scholarly journals Quantitative standardization of pharmacologically active components from antiplasmodial plant Solanum nudum Dunal (wild and in vitro)

2022 ◽  
Vol 21 (1) ◽  
pp. 41-50
Author(s):  
Ana Maria Mesa-Vanegas ◽  
◽  
Esther Julia Naranjo-Gomez ◽  
Felipe Cardona ◽  
Lucia Atehortua-Garces ◽  
...  
Keyword(s):  
Pacific Coast ◽  
Inhibitory Concentration ◽  
Quality Parameter ◽  
Antimalarial Treatment ◽  
Active Components ◽  
Steroidal Compound ◽  
Pharmacologically Active ◽  
Article Study ◽  
Over Time

Solanum nudum Dunal (Solanaceae) is most commonly known and used by the population of the colombian Pacific coast as an antimalarial treatment. This article study into optimization and quantitative analysis of compounds steroidal over time of development of this species when grown in vitro and wild. A new steroidal compound named SN6 was elucidated by NMR and a new method of quantification of seven steroidal compounds (Diosgenone DONA and six steroids SNs) using HPLC-DAD-MS in extracts of cultures in vitro and wild was investigated. Biology activity of extracts was found to a range of antiplasmodial activity in FCB2 and NF-54 with inhibitory concentration (IC50) between (17.04 -100 μg/mL) and cytotoxicity in U-937 of CC50 (7.18 -104.7 μg/mL). This method creates the basis for the detection of seven sterols antiplasmodial present in extracts from S. nudum plant as a quality parameter in the control and expression of phytochemicals.

scholarly journals In vitro antimicrobial activity of plant active components against Pseudomonas lundensis and Listeria monocytogenes

2020 ◽  
Author(s):  
Khabat Noori Hussein ◽  
Tímea Molnár ◽  
Richard Pinter ◽  
Adrienn Toth ◽  
Emna Ayari ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Listeria Monocytogenes ◽  
Inhibitory Concentration ◽  
Agar Plate ◽  
Diffusion Method ◽  
Active Components ◽  
Plate Method ◽  
Gradient Plate ◽  
Strong Antimicrobial Activity

AbstractThis work aimed to study the antimicrobial activity of eight various components of plant origin on the growth of Pseudomonas lundensis and Listeria monocytogenes. Different in vitro methods were used: agar plate diffusion, micro atmosphere, agar hole diffusion, micro-dilution, and gradient-plate method. In the first agar plate assay, p-cymene and γ-terpinene did not inhibit the growth of the tested bacteria therefore they were not used in further experiments. Both α-pinene and limonene were only partially effective, but these were screened only for their partial inhibition. The other four components completely inhibited the growth of the tested bacteria. Using the agar-well diffusion method showed that carvacrol and thymol were found to be the most effective active components, thymol had minimum inhibitory concentration (MIC) at 1.563 mg/mL, however, in the case of carvacrol, MIC was 7.813 μL/mL. Additionally, eugenol and camphor show the same results but in higher concentrations. Gradient plate method was used to determine MIC values, in which it has been proved that carvacrol and thymol possess strong antimicrobial activity, no growth of tested bacteria was observed with carvacrol (100 μL/mL), while thymol exhibited MIC of 1.887 mg/mL against P. lundensis and 0.943 mg/mL needed to show complete inhibition of Listeria monocytogenes. Further experiments are needed to determine the optimum concentrations of the active components against P. lundensis and L. monocytogenes.

Absorption, metabolism, and excretion of 14C gimatecan (LBQ707) after oral administration in patients with advanced cancer

2007 ◽  
Vol 25 (18_suppl) ◽  
pp. 2564-2564 ◽  
Author(s):  
M. M. Woo ◽  
L. Rodriguez ◽  
H. Gu ◽  
K. Crenshaw-Williams ◽  
F. Rocha ◽  
...  
Keyword(s):  
Advanced Cancer ◽  
Topoisomerase I ◽  
Oral Absorption ◽  
Total Radioactivity ◽  
Fecal Excretion ◽  
Active Components ◽  
Good Tolerability ◽  
Radiometric Detection ◽  
Pharmacologically Active

