Flavonoids are polyphenols that are found in numerous edible plant species. Data obtained from preclinical and clinical studies suggest that specific flavonoids are chemo-preventive and cytotoxic against various cance...Flavonoids are polyphenols that are found in numerous edible plant species. Data obtained from preclinical and clinical studies suggest that specific flavonoids are chemo-preventive and cytotoxic against various cancers via a multitude of mechanisms. However, the clinical use of flavonoids is limited due to challenges associated with their e ective use, including(1) the isolation and purification of flavonoids from their natural resources;(2) demonstration of the e ects of flavonoids in reducing the risk of certain cancer, in tandem with the cost and time needed for epidemiological studies, and(3) numerous pharmacokinetic challenges(e.g., bioavailability, drug–drug interactions, and metabolic instability). Currently, numerous approaches are being used to surmount some of these challenges, thereby increasing the likelihood of flavonoids being used as chemo-preventive drugs in the clinic. In this review, we summarize the most important challenges and e orts that are being made to surmount these challenges.展开更多
In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-...In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives retrieved from our in-house database were evaluated for their cytotoxic activity against nine cancer cell lines. The results indicated that the compounds showed moderate cytotoxic activity against MCF-7, MDA-MB-468, K562 and SaOS2 cells, with K562 being the most sensitive among the four cancer cell lines. The eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives were also evaluated for their COX-1 and COX-2 inhibitory activity in vitro. The results showed that compound 3f exhibited 2-fold selectivity with IC_(50) values of 9.2 and 21.8 mmol/L against COX-2 and COX-1, respectively. Molecular docking studies on the most active compound 3f revealed a binding mode similar to that of celecoxib in the active site of the COX-2 enzyme.展开更多
Background: Iron deficiency anemia (IDA) in children and infants is a common nutritional problem all over the world. Infants and young children have a high risk for developing iron deficiency (ID) because they have hi...Background: Iron deficiency anemia (IDA) in children and infants is a common nutritional problem all over the world. Infants and young children have a high risk for developing iron deficiency (ID) because they have high demand for iron during the period of rapid growth. This is aggravated by the insufficiency of iron in their diet. Iron supplementation programs using pediatric tablets or drops have not been successful in the control of anemia amongst infants and children in some countries. “Sprinkles” is an innovative multi-micronutrient home fortification strategy to control iron deficiency and anemia to be more useful. Objective: The objective was to estimate the prevalence ID and IDA in infants and children in Ibb City, Yemen Republic;evaluate the use of a new form of iron and determine the hematologic response to different doses and forms of iron in Sprinkles and iron drops. Design: Using a prospective, randomized, controlled design, we studied 337 randomly children aged 24 - 48 months and infants aged 6 - 24 months in Ibb City (hemoglobin: 70 - 99 g/L). One group received a daily sachet of microencapsulated ferrous fumarate (80 mg elemental Fe) in powder form plus ascorbic acid to be sprinkled onto any complementary food eaten (sprinkles group);a control group received ferrous sulfate drops 3 times/d for 2 months (total dose: 40 mg elemental Fe). Hemoglobin and serum ferritin concentrations were measured at baseline and at the end of treatment. Results: Successful treatment of anemia (hemoglobin > 100 g/L) occurred in 58% of the sprinkles group and in 56% of the drops group, with minimal side effects in both groups. Geometric mean ferritin concentrations increased significantly in each group from baseline to the end of treatment (P Conclusion: Use of ferrous sulfate drops or a single daily dose of microencapsulated ferrous fumarate sprinkles plus ascorbicacid resulted in a similar rate of successful treatment of anemia without side effects. To our knowledge, this is the first demonstration of the use of 展开更多
基金supported by seed-fund to AKT from Department of Pharmacology and Experimental Therapeutics at UT
文摘Flavonoids are polyphenols that are found in numerous edible plant species. Data obtained from preclinical and clinical studies suggest that specific flavonoids are chemo-preventive and cytotoxic against various cancers via a multitude of mechanisms. However, the clinical use of flavonoids is limited due to challenges associated with their e ective use, including(1) the isolation and purification of flavonoids from their natural resources;(2) demonstration of the e ects of flavonoids in reducing the risk of certain cancer, in tandem with the cost and time needed for epidemiological studies, and(3) numerous pharmacokinetic challenges(e.g., bioavailability, drug–drug interactions, and metabolic instability). Currently, numerous approaches are being used to surmount some of these challenges, thereby increasing the likelihood of flavonoids being used as chemo-preventive drugs in the clinic. In this review, we summarize the most important challenges and e orts that are being made to surmount these challenges.
文摘In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives retrieved from our in-house database were evaluated for their cytotoxic activity against nine cancer cell lines. The results indicated that the compounds showed moderate cytotoxic activity against MCF-7, MDA-MB-468, K562 and SaOS2 cells, with K562 being the most sensitive among the four cancer cell lines. The eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives were also evaluated for their COX-1 and COX-2 inhibitory activity in vitro. The results showed that compound 3f exhibited 2-fold selectivity with IC_(50) values of 9.2 and 21.8 mmol/L against COX-2 and COX-1, respectively. Molecular docking studies on the most active compound 3f revealed a binding mode similar to that of celecoxib in the active site of the COX-2 enzyme.
文摘Background: Iron deficiency anemia (IDA) in children and infants is a common nutritional problem all over the world. Infants and young children have a high risk for developing iron deficiency (ID) because they have high demand for iron during the period of rapid growth. This is aggravated by the insufficiency of iron in their diet. Iron supplementation programs using pediatric tablets or drops have not been successful in the control of anemia amongst infants and children in some countries. “Sprinkles” is an innovative multi-micronutrient home fortification strategy to control iron deficiency and anemia to be more useful. Objective: The objective was to estimate the prevalence ID and IDA in infants and children in Ibb City, Yemen Republic;evaluate the use of a new form of iron and determine the hematologic response to different doses and forms of iron in Sprinkles and iron drops. Design: Using a prospective, randomized, controlled design, we studied 337 randomly children aged 24 - 48 months and infants aged 6 - 24 months in Ibb City (hemoglobin: 70 - 99 g/L). One group received a daily sachet of microencapsulated ferrous fumarate (80 mg elemental Fe) in powder form plus ascorbic acid to be sprinkled onto any complementary food eaten (sprinkles group);a control group received ferrous sulfate drops 3 times/d for 2 months (total dose: 40 mg elemental Fe). Hemoglobin and serum ferritin concentrations were measured at baseline and at the end of treatment. Results: Successful treatment of anemia (hemoglobin > 100 g/L) occurred in 58% of the sprinkles group and in 56% of the drops group, with minimal side effects in both groups. Geometric mean ferritin concentrations increased significantly in each group from baseline to the end of treatment (P Conclusion: Use of ferrous sulfate drops or a single daily dose of microencapsulated ferrous fumarate sprinkles plus ascorbicacid resulted in a similar rate of successful treatment of anemia without side effects. To our knowledge, this is the first demonstration of the use of
