scholarly journals Effects of Osthol Isolated from Cnidium monnieri Fruit on Urate Transporter 1

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2837 ◽  
Author(s):  
Yuusuke Tashiro ◽  
Ryo Sakai ◽  
Tomoko Hirose-Sugiura ◽  
Yukio Kato ◽  
Hirotaka Matsuo ◽  
...  
Keyword(s):  
Uric Acid ◽  
Active Ingredient ◽  
Folk Medicine ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Mature Fruit ◽  
Urate Transporter ◽  
New Chemical Entities ◽  
Crude Drugs ◽  
Inhibitory Potential

(1) Background: Crude drugs used in traditional Japanese Kampo medicine or folk medicine are major sources of new chemical entities for drug discovery. We screened the inhibitory potential of these crude drugs against urate transporter 1 (URAT1) to discover new drugs for hyperuricemia. (2) Methods: We prepared the MeOH extracts of 107 different crude drugs, and screened their inhibitory effects on URAT1 by measuring the uptake of uric acid by HEK293/PDZK1 cells transiently transfected with URAT1. (3) Results: We found that the extract of the dried mature fruit of Cnidium monnieri inhibited urate uptake via URAT1. We isolated and identified osthol as the active ingredient from this extract. Osthol noncompetitively inhibited URAT1 with an IC50 of 78.8 µM. We evaluated the effects of other coumarins and found that the prenyl group, which binds at the 8-position of coumarins, plays an important role in the inhibition of URAT1. (4) Conclusions: Cnidium monnieri fruit may be useful for the treatment of hyperuricemia or gout in traditional medicine, and its active ingredient, osthol, is expected to be a leading compound for the development of new drugs for hyperuricemia.

scholarly journals Total Phenolics, Flavonoids, Condensed Tannins Content of Eight Centaurea Species and Their Broad Inhibitory Activities against Cholinesterase, Tyrosinase, α-Amylase and α-Glucosidase

2016 ◽  
Vol 44 (1) ◽  
pp. 195-200 ◽  
Author(s):  
Gokhan ZENGIN ◽  
Marcello LOCATELLI ◽  
Simone CARRADORI ◽  
Andrei M. MOCAN ◽  
Abdurrahman AKTUMSEK
Keyword(s):  
Ethyl Acetate ◽  
Condensed Tannins ◽  
Total Phenolics ◽  
Condensed Tannin ◽  
Folk Medicine ◽  
Chloroform Extract ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Synthetic Drugs ◽  
Starting Point

Several bioactive compounds originate from natural sources and their uses are generally related with traditional or folk medicine. Synthetic drugs can have adverse side effects and, for this reason, the investigation of novel, safe, and natural-occurring products can account for the development of new drugs. The genus Centaurea L. is one of the most important genera of the Asteraceae family, containing more than 200 species in the Turkish flora, about 140 of which are endemic. The aim of the present work was to determine enzyme inhibitory potentials of two extracts (chloroform and ethyl acetate) from eight Centaurea species against cholinesterase, tyrosinase, amylase, and glucosidase. The total phenolics, flavonoids and condensed tannin contents were also reported for each extract. These components in the extracts varied according to species and extraction solvents as well as enzyme inhibitory effects. The highest level of phenolics was found to be in the chloroform extract of C. pulchella (119.23 mg GAEs/g extract). Generally, chloroform extracts exhibited stronger enzyme inhibitory effects as compared to ethyl acetate. Additionally, possible correlations with total phenolics, flavonoids, and condensed tannins content were also highlighted. This paper is the first report of the inhibitory capacities of the eight Centaurea species on the selected enzymes. The present results may be a valuable starting point in the development of new bioactive formulations.

scholarly journals Serum uric acid, disease severity and outcomes in COVID-19

Critical Care ◽  
2021 ◽  
Vol 25 (1) ◽  
Author(s):  
Inès Dufour ◽  
Alexis Werion ◽  
Leila Belkhir ◽  
Anastazja Wisniewska ◽  
Marie Perrot ◽  
...  
Keyword(s):  
Mechanical Ventilation ◽  
Uric Acid ◽  
Respiratory Failure ◽  
Confidence Interval ◽  
Proximal Tubule ◽  
Disease Severity ◽  
Serum Levels ◽  
Kidney Proximal Tubule ◽  
Urate Transporter ◽  
Low Serum

