Health beneficial and pharmacological properties of p-cymene
Food Chem Toxicol. 2021 May 10:112259. doi: 10.1016/j.fct.2021.112259. Online ahead of print.ABSTRACTp-cymene also known as p-cymol or p-isopropyltoluene is an alkyl-substituted aromatic compound naturally occurring in essential oils (EOs) of various aromatic plants, including the genus of Artemisia, Protium, Origanum, and Thymus. It is related to the family of terpenes, especially monocyclic monoterpenes. p-cymene is also present in several food-based plants such as carrots, orange juice, grapefruit, tangerine, raspberries and several spices. Numerous studies have demonstrated the pharmacological properties of the monoter...
Source: Food and Chemical Toxicology - May 13, 2021 Category: Food Science Authors: Abdelaali Balahbib Nasreddine El Omari Naoufal El Hachlafi Fatima Lakhdar Naoual El Menyiy Najoua Salhi Hanae Naceiri Mrabti Saad Bakrim Gokhan Zengin Abdelhakim Bouyahya Source Type: research
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Biol Pharm Bull. 2021;44(5):653-658. doi: 10.1248/bpb.b20-00947.ABSTRACTAlogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4'-di...
Source: Biological and Pharmaceutical Bulletin - May 6, 2021 Category: Drugs & Pharmacology Authors: Kaori Morimoto Momona Sasaki Erika Oikawa Maho Abe Tatsuro Kikuchi Makoto Ishii Takuo Ogihara Mikio Tomita Source Type: research
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents
ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized and these new compounds were tested against several strains of bacteria. Some of these compounds (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds ar...
Source: ChemMedChem - May 6, 2021 Category: Chemistry Authors: Ibrahim Alkhaibari Hansa Raj Kc Rawan Alnufaie David F Gilmore Mohammad Abrar Alam Source Type: research
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Biol Pharm Bull. 2021;44(5):653-658. doi: 10.1248/bpb.b20-00947.ABSTRACTAlogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4'-di...
Source: Biological and Pharmaceutical Bulletin - May 6, 2021 Category: Drugs & Pharmacology Authors: Kaori Morimoto Momona Sasaki Erika Oikawa Maho Abe Tatsuro Kikuchi Makoto Ishii Takuo Ogihara Mikio Tomita Source Type: research
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents
ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized and these new compounds were tested against several strains of bacteria. Some of these compounds (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds ar...
Source: ChemMedChem - May 6, 2021 Category: Chemistry Authors: Ibrahim Alkhaibari Hansa Raj Kc Rawan Alnufaie David F Gilmore Mohammad Abrar Alam Source Type: research
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Biol Pharm Bull. 2021;44(5):653-658. doi: 10.1248/bpb.b20-00947.ABSTRACTAlogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4'-di...
Source: Biological and Pharmaceutical Bulletin - May 6, 2021 Category: Drugs & Pharmacology Authors: Kaori Morimoto Momona Sasaki Erika Oikawa Maho Abe Tatsuro Kikuchi Makoto Ishii Takuo Ogihara Mikio Tomita Source Type: research
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents
ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized and these new compounds were tested against several strains of bacteria. Some of these compounds (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds ar...
Source: ChemMedChem - May 6, 2021 Category: Chemistry Authors: Ibrahim Alkhaibari Hansa Raj Kc Rawan Alnufaie David F Gilmore Mohammad Abrar Alam Source Type: research
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Biol Pharm Bull. 2021;44(5):653-658. doi: 10.1248/bpb.b20-00947.ABSTRACTAlogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4'-di...
Source: Biological and Pharmaceutical Bulletin - May 6, 2021 Category: Drugs & Pharmacology Authors: Kaori Morimoto Momona Sasaki Erika Oikawa Maho Abe Tatsuro Kikuchi Makoto Ishii Takuo Ogihara Mikio Tomita Source Type: research
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Biol Pharm Bull. 2021;44(5):653-658. doi: 10.1248/bpb.b20-00947.ABSTRACTAlogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4'-di...
Source: Biological and Pharmaceutical Bulletin - May 6, 2021 Category: Drugs & Pharmacology Authors: Kaori Morimoto Momona Sasaki Erika Oikawa Maho Abe Tatsuro Kikuchi Makoto Ishii Takuo Ogihara Mikio Tomita Source Type: research
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents
ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized and these new compounds were tested against several strains of bacteria. Some of these compounds (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds ar...
