Bio-guided Isolation of Natural Iron Chelators from Mangifera indica Leaves and their Comparative Study to Desferal®

Through bio-guided isolation, two natural iron chelators were isolated from Mangifera indica L. leaves, identified as mangiferin (1) and iriflophenone-3-C-β-D-glucoside (2). Their iron-chelating activity was compared to that of Desferal® using bipyridyl assay and EDTA as a standard. Mangiferin showed the highest activity with IC50 value of 0.385 mM (162.85 μg/mL). Furthermore, two combinations of mangiferin with Desferal® (M-D) and iriflophenone-3-C-β-D-glucoside (M-I) were evaluated. The results showed that mangiferin potentiated the iron chelation activity of Desferal® about 46%, also that M-I combination is a promising candidate formula for iron chelation therapy. In addition, mangiferin and Desferal-iron complexes were prepared and characterized by IR, UV, and Mass spectra to compare their mode of chelation to iron. Their structural stability was studied by DFT calculations. Furthermore, they displayed increased ABTS antioxidant activity when bound to iron as compared to their free form, which enhances their pharmacological importance.

Bio-guided Isolation of Natural Iron Chelators from Mangifera indica Leaves and their Comparative Study to Desferal®

Through bio-guided isolation, two natural iron chelators were isolated from Mangifera indica L. leaves, identified as mangiferin (1) and iriflophenone-3-C-β-D-glucoside (2). Their iron-chelating activity was compared to that of Desferal® using bipyridyl assay and EDTA as a standard. Mangiferin showed the highest activity with IC50 value of 0.385 mM (162.85 μg/mL). Furthermore, two combinations of mangiferin with Desferal® (M-D) and iriflophenone-3-C-β-D-glucoside (M-I) were evaluated. The results showed that mangiferin potentiated the iron chelation activity of Desferal® about 46%, also that M-I combination is a promising candidate formula for iron chelation therapy. In addition, mangiferin and Desferal-iron complexes were prepared and characterized by IR, UV, and Mass spectra to compare their mode of chelation to iron. Their structural stability was studied by DFT calculations. Furthermore, they displayed increased ABTS antioxidant activity when bound to iron as compared to their free form, which enhances their pharmacological importance.

Role of some mycotoxins in inducing kidney diseases in upper Egypt

Egypt has a climate that favors the growth of fungi specially those producing mycotoxins. Mycotoxins are found all over the world in human food and blood as well as in animal blood and tissues. The most threatening effects are their nephrotoxicity and carcinogenicity. The aim of this study was to identify the role of some mycotoxins namely; ochraloxin A [OTA] and fumonisin B[1] [FB1] in the occurrence of chronic renal disease of unknown aetiology in Upper Egypt. This study was carried out on 134 subjects who were classified as: 47 patients suffered from chronic renal failure of unknown aetiology before dialysis treatment [group A], 35 subjects who were relatives of patients in group A considering that they share them in the same environmental conditions [group B], 28 subjects working in the Middle Egypt Company [MEC] for grinding of cereals as an occupational risk group for exposure to inhalation of mycotoxins [group C] and 24 subjects with normal kidney functions as a control group. They exposed to a detailed history, their occupation, family history and kidney function tests. Indices of early kidney affection and levels of OTA and FB[1] in urine and serum for all subjects in all groups were also done. As regard group A, OTA was significantly increased while FBI was non-significantly increased in both serum and urine of patients compared to control group. There was positive correlation between the levels of OTA in both serum and urine versus the level of blood urea. It was found also that the patients with positive ochratoxicity had mild proteinuria. As regard group B, OTA and FB[1] were detected in urine and plasma, although with levels lower than that in group A but significantly higher than that of controls. As regard group C, OTA was found to be nearly equal to that in controls both in serum and urine which may indicate the low contamination levels of cereals in MEC due to good storage conditions. However, FB[1] was found in serum to be insignificantly higher than that in groups A and controls. Also FB[1] was detected in urine insignificantly lower than that in group A and insignificantly higher than that in controls. Although the results were statistically non significant but may indicate the increased risk of exposure to FB[1] in this group. We concluded that the presence of OTA and FB[1] in serum and urine of our control group may indicate the presence of these two mycotoxins as contaminants in the food in our locality. Also, these toxins may play a role in inducing chronic renal diseases in our locality. We advise a continuous follow up for all subjects exposed to these toxins, giving instructions about ways for protection and treatment as well as good storage for cereals and foods

