Scavestrogen sulfamates: correlation between estrone sulfatase inhibiting and antioxidant effects

1998 ◽  
Vol 76 (2) ◽  
pp. 99-109 ◽  
Author(s):  
Wolfgang Römer ◽  
Michael Oettel ◽  
Sigfrid Schwarz

In the present study estrone sulfatase (steryl-sulfatase; EC 3.1.6.2) and phenylsulfatase (arylsulfatase B; EC 3.1.6.1) inhibiting as well as antioxidant effects exerted by ring B,C unsaturated sulfamates of estrone (J 1025), 17 beta -estradiol (J 1054, J 1059, J 1067), and 17 alpha -estradiol (J 1051, J 1064, J 1065) were examined as compared with their parent compounds, J 994, J 995, and J 1050, using six different in vitro models: (i) estrone sulfatase activity in human placental microsomes, (ii) phenylsulfatase activity isolated from Helix pomatia, (iii) Fenton reaction driven lipid peroxidation in rat synaptosomes, (iv) Fe(II)-chelating activities, (v) formation of superoxide anion radicals, and (vi) total antioxidative activities. Ring B,C unsaturated estrogen (so-called scavestrogen) sulfamates were found to act as potent inhibitors of the following enzyme activities and generated radicals: estrone sulfatase, phenylsulfatase, lipid peroxyl, and superoxide anion. In addition, scavestrogen sulfamates were able to influence the iron redox chemistry and total antioxidative activities. These findings indicate that relatively minor modifications in the chemical structure of classical steroid sulfamates can preserve or enhance their estrone sulfatase inhibiting properties and, simultaneously, amplify their antioxidant capacity to a great extent. Taken together, our data suggest that scavestrogen sulfamates such as J 1025, J 1051, or J 1054 (17 beta -dihydroequilenin sulfamate) may serve as a very promising basis for the development of steroid-derived estrone sulfate - sulfatase inhibitors characterized by promising estrone sulfatase inhibiting activities in combination with a "good" antioxidant potency.Key words: estrogen 3-O-sulfamates, estrone sulfatase, phenylsulfatase, lipid peroxidation, iron redox chemistry, human placental microsomes, radical scavenging effects.

Author(s):  
Abhishek Chatterjee ◽  
Dileep Singh Baghel ◽  
Bimlesh Kumar ◽  
Saurabh Singh ◽  
Narendra Kumar Pandey ◽  
...  

Objective: The aims of the present investigation were to develop the herbal and/or herbomineral formulations of Hinguleswara rasa and to compare their anti-inflammatory and antioxidant activities, in vitro, with that of standard drug samples.Methods: This study was an interventional investigation in three samples: In the first sample, Hinguleswara rasa (HR1) was prepared as per methodology described in Rasatarangini using Shuddha Hingula (10 g), Shuddha Vatsanabha (10 g), and Pippali (10 g). In the second and third sample, respectively, Hinguleswara rasa was prepared by replacing Shuddha Hingula with Kajjali where Kajjali made from Hingulotha parada and Sodhita parada constitutes two varieties of Hinguleswara rasa, i.e. HR2 and HR3. In vitro antioxidant activity was studied using 2,2-diphenyl-1-picrylhydrazyl, and the absorbance was recorded at 517 nm. For evaluating the in vitro anti-inflammatory studies, the inhibition of albumin denaturation technique was performed.Results: The results showed that the formulation of Hinguleswara rasa has shown dose-dependent activity which was observed in 100 μg concentration. HR1, HR2, and HR3 showed 36.11, 17.22, and 16.11% radical scavenging activity.Conclusion: It could be concluded that the changes made in the formulations did not affect the in vitro anti-inflammatory and antioxidant effects of the herbomineral formulations.


Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4055 ◽  
Author(s):  
Mariusz Banach ◽  
Magdalena Wiloch ◽  
Katarzyna Zawada ◽  
Wojciech Cyplik ◽  
Wojciech Kujawski

Aronia fruits contain many valuable components that are beneficial to human health. However, fruits are characterized by significant variations in chemical composition dependent on the growing conditions and harvesting period. Therefore, there is a need to formulate the extracts with a precisely defined content of health-promoting substances. Aronia dry extracts (ADE) were prepared from frozen pomace applying water extraction, followed by purification and spray-drying. Subsequently, the content of anthocyanins, phenolic acids, and polyphenols was determined. The high-quality chokeberry pomace enabled obtaining extracts with anthocyanin content much higher than the typical market standards. Moreover, it was found that the antioxidant capacity of aronia extracts exceeded those found in other fruit preparations. Antioxidant and free-radical scavenging properties were evaluated using a 2,2′-diphenyl-1-picrylhydrazyl using Electron Paramagnetic Resonance (EPR) spectroscopy (DPPH-EPR) test and Oxygen Radical Absorbance Capacity (ORAC) assay. The inhibition of lipid peroxidation and the level of inflammatory markers have been also investigated using lipopolysaccharide (LPS)-stimulated RAW 264 cells. It was revealed that ADE standardized to 25% of anthocyanins depresses the level of markers of inflammation and lipid peroxidation (Interleukin 1 beta (IL-1β), tumor necrosis factor alpha (TNF-α), and malondialdehyde (MDA)) in in vitro conditions. Additionally, it was confirmed that ADE at all analyzed concentrations did not show any cytotoxic effect as demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.


2010 ◽  
Vol 5 (2) ◽  
pp. 224-230 ◽  
Author(s):  
Boobalan Raja ◽  
Kodukkur Pugalendi

AbstractIn this study, an aqueous extract of leaves from Melothria maderaspatana was tested for in vitro antioxidant activity. Free radical scavenging assays, such as hydroxyl radical, hydrogen peroxide, superoxide anion radical and 2,2-diphenyl-1-picryl hydrazyl (DPPH), 2,2’-azinobis-(3-ethyl-enzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, and reducing power assay, were studied. The extract effectively scavenged hydroxyl radical, hydrogen peroxide and superoxide anion radicals. It also scavenged DPPH and ABTS radicals. Furthermore, it was found to have reducing power. All concentrations of leaf extract exhibited free radical scavenging and antioxidant power, and the preventive effects were in a dose-dependent manner. The antioxidant activities of the above were compared to standard antioxidants such as butylated hydroxytoluene (BHT), ascorbic acid, and α-tocopherol. The results obtained in the present study indicate that the M. maderaspatana extract could be considered a potential source of natural antioxidant.


1979 ◽  
Vol 105 (4) ◽  
pp. 527-529 ◽  
Author(s):  
DAVID S. SMITH ◽  
STIG REHNCRONA ◽  
EVA WESTERBERG ◽  
BJORN AKESSON ◽  
BO K. SIESJÖ

2020 ◽  
Vol 21 (47) ◽  
pp. 12-18
Author(s):  
Wu Lan Gerile ◽  
Naranchimeg Dorjpalam ◽  
Wanyuan Gui ◽  
Liang Xu ◽  
Jinglin Liu

The polysaccharides isolated from Polygonatum odoratum (Mill.) Druce (POPs) by water extraction, after precipitation with ethanol were purified through deproteinization, decolorization, dialysis, and column chromatography leading to a purified polysaccharide (POPs-I) content of 90.7 %. The scavenging of oxygen free radicals and inhibition of lipid peroxidation (LPO) by POPs-I were analyzed using a colorimetric method. The results showed that the hydroxyl radical scavenging ability of the polysaccharides was weaker than that of benzoic acid, but stronger than those of ascorbic acid and mannitol, and that the superoxide anion radical scavenging ability was inferior to those of all three. When the concentration was higher than 1.0 mg/mL, the POPs-I could inhibit LPO by superoxide anion radicals to a certain degree. Therefore, this work suggests that POPs-I are potential antioxidant agents in medicine and functional food.