Source: ChemMedChem - May 6, 2021 Category: Chemistry Authors: Ibrahim Alkhaibari Hansa Raj Kc Rawan Alnufaie David F Gilmore Mohammad Abrar Alam Source Type: research
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents
ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized and these new compounds were tested against several strains of bacteria. Some of these compounds (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds ar...
Source: ChemMedChem - May 6, 2021 Category: Chemistry Authors: Ibrahim Alkhaibari Hansa Raj Kc Rawan Alnufaie David F Gilmore Mohammad Abrar Alam Source Type: research
Fertility and early embryonic development toxicity assessment of naringin in Sprague-Dawley rats
Regul Toxicol Pharmacol. 2021 Apr 29:104938. doi: 10.1016/j.yrtph.2021.104938. Online ahead of print.ABSTRACTNaringin is a dihydroflavonoid abundantly existed in grapefruit and related citrus species. The double directional adjusting function of estrogenic and anti-estrogenic activities of naringin and its aglycone naringenin has raised concern about possible risks of unwanted interference with endocrine regulation. Herein we assessed the safety of naringin on fertility and early embryonic development toxicity in Sprague-Dawley rats. Twenty-two male and 22 female rats per group were orally given naringin at 0, 50, 250, and...
Source: Regulatory Toxicology and Pharmacology : RTP - May 2, 2021 Category: Toxicology Authors: Yonggang Wang Hao Wu Pan Chen Weiwei Su Wei Peng Peibo Li Source Type: research
Fertility and early embryonic development toxicity assessment of naringin in Sprague-Dawley rats
Regul Toxicol Pharmacol. 2021 Apr 29:104938. doi: 10.1016/j.yrtph.2021.104938. Online ahead of print.ABSTRACTNaringin is a dihydroflavonoid abundantly existed in grapefruit and related citrus species. The double directional adjusting function of estrogenic and anti-estrogenic activities of naringin and its aglycone naringenin has raised concern about possible risks of unwanted interference with endocrine regulation. Herein we assessed the safety of naringin on fertility and early embryonic development toxicity in Sprague-Dawley rats. Twenty-two male and 22 female rats per group were orally given naringin at 0, 50, 250, and...
Source: Regulatory Toxicology and Pharmacology : RTP - May 2, 2021 Category: Toxicology Authors: Yonggang Wang Hao Wu Pan Chen Weiwei Su Wei Peng Peibo Li Source Type: research
Association of single nucleotide polymorphisms with taste and food preferences of the Hungarian general and Roma populations
Appetite. 2021 Apr 27:105270. doi: 10.1016/j.appet.2021.105270. Online ahead of print.ABSTRACTIt is reasonable to suppose that poor diet underlies the unfavorable health status of the Roma population of Europe. Previously in the framework of a complex health survey, fruit and vegetable consumption, quantity of sugar added, salting frequency; bitter, salty, sweet and fat taste preferences were evaluated of Hungarian (HG, n=410) and Roma (HR, n=387) populations. In the present study the associations of taste and food preferences with TAS1R3, CD36, SCNN1B, TRPV1, TAS2R38, TAS2R19 and CA6 polymorphisms were tested in the same ...
Source: Appetite - April 30, 2021 Category: Nutrition Authors: Judit Di ószegi Ali Abbas Mohammad Kurshed P éter Pikó Zsigmond K ósa J ános Sándor R óza Ádány Source Type: research
Association of single nucleotide polymorphisms with taste and food preferences of the Hungarian general and Roma populations
Appetite. 2021 Apr 27:105270. doi: 10.1016/j.appet.2021.105270. Online ahead of print.ABSTRACTIt is reasonable to suppose that poor diet underlies the unfavorable health status of the Roma population of Europe. Previously in the framework of a complex health survey, fruit and vegetable consumption, quantity of sugar added, salting frequency; bitter, salty, sweet and fat taste preferences were evaluated of Hungarian (HG, n=410) and Roma (HR, n=387) populations. In the present study the associations of taste and food preferences with TAS1R3, CD36, SCNN1B, TRPV1, TAS2R38, TAS2R19 and CA6 polymorphisms were tested in the same ...
Source: Appetite - April 30, 2021 Category: Nutrition Authors: Judit Di ószegi Ali Abbas Mohammad Kurshed P éter Pikó Zsigmond K ósa J ános Sándor R óza Ádány Source Type: research
