Bioassay-Guided Separation of an α-Amylase Inhibitor Anthocyanin from Vaccinium arctostaphylos Berries

2010 ◽  
Vol 65 (9-10) ◽  
pp. 567-570 ◽  
Author(s):  
Bahman Nickavar ◽  
Gholamreza Amin
Keyword(s):  
Diabetes Mellitus ◽  
Medicinal Plant ◽  
Inhibitory Effect ◽  
Natural Sources ◽  
Amylase Inhibitor ◽  
Treatment Of Diabetes ◽  
Dose Dependent

Vaccinium arctostaphylos is a traditional medicinal plant in Iran used for the treatment of diabetes mellitus. In our search for antidiabetic compounds from natural sources, we found that the extract obtained from V. arctostaphylos berries showed an inhibitory effect on pancreatic α-amylase in vitro [IC50 = 1.91 (1.89 -1.94) mg/mL]. The activity-guided purification of the extract led to the isolation of malvidin-3-O-β-glucoside as an α-amylase inhibitor. The compound demonstrated a dose-dependent enzyme inihibitory activity [IC50 = 0.329 (0.316 - 0.342) mM].

scholarly journals In Vitro Effects of Doxycycline on Replication of Feline Coronavirus

Pathogens ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 312
Author(s):  
Magdalena Dunowska ◽  
Sayani Ghosh
Keyword(s):  
Inhibitory Concentration ◽  
Infectious Virus ◽  
Treatment Options ◽  
Inhibitory Effect ◽  
Virus Titration ◽  
Reverse Transcription Quantitative Pcr ◽  
In Vitro Effects ◽  
Dose Dependent ◽  
Feline Coronavirus

Feline infectious peritonitis (FIP) is a sporadic fatal disease of cats caused by a virulent variant of feline coronavirus (FCoV), referred to as FIP virus (FIPV). Treatment options are limited, and most of the affected cats die or are euthanized. Anecdotally, doxycycline has been used to treat FIP-affected cats, but there are currently no data to support or discourage such treatment. The aim of this study was to establish whether doxycycline inhibits replication of FIPV in vitro. The virus was cultured in Crandell-Rees feline kidney cells with various concentrations of doxycycline (0 to 50 µg/mL). The level of FIPV in cultures was determined by virus titration and FCoV-specific reverse-transcription quantitative PCR. Cell viability was also monitored. There was no difference in the level of infectious virus or viral RNA between doxycycline-treated and untreated cultures at 3, 12- and 18-hours post-infection. However, at 24 h, the growth of FIPV was inhibited by approximately two logs in cultures with >10 µg/mL doxycycline. This inhibition was dose-dependent, with inhibitory concentration 50% (IC50) 4.1 µg/mL and IC90 5.4 µg/mL. Our data suggest that doxycycline has some inhibitory effect on FIPV replication in vitro, which supports future clinical trials of its use for the treatment of FIP-affected cats.

scholarly journals In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

Abstract Background Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Methods Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Results Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1. Conclusions The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.

Immunomodulatory activities of whey fractions in efferent prefemoral lymph of sheep

1996 ◽  
Vol 63 (2) ◽  
pp. 257-267 ◽  
Author(s):  
Chun W. Wong ◽  
Geoffrey O. Regester ◽  
Geoffrey L. Francis ◽  
Dennis L. Watson
Keyword(s):  
Immune Responses ◽  
Bovine Milk ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Milk Whey ◽  
Significant Difference ◽  
Lymphocyte Phenotypes ◽  
Dose Dependent

SummaryStudies on the immunomodulatory activities of ruminant milk and colostral whey fractions were undertaken. By comparing with boiled colostral whey in a preliminary experiment, a putative heat-labile immunostimulatory factor for antibody responses was found to be present in ovine colostral whey. Studies were then undertaken in sheep in which the efferent prefemoral lymphatic ducts were cannulated bilaterally, and immune responses in the node were measured following subcutaneous injection in the flank fold of whey protein preparations of various purities. A significant sustained decline of efferent lymphocyte output was observed following injection with autologous crude milk whey or colostral whey preparations, but no changes were observed in interferon-gamma levels in lymph plasma. Two bovine milk whey fractions (lactoperoxidase and lactoferrin) of high purity were compared in bilaterally cannulated sheep. A transient decline over the first 6 h was seen in the efferent lymphocyte output and lymph flow rate after injection of both fractions. A significant difference was seen between the two fractions in interferongamma levels in lymph at 6 h after injection. However, no significant changes in the proportion of the various efferent lymphocyte phenotypes were seen following either treatment. Whereas both fractions showed a significant inhibitory effect in a dose-dependent manner on the proliferative response of T lymphocytes, but not B lymphocytes, to mitogenic stimulation in vitro, no similar changes were seen following in vivo stimulation with these two fractions.