2564 Background: Gimatecan (Gim), a new potent oral topoisomerase I inhibitor is a lipophilic 7-oxyiminomethyl derivative of camptothecin. Its in vitro cytoxicity is more sustained than CPT-11 and topotecan, it has excellent anti-tumor activity in mouse xenografts, and shown good tolerability with Ph I activity. The study aim was to profile its disposition in cancer patients. Methods: 4 patients with advanced cancer received a single oral 1.5 mg dose of [14C] Gim (60 μCi) followed by standard Gim treatment on Day 15. Whole blood, plasma, urine, and feces were collected over 7 days with spot fecal collections up to Day 19. Total radioactivity was measured by liquid scintillation counting. Gim and metabolite concentrations in plasma and excreta were measured by LC- MS/MS and HPLC with radiometric detection. Results: Gim showed a rapid first-order absorption and a long elimination phase and was well tolerated. The median (range) Tmax for Gim was 1 h (0.5 to 3 h) and mean t1/2 and oral clearance values were 91 h and 0.6 L/h, respectively. Gim was the major moiety and its active metabolite LCF775 (t-butyl-mono-hydroxy Gim) was the main metabolite (albeit minor, 2–9%) in plasma. Trace glucuronide and sulfate metabolites were also detected in plasma. Mean recovery of radioactivity in urine (0-Day 7) and feces (0-Day 11) was 70.5 % (56.2–80.0%) of the dose. Incomplete recovery is attributed to opiates use in 2 patients and incomplete (sporadic) fecal sampling at later timepoints. Fecal excretion (0-Day 11) was prolonged and major in 3/4 patients (46- 73% of the dose, of which 14–23% is the unchanged Gim suggesting the drug is well absorbed). An additional 1.3–3.5% was recovered in spot collections (Days 14, 15 and 19). Urine excretion (0-Day 7) was 7.2–10.3% of the dose in 3 patients, one patient (cachectic, on opiates) excreted only 21% in feces and 46% in urine. Gim and several Gim metabolites (and glucuronide conjugates thereof) were the major components in excreta. Conclusions: Gim and its minor metabolite, LCF775 were the principal pharmacologically active components in plasma. Fecal excretion is the main elimination pathway in most patients. A long half-life (90hr) of Gim, uncomplicated metabolism, and good oral absorption make Gim an attractive candidate for Ph II development. [Table: see text]

IN VITRO CHARACTERIZATION OF ANTIFUNGAL ACTIVITY OF SELECTED ESSENTIAL OILS

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (12) ◽  
pp. 61-64
Author(s):  
C. Rath Chandi ◽  
A. Samal
Keyword(s):  
Antifungal Activity ◽  
Essential Oils ◽  
Inhibitory Concentration ◽  
Inhibition Mechanism ◽  
Active Components ◽  
Irreversible Damage ◽  
Antifungal Activities ◽  
In Vitro Characterization

Antifungal activity of seven essential oils was studied primarily against C. albicans and E. floccosum. Four essential oils viz. turmeric, palmarosa, lemongrass and citronella, that revealed better antifungal activities during screening, were characterized further. Minimum Inhibitory concentration (MIC) and phenol coefficient values of the oils ranged between 0.97 to 62.5 µl/ml and 0125 to 0.75 respectively. The oils retained the antifungal activities when treated at high temperature (1000 C for 1h) and pressure (autoclaved), indicating presence of thermostable and barostable active components in them. The oils also resisted sonication (33,000Hz for 30min) and revealed antifungal activities against the two pathogens. Immediate killing of E. floccosum, is attributable to an irreversible damage to the cells. Antifungal activity of these oils as recorded during the study, could be attributable to the membrane inhibition mechanism and was observed to be fungicidal in nature.

scholarly journals Inhibitory effects of siwak (Salvadora persica. L) extract on the growth of Enterococcus faecalis planktonics and biofilms by in vitro

2016 ◽  
Vol 49 (3) ◽  
pp. 158
Author(s):  
Ika Rhisty Cendana Sari ◽  
Rini Devijanti Ridwan ◽  
Diah Savitri Ernawati
Keyword(s):  
Enterococcus Faecalis ◽  
Inhibitory Concentration ◽  