 200 microg ml(-1) respectively. Both SRPP and MSRPP induced apoptosis up to 80% at 100 microg ml(-1) concentration by activating approximately 2 and 8 folds of Caspase-3 activity. Sugar composition analysis and its correlation with the galectin inhibitory property indicated that pectic polysaccharides with higher arabinose and galactose content-arabinogalactan inhibited hemagglutination significantly.
Background:Hemidesmus indicus R.Br. is a twining shrub commonly found in India, which was known to have wide pharmacological actions. 2-hydroxy-4-methoxy-benzoic acid (HMBA) and a number of pregnane glycosides were believed to be responsible for its various bioactivities. Until now, there are no reports regarding the antioxidant properties of phenolics from H. indicusObjective:To establish the role of phenolics in the properties of H.indicus.Materials and Methods:Hemidesmus free phenolic fraction (HDFP) and Hemidesmus bound phenolic fraction (HDBP) have been isolated from H. indicus, and the antioxidant activity was evaluated for inhibition of lipid peroxidation, DNA protection, free radical scavenging (FRS), reducing power and cytoprotective activities.Results:HDFP and HDBP exhibited potent inhibition of lipid peroxidation (IC50 - 19.5 ±0.5 and 21.7 ±0.5 μg gallic acid equivalent - GAE/mL), FRS (IC50 - 7 ± 0.2 and 8.6 ± 0.2 μgGAE/mL), reducing power (110.3 ± 2 and 33.5 ± 1 U/g) and red blood cell protection (14.8 ± 0.4 and 14.5 ± 0.5 mg GAE/mL). HDFP is constituted by gallic (18%), caffeic (17%), ferulic acids (16%) and HDBP by syringic acid (35%) as major phenolic acids. Besides, both HDFP and HDBP contained significant levels of HMBA; in HDFP (10%) and HDBP (57%), respectively. Results indicated a 34-and 27-folds better contribution to the antioxidant activity by HDFP and HDBP, respectively, than that of HMBA.Conclusion:Potent antioxidant activities of phenolics may be one of the mechanisms by which H.indicus is effective against several health disorders as encountered in traditional medicines.
Oxidative stress and upregulation of gastric H + , K + -ATPase enzyme activity have been known to cause ulcer pathogenicity for which safer drugs are yet to be identified. Aqueous extracts of seven commonly consumed vegetable sources were screened for inhibition of H + , K + -ATPase and antioxidant activities. Results indicated that Z. officinale (Ginger) followed by M. arvensis (Pudina) are potent gastroprotective sources with inhibition of H + , K + -ATPase of IC 50 of 18.3 ± 0.7 and 25.2 ± 0.9 µg gallic acid equivalents/ml respectively, which is almost equivalent or better than the known inhibition of H + , K + -ATPase-Omeprazole (IC 50 ∼27 µg/ml). Further, all these vegetable extracts showed multi-potent antioxidant activity, such as free radical scavenging, reducing power ability, and inhibition of lipid peroxidation, which are required to inhibit complex steps of ulcerations. On the basis of the absolute amounts and potency of inhibition of H + , K + -ATPase as well as antioxidant activity of individual phenolic acids, the relative percentage contribution of phenolic acids from different vegetable extracts to both inhibition of H + , K + -ATPase and antioxidant activity was calculated and data revealed that gentisic and protocatechuic acid contributes significantly to both inhibition of H + , K + -ATPase and antioxidant activity.
Among several Andrographis species, only A. panniculata had been extensively studied and the bioactivity was attributed to the active component Andrographolide (AG). In the current investigation, we report that aqueous (ASAE) and methanol (ASME) extracts of Andrographis serpyllifolia contained phenolic acids up to 3-5%, in addition to AG which is present at ~2% level. Aqueous extract exhibited ~2 and 10 fold better free radical scavenging and reducing power activities than those of methanol extract and the isolated andrographolide, suggesting that Andrographis species may contain antioxidant components other than Andrographolide as well. Further, about 70-80% of DNA and red blood cells were protected against oxidant-induced damages at 4 ?g/mL, and there was about 80% inhibition of proliferation of highly metastatic MDA-MB-231 cells at 10 ?g/mL, which suggests the anticancer potential of A. Serpyllifolia. Identification of phenolic acids contributing to antioxidant potency revealed that gentisic (48%) followed by gallic (25%), protocatechuic (14%) & cinnamic (11%) acids in ASAE, while protocatechuic (59%), followed by ferulic (30%) and p-coumaric (8%) acids in ASME contributed to the activity. Thus, phenolics and andrographolide in A. Serpyllifolia may be implicated in anticancer properties as observed in traditional therapies.
Background: Andrographis serpyllifolia, used as a medicinal plant in traditional practices in India, where in cancer patients are treated using the leaves of A. serpyllifolia. The crude extracts of A. serpyllifolia not only contain a wide variety of phenolic compounds but also show an excellent antioxidant activity. Therefore, this plant might be a good candidate for further development for its antioxidant remedies. However, the biological activities of the phenolic extracts of A. serpyllifolia on cancer have not been studied to date. Objective: To investigate the antioxidant and antiproliferative properties of the phenolics of A. serpyllifolia. Materials and methods: Free and (ASFP) and bound (ASBP) phenolics of A. serpyllifolia were isolated and determined antioxidant and antiproliferative abilities that are required for anticancer properties. Results: Individual phenolic constituents present in each of these fractions and their precise contribution to both antioxidant and antiproliferative activities were determined to justify the traditionally observed result of anticancer properties. Treatment of HeLa cells with ASFP and ASBP showed antiproliferative activity with increased malondialdehyde (MDA) as well as decreased levels of reduced glutathione (GSH). The present experimental data suggest that components within the ASFP may have inherent properties that suppress cancer cell proliferation. The phenolic fractions were also screened for their potential antioxidant activities using DPPH, reducing power, DNA protection, inhibition of lipid peroxidation and protein carbonyls model systems. ASFP exhibited highest antioxidant activity in all the model systems employed to study antioxidant activity. The positive correlation between polyphenolic content of A. serpyllifolia to its antioxidant activity was seen. Conclusion: Potent antiproliferative and DNA protective activity of ASFP and ASBP may contribute significantly against cancer pathogenesis. INTRODUCTIONAndrographis serpyllifolia, an edible, railing and rooting herb known for its traditional medicinal properties. The herb belongs to the family Acanthaceae is widely distributed throughout Deccan and carnatic region of south India [1] and China. Although the related species A. paniculata is well characterized, only a very few studies report the presence of serpyllin, apigen, 7,4'-dimethyl ether and tectochrysin compounds [2,3] and, their implications on bioactivity is not clearly understood. Andrographolide (AG) has been reported as one of the potential active component and believed to be responsible for various bioactivities. [4][5][6] We reported for the first time, the antimetastatic property of pectic polysaccharide [7] and antioxidant activities of crude extracts of A. serpyllifolia. Excessive generation of free radicals is implicated in an ever growing number of disease conditions, including cancer, atherosclerosis, and neurodegenerative diseases. [9,10]
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