scholarly journals In vitro inhibitory effect of obtusofolin on the activity of CYP3A4, 2C9, and 2E1

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Na Liu ◽  
Ping Chen ◽  
Xiaojun Du ◽  
Junxia Sun ◽  
Shasha Han
Keyword(s):  
Human Liver ◽  
Competitive Inhibition ◽  
Liver Microsomes ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Inhibition Model ◽  
Dose Dependent

Abstract Background Obtusofolin is the major active ingredient of Catsia tora L., which possesses the activity of improving eyesight and protecting the optic nerve. Investigation on the interaction of obtusofolin with cytochrome P450 enzymes (CYP450s) could provide a reference for the clinical application of obtusofolin. Methods The effect of obtusofolin on the activity of CYP450s was investigated in the presence of 100 μM obtusofolin in pooled human liver microsomes (HLMs) and fitted with the Lineweaver–Burk plots to characterize the specific inhibition model and kinetic parameters. Results Obtusofolin was found to significantly inhibited the activity of CYP3A4, 2C9, and 2E1. In the presence of 0, 2.5, 5, 10, 25, 50, and 100 μM obtusofolin, the inhibition of these CYP450s showed a dose-dependent manner with the IC50 values of 17.1 ± 0.25, 10.8 ± 0.13, and 15.5 ± 0.16 μM, respectively. The inhibition of CYP3A4 was best fitted with the non-competitive inhibition model with the Ki value of 8.82 μM. While the inhibition of CYP2C9 and 2E1 was competitive with the Ki values of 5.54 and 7.79 μM, respectively. After incubating for 0, 5, 10, 15, and 30 min, the inhibition of CYP3A4 was revealed to be time-dependent with the KI value of 4.87 μM− 1 and the Kinact value of 0.0515 min− 1. Conclusions The in vitro inhibitory effect of obtusofolin implying the potential drug-drug interaction between obtusofolin and corresponding substrates, which needs further in vivo validations.

scholarly journals Preliminary in vitro study of anti-oxidant activity and anti-diabetic potential of plant extracts from 4 herbal substances not traditionally used for treatment of diabetes mellitus

Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 755-762
Author(s):  
Dora Trifonova ◽  
Anna Gavrilova ◽  
Galina Dyakova ◽  
Genadi Gavrilov ◽  
Maya Yotova ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Biologically Active ◽  
Total Phenolic ◽  
Water Extracts ◽  
Sambucus Ebulus ◽  
Anti Oxidant ◽  
Treatment Of Diabetes

The focus of the presented study is the in vitro anti-oxidant activity and anti-diabetic potential of water extracts from the following four herbal substances, not traditionally used for treatment of diabetes mellitus – leaves of Sambucus ebulus L. and Prunus mahaleb L., and flowering stems of Cichorium intybus L. and Satureja kitaibelii Wierzb. ex Heuff. The water extracts are obtained through ultrasonication. The extract of S. kitaibelii stands out due to its highest values in all studied indicators – total phenolic content, scavenging potential (DPPH, ABTS) and α-glucosidase inhibitory activity which was six times higher than acarbose. The extract of C. intybus also showed significant α-glucosidase inhibitory activity compared to acarbose. The flowering stems of both species are promising sources of biologically active substances for blood sugar control in diabetes mellitus.

Antinociceptive properties of shikonin: in vitro and in vivo studies

2016 ◽  
Vol 94 (7) ◽  
pp. 788-796 ◽  
Author(s):  
Bhawana Gupta ◽  
Sabyasachi Chakraborty ◽  
Soumya Saha ◽  
Sunita Gulabsingh Chandel ◽  
Atul Kumar Baranwal ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Inhibitory Effect ◽  
Pain Modulation ◽  
In Vivo Studies ◽  
Channel Modulation ◽  
Pain Models ◽  
A Cell ◽  
Dose Dependent