Abstract Background The severity of coronavirus disease 2019 (COVID-19) is highly variable between individuals, ranging from asymptomatic infection to critical disease with acute respiratory distress syndrome requiring mechanical ventilation. Such variability stresses the need for novel biomarkers associated with disease outcome. As SARS-CoV-2 infection causes a kidney proximal tubule dysfunction with urinary loss of uric acid, we hypothesized that low serum levels of uric acid (hypouricemia) may be associated with severity and outcome of COVID-19. Methods In a retrospective study using two independent cohorts, we investigated and validated the prevalence, kinetics and clinical correlates of hypouricemia among patients hospitalized with COVID-19 to a large academic hospital in Brussels, Belgium. Survival analyses using Cox regression and a competing risk approach assessed the time to mechanical ventilation and/or death. Confocal microscopy assessed the expression of urate transporter URAT1 in kidney proximal tubule cells from patients who died from COVID-19. Results The discovery and validation cohorts included 192 and 325 patients hospitalized with COVID-19, respectively. Out of the 517 patients, 274 (53%) had severe and 92 (18%) critical COVID-19. In both cohorts, the prevalence of hypouricemia increased from 6% upon admission to 20% within the first days of hospitalization for COVID-19, contrasting with a very rare occurrence (< 1%) before hospitalization for COVID-19. During a median (interquartile range) follow-up of 148 days (50–168), 61 (12%) patients required mechanical ventilation and 93 (18%) died. In both cohorts considered separately and in pooled analyses, low serum levels of uric acid were strongly associated with disease severity (linear trend, P < 0.001) and with progression to death and respiratory failure requiring mechanical ventilation in Cox (adjusted hazard ratio 5.3, 95% confidence interval 3.6–7.8, P < 0.001) or competing risks (adjusted hazard ratio 20.8, 95% confidence interval 10.4–41.4, P < 0.001) models. At the structural level, kidneys from patients with COVID-19 showed a major reduction in urate transporter URAT1 expression in the brush border of proximal tubules. Conclusions Among patients with COVID-19 requiring hospitalization, low serum levels of uric acid are common and associate with disease severity and with progression to respiratory failure requiring invasive mechanical ventilation.

The Pharmacological and Pathological Studies on Taiwan Folk Medicine (VI): The Effects of Elephantopus scaber subsp. oblanceolata, E. mollis and Pseudoelephantopus spicatus

1991 ◽  
Vol 19 (01) ◽  
pp. 41-50 ◽  
Author(s):  
Chun-Ching Lin ◽  
Ming-Hong Yen ◽  
Hui-Fen Chiu
Keyword(s):  
Protective Effect ◽  
Liver Enzyme ◽  
Folk Medicine ◽  
Serum Transaminase ◽  
Functional Test ◽  
Fatty Metamorphosis ◽  
Elephantopus Scaber ◽  
Acute Increase ◽  
Crude Drugs

The liver protective effect of Elephantopus scaber subsp. oblanceolata, E. mollis and Pseudoelephantopus spicatus on CCL 4 induced hepatotoxicity has been determined by liver enzyme functional test and pathological studies. As the result indicatep, the acute increase of serum transaminase (SGOT and SGPT level which was caused by CCL 4 administration (3.0ml/kg, s.c.) can be significantly reduced when treating with E. scaber subsp. oblanceolata( p < 0.001), E. mollis( p < 0.01), P. spicatus( p < 0.01). The hepatic fatty metamorphosis and necrosis of central lobule were obviously improved by treating with E. scaber subsp. oblanceolata and E. mollis, while treated with P. spicatus demonstrated only a moderate protective effect. All pharmacological and pathological effects of these three crude drugs were compared with Bupleurum chinense which has been reported previously as a treatment criteria.

scholarly journals Purification, Preliminary Characterization, and Immunological Activity of Polysaccharides from Crude Drugs of Sijunzi Formula