2020 ◽  
Vol 10 (4) ◽  
pp. 70-78
Author(s):  
Abir Rezzagui ◽  
Abderrahmane Senator ◽  
Soumia Benbrinis ◽  
Hamama Bouriche

This study was undertaken to evaluate the antioxidant and anti-hemolytic properties of Algerian Drimia maritima Baker flower extracts. Determination of phenolic content was carried out to estimate the chemical composition of D. maritima extracts. Antioxidant properties were investigated in all extracts using free radical scavenging activity (against DPPH, ABTS, hydroxyl radical, and superoxide anion), reducing power, inhibition of lipid peroxidation, and anti-hemolytic capacity. Phenolic determination revealed that D. maritima flowers contain phenolic compounds, flavonoids, and tannins. Ethyl acetate extract showed the highest reducing power and scavenging activity using DPPH and ABTS assays. However, aqueous extract was the most effective against hydroxyl radical, superoxide anion, and lipid peroxidation. The half-time of hemolysis indicates that chloroform extract exhibited the best anti-hemolytic capacity in the AAPH induced hemolysis model. The results of this study suggest that D. maritima could be used as a possible source of antioxidant phenolic compounds and that further determination of these compounds may provide more information on their medicinal value.  Keywords: Drimia maritima, phenolic compounds, scavenging activity, reducing power, anti-hemolytic.


2011 ◽  
Vol 1 (7) ◽  
pp. 232 ◽  
Author(s):  
Xican Li ◽  
Xiaozhen Wang ◽  
Dongfeng Chen ◽  
Shuzhi Chen

Background: Protocatechuic acid (PCA) is a natural phenolic acid widely distributed in plants and is considered as an active component of some traditional Chinese herbal medicines such as Cibotium barometz (L.) J.Sm, Stenoloma chusanum (L.) Ching, Ilex chinensis Sims. PCA was reported to possess various pharmacological effects which may be closely correlated with its antioxidant activities. However, the antioxidant of PCA has not been investigated systematically yet. Methods: In the study, the antioxidant activities of protocatechuic acid were measured in vitro using various antioxidant assays including 1,1-diphenyl-2-picryl-hydrazyl (DPPH•), 2,2’-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS+•), superoxide anion radicals (•O2-) and hydroxyl radical (•OH) scavenging activity, ferric ions (Fe3+) and cupric ions (Cu2+) reducing power, ferrous ions (Fe2+) and cupric ions (Cu2+) chelating activity, compared with the positive controls Trolox or BHT.Results: In all assays, PCA along with positive controls exhibited dose-dependently antioxidant ability. Comparing to a standard antioxidant Trolox, the relative antioxidant activity of PCA (i.e. the ratio of IC50(Trolox)/IC50(PCA) ) was calculated as 2.8, 2.3, 3.7, 6.1, 4.2, 1.0, 2.7, 1.5, respectively, for DPPH, ABTS, reducing power (Fe3+), reducing power (Cu2+), superoxide anion radical-scavenging, hydroxyl radical-scavenging, chelating ability (Fe2+) and chelating ability (Cu2+). Conclusion: Comparing to Trolox, PCA shows much more effective antioxidant activity in vitro in both lipid and aqueous media. Hence, it could therefore be used in pharmacological or food industry as a natural antioxidant. It may exhibit antioxidant activity by both chelating metal transition ions as well as by scavenging free radicals via donating hydrogen atom (H•) or electron (e).Keywords: Protocatechuic acid, antioxidant, reducing power, free radical-scavenging, chelating ability.


2006 ◽  
Vol 1 (7) ◽  
pp. 1934578X0600100
Author(s):  
Shizuo Toda ◽  
Yoshiaki Shirataki

The possible antioxidant effect of two isoflavanones, echinoisoflavanone and sophoraisoflavanone D from Sophora chrysophylla Seem. was investigated. Both these compounds inhibited the superoxide anion-mediated lipid peroxidation of lecithin and scavenged superoxide anion generated by the xanthine-xanthine oxidase system. These results indicated the impressive antioxidant property of these two compounds.


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