Biological evaluation and study of polysaccharides of Dalbergia sissoo Roxb growing in Egypt

The extracts of Dalbergia sissoo Roxb growing in Egypt, the polysaccharides prepared from leaves, stem and bark and the major constituent in the plant [biochanin A] were subjected to screening of anti-inflammatory, anti-pyretic and analgesic activities adopting new methodology. The anti-tumor, anti-oxidant, and antimicrobial activities of these substances were also examined. Since the polysaccharides prepared from different organs [leaves 2.5%, stem 2.2%, bark 1.2%] possessed anti-inflammatory activities, they were subjected to further phytochemical studies, using paper chromato-graphy and GC/MS analysis. The polysaccharides were heterogeneous in nature and lacked uronic acids. The use of GC/MS to study the monomeric composition of polysaccharides in the acid hydrolysate indicated that the leaf polysaccharides consist mainly of rhamnose [77%] in addition to glucose [23%]. The stem polysaccharide consists of rhamnose [47%], glycerol [46%] and galactose [7%]. The bark polysaccharide consists of rhamnose [18%], fructose [2.5%], glucose [74.5%] and galactose [6%]

Effect of selected natural products, thioproline and pegasys on hepatic platelet activating factor [PAF] in CCl[4]-induced hepatic fibrosis in rats

This study aimed to estimate hepatic levels of platelet activating factor [PAF] in liver fibrosis induced by CC1[4] in rats. A group of selected natural products; boswellic acids, curcumin and glycyrrhizin [preparation named OMNI[R]; a drug under clinical trials for treatment of hepatitis C virus], Mirazid[R] [a commercially available schistomicidal drug], Thioproline [a commercially available hepatoprotective agent] and Pegasys[R] [peg interferon alpha-2a; a commercially available therapy for treatment of hepatitis C virus] were examined for their effect on hepatic PAF after CC1[4] intoxication. For this purpose, 54 rats were used in the study. Rats were divided into 6 groups each comprised 9 rats. Group 1 was treated only with CC1[4], groups 2 to 5 were treated with OMNI[R], Mirazid[R], Thioproline and Pegasys[R], respectively, whereas the sixth group was the normal control group [with no treatment, except an injection of the vehicle]. Liver damage was induced in all groups except normal control group [groups 1 to 5] by i.p. injection of 40% CC1[4] in corn oil [0.375 ml/kg] 3 times a week for 3 weeks. One week after CC1[4] intoxication, all tested drugs were injected i.p. daily for 3 weeks. Hepatic PAF concentration was estimated by HPTLC [high performance thin layer chromatography], while, levels of serum transaminases [ALT, AST], hepatic hydroxyproline [as markers of liver fibrosis], serum malondialdehyde and catalase [as markers of oxidative stress] were estimated spectrophotometrically. The hepatic PAF levels were significantly higher in CC1[4] group [24.24 +/- 2.01 pmol equiv./mg] as compared to normal control [8.81 +/- 1.09 pmol equiv./mg] [p<0.001]. Treatment with OMNI[R], Mirazid[R], Thioproline and Pegasys[R] reduced hepatic PAF significantly to be 11.84 +/- 0.22, 14.5 +/- 1.00, 13.17 +/- 0.54 and 14.26 +/- 1.09 pmol equiv./mg, respectively. This study may add further rational to the anti-fibrotic activity of the tested drugs via reduction of hepatic PAF

Synthesis and biological evaluation of certain new substituted pyrido [2,3-d] pyrimidin- 4[1H] -one and pyrido [2,3-d] Triazolo [3,4-b] pyrimidine analogs

The synthesis of a new series of Pyrido[2,3-d]-pyrimidine derivatives 8-13 and their corresponding S-methyl analogs 14

Phytochemical and biological investigation of leptadenia pyrotechnica dence growing in Egypt

The phytochemical investigation of Leptadenia pyrotechnica Dence [Family Asclepiadaceae] growing in Egypt was performed in this study. Sterols and triterpenes were isolated; namely, beta-amyrin, beta-sitosterol, lupeol and betulin. In addition, five flavonoid compounds, viz. quercetin, kaempferol-3-O-beta-D-glucoside, isorhamnetin-3-O-rutinoside, quercetin-3'- O-beta-D-glucoside and rutin. The isolation and identification of these compounds were achieved through different chromatographic and spectroscopic methods. The isolated pure compounds were subjected to a DNA-binding assay to reveal any antitumor activity of these compounds. Only betulin showed a moderate DNA-binding activity at IC50, 42 mug/ml