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Yunfei Ji ◽  
Ruijun Wang ◽  
Ying Peng ◽  
Chongsheng Peng ◽  
Xiaobo Li
Keyword(s):  
Monosaccharide Composition ◽  
Raw 264.7 Cells ◽  
No Production ◽  
Inhibitory Effects ◽  
Immunological Activity ◽  
Spleen Deficiency ◽  
Radix Glycyrrhizae ◽  
Crude Drugs ◽  
The Complement System ◽  
Necrosis Factor

Sijunzi Decoction (SJZD) is a conventional prescription for curing spleen deficiency in Traditional Chinese Medicine and polysaccharide is its main ingredient. In order to explore the effective ingredients contributing to the immunological activity of SJZD, we isolated and purified seven homogeneous polysaccharides from Radix Ginseng (RS-3-1 and RS-3-2), Rhizoma Atractylodis Macrocephalae (BZ-3-1, BZ-3-2, and BZ-3-3), Poria (FL-3-1), and Radix Glycyrrhizae (GC-3-1) decoctions, respectively. The molecular weight of seven homogeneous polysaccharides ranged from 5.42 × 104 to 5.65 × 104 Da. Monosaccharide composition determined by GC-MS analysis showed that these polysaccharides were primarily composed of Rha, Ara, Xyl, Man, Glc, and Gal with various ratios. Immunological activity assay revealed that polysaccharides from four crude drug components of SJZD displayed inhibitory effects on the complement system. RS-3-1, BZ-3-1, FL-3-1, and GC-3-1 could significantly enhance the phagocytosis and increase the NO production and tumor necrosis factor (TNF-α) level in RAW 264.7 cells (p<0.05). These results demonstrated the immunological activities of these polysaccharides from the four crude drugs. This study supports the therapeutic effect of SJZD in clinical use and is essential for further identification the immunopolysaccharide from SJZD decoction.

scholarly journals Effect of Fenofibrate on Uric Acid Metabolism and Urate Transporter 1

2010 ◽  
Vol 49 (2) ◽  
pp. 89-94 ◽  
Author(s):  
Daijiro Uetake ◽  
Iwao Ohno ◽  
Kimiyoshi Ichida ◽  
Yuichiro Yamaguchi ◽  
Hajime Saikawa ◽  
...  
Keyword(s):  
Uric Acid ◽  
Acid Metabolism ◽  
Urate Transporter

scholarly journals Formulation and Evaluation of Wound Healing Effect of Aqueous Herbal Cream Containing Various Extracts of Passiflora foetida Linn., Leaves

2019 ◽  
pp. 490-499
Author(s):  
Akila E ◽  
C. Geetha Priya
Keyword(s):  
Wound Healing ◽  
Chronic Wounds ◽  
Soft Tissues ◽  
Folk Medicine ◽  
New Drugs ◽  
Herbal Remedies ◽  
Control Group ◽  
Wound Model ◽  
Number Of Patients ◽  
Passiflora Foetida

Wounds are a major cause of concern for the patient and clinician alike; chronic Wounds affect a large number of patients and seriously reduce their quality of life. Wound healing is the process of repair that follows injury to the skin and other soft tissues. A cream is a preparation of a medication for topical use that contains a water base. Essentially, it is a preparation of oil in water. Herbal remedies used in folk medicine provide an interesting and still largely unexplored source for the creation and development of potentially new drugs, which might help to overcome the growing problem of resistance and also the toxicity of the currently available commercial antibiotics. In this study we have formulated an Aqueous herbal cream satisfying almost all pharmaceutical parameters which shows better wound healing activity. The wound healing of effect of Aqueous Herbal cream of various extracts of leaves of Passiflora foetida L. was evaluated by incision and excision wound model. The experimental results and histopathological studies showed that Aqueous Herbal Cream of Passiflora foetida L. leaves exhibits significant wound healing property as compared to control group of animals.

scholarly journals Sickle hemoglobin polymerization and antisickling medicinal plants