Shikonin possess a diverse spectrum of pharmacological properties in multiple therapeutic areas. However, the nociceptive effect of shikonin is not largely known. To investigate the antinociceptive potential of shikonin, panel of GPCRs, ion channels, and enzymes involved in pain pathogenesis were studied. To evaluate the translation of shikonin efficacy in vivo, it was tested in 3 established rat pain models. Our study reveals that shikonin has significant inhibitory effect on pan sodium channel/N1E115 and NaV1.7 channel with half maximal inhibitory concentration (IC50) value of 7.6 μmol/L and 6.4 μmol/L, respectively, in a cell-based assay. Shikonin exerted significant dose dependent antinociceptive activity at doses of 0.08%, 0.05%, and 0.02% w/v in pinch pain model. In mechanical hyperalgesia model, dose of 10 and 3 mg/kg (intraperitoneal) produced dose-dependent analgesia and showed 67% and 35% reversal of hyperalgesia respectively at 0.5 h. Following oral administration, it showed 39% reversal at 30 mg/kg dose. When tested in first phase of formalin induced pain, shikonin at 10 mg/kg dose inhibited paw flinching by ∼71%. In all studied preclinical models, analgesic effect was similar or better than standard analgesic drugs. The present study unveils the mechanistic role of shikonin on pain modulation, predominantly via sodium channel modulation, suggesting that shikonin could be developed as a potential pain blocker.

The Indian Medicinal Plant Aegle marmelos in the Treatment of Diabetes Mellitus

2013 ◽  
pp. 519-536
Author(s):  
P.L. Palatty ◽  
A.R. Shivashankara ◽  
M.S. Baliga ◽  
A. Jaiswal ◽  
P. Pankaj ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Medicinal Plant ◽  
Aegle Marmelos ◽  
Indian Medicinal Plant ◽  
Treatment Of Diabetes

scholarly journals Antidiabetic Mechanisms of Rosa canina Fruits

2016 ◽  
Vol 22 (1) ◽  
pp. 127-133 ◽  
Author(s):  
Ali Fattahi ◽  
Fatemeh Niyazi ◽  
Behzad Shahbazi ◽  
Mohammad Hosein Farzaei ◽  
Gholamreza Bahrami
Keyword(s):  
Diabetes Mellitus ◽  
Cell Line ◽  
Mechanism Of Action ◽  
Glucose Absorption ◽  
Rosa Canina ◽  
Glucose Diffusion ◽  
Treatment Of Diabetes ◽  
Hepatocellular Carcinoma Cell Line ◽  
Natural Agent

Rosa canina fruits have been used traditionally for the treatment of diabetes mellitus and its complications. The aim of current study was to evaluate the in vitro mechanism of action of R canina in managing diabetes mellitus. Cell proliferation and cytotoxicity assay were performed on pancreatic β-cells, βTC6. The protective activity of the extract on streptozotocin-induced death in βTC6 cells was studied. The effect of R canina on the metabolism of glucose in HepG2, a hepatocellular carcinoma cell line, was evaluated. The effect of the extract on glucose diffusion across the dialysis membrane, which is a comfortable model for assessing cellular glucose absorption, was evaluated. The results obtained from current study confirmed that R canina extract can act as a growth factor for pancreatic β-cell line providing a novel mechanism for the observed antidiabetic effect of this natural agent. Further preclinical studies are necessary to evaluate the perfect mechanism of action of R canina in diabetes mellitus.

scholarly journals In Vitro Effect of Local Anesthetics onCandida albicansGerm Tube Formation

1994 ◽  
Vol 1 (4) ◽  
pp. 193-197 ◽  
Author(s):  
Acácio Rodrigues ◽  
Cidália Pina Vaz ◽  
A. Freitas Fonseca ◽  
J. Martinez de Oliveira ◽  
Henrique Barros
Keyword(s):  
Germ Tube ◽  
Inhibitory Effect ◽  
Tube Formation ◽  
Vaginal Candidiasis ◽  
Sabouraud Agar ◽  
Colony Forming Units ◽  
Vitro Effect ◽  
Phosphate Buffered Saline ◽  
Dose Dependent

Objective:This study was planned to clarify the in vitro effect of lidocaine and bupivacaine on germ tube formation byCandida albicansisolates from cases of clinical vaginal candidiasis.Methods:FourteenC. albicansstrains (clinical vaginal isolates) were grown on Sabouraud agar for 24 h at 37℃ and tested as follows: 100 μl of a yeast suspension [105colony forming units (CFU)/ml of phosphate buffered saline (PBS)] was added to 500 μl of fresh human serum with lidocaine or bupivacaine (pure salts) in serial concentrations. The test was run in duplicate. Controls were prepared for each strain. After 4 h of incubation at 37℃, samples were taken from each vial and 200 yeasts were counted in a counting chamber. The pH of each suspension was measured.Results:The results are given as the mean of the 2 readings and are expressed as the percentage of blastoconidia with germ tubes/total blastoconidia.Conclusions:Our experiments show that both lidocaine and bupivacaine have a dose-dependent inhibitory effect, pH-independent, on germ tube formation byC. albicansand that both drugs seem to be promising in the treatment of genital candidiasis due to the combination of anesthetic and antifungal properties.

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