2021 ◽  
Vol 10 (2) ◽  
pp. 126-133
Author(s):  
Franklyn O. Ohiagu ◽  
◽  
Paul C. Chikezie ◽  
Chinwendu M. Chikezie ◽  
◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Transplant Rejection ◽  
Gene Replacement ◽  
New Drugs ◽  
Cell Disease ◽  
Inhibitory Effects ◽  
Therapeutic Approaches ◽  
Sickle Hemoglobin ◽  
Adverse Health Effects ◽  
Gene Replacement Therapy

Sickle cell disease (SCD) is a dilapidating disorder that is associated with organ destruction and decreased life expectancy. Therapeutic remedies that lead to fundamental cure of SCD such as, bone marrow and stem cell transplantations, as well as gene replacement therapy, are very costly and unaffordable to the disease sufferers in developing countries. In regions where these therapeutic approaches are possible, there are also limitations such as immunologic transplant rejection, difficulty in prognosis, difficulty in obtaining a suitable donor, end-organ dysfunction, and adverse health effects, especially among the older sufferers of this disease. The eagerness of researchers to develop new drugs for the amelioration of the crisis associated with SCD and a possible cure of the disease has led to the discovery of biomolecular agents that inhibit the mechanisms of HbS polymerization as well as medicinal plants with antisickling potentials. The antisickling potency of medicinal plants should be harnessed through research funding and efforts geared towards the discovery of molecules in such plants with HbS polymerization inhibitory effects.

scholarly journals Inhibitory effects of pentamidine analogues on protein biosynthesis in vitro.

2000 ◽  
Vol 47 (1) ◽  
pp. 113-120 ◽  
Author(s):  
K Bielawski ◽  
A Galicka ◽  
A Bielawska ◽  
K Sredzińska
Keyword(s):  
Protein Biosynthesis ◽  
Elongation Factor ◽  
Inhibitory Effect ◽  
New Drugs ◽  
Clinical Use ◽  
Inhibitory Effects ◽  
Inhibit Protein Synthesis ◽  
Primary Target ◽  
Eukaryotic Elongation Factor

Pentamidine despite its rather high toxicity, is currently in clinical use. For development of new drugs of this type it is important to know the mechanism of their action. Two new amidines (I and II) and 4',6-diamidino-2-phenylindole (DAPI) were found in preliminary experiments to inhibit protein synthesis in vitro in the cell-free rat liver system. The three compounds differed in the precise mode of action. The inhibitory effect of I on the activity of the eukaryotic elongation factor eEF-2 and ribosomes seems to suggest that the binding site of eEF-2 on the ribosome was blocked by this compound. eEF-2 has been identified as the primary target of II and eEF-1 as the primary target of DAPI in the system studied.

Therapeutic and Pharmaceutical Potential of Cinnamon

2022 ◽  
pp. 698-710
Author(s):  
Neha Mishra ◽  
Rashmi Srivastava
Keyword(s):  
Wide Spectrum ◽  
Folk Medicine ◽  
Common Species ◽  
New Drugs ◽  
Bioactive Constituents ◽  
Rheumatic Arthritis ◽  
The Family ◽  
Pharmacological Studies ◽  
Therapeutic Properties ◽  
The Himalaya

Cinnamon has been used as a spice, condiment, and aromatic plant since centuries ago. Cinnamon is a small evergreen tree belonging to the genus Cinnamomum in the family Lauraceae. There are more than 250 species of cinnamon worldwide. In India, Cinnamomum verum and Cinnamomum cassia are the most common species grown in the Himalaya region. They have been used as folk medicine for the treatment of nausea, flatulent dyspepsia, coughs, diarrhea, malaria, gastric disorder, and to alleviate pain and inflammation in rheumatic arthritis. Therapeutic properties of cinnamon are due to the presence of bioactive constituents such as p-coumaric, cinnamaldehyde, cinnamic acid, and eugenol. Cinnamaldehyde and eugenol are the major active constituents responsible for its characteristic flavor, aroma, and therapeutic properties. Pharmacological studies found that it could be a promising candidate with potential for designing new drugs. This review is aimed to summarize the ethanomedicinal importance, phytochemistry, and wide spectrum of pharmacological and therapeutic applications of cinnamon.

Sign in / Sign up

Export Citation Format

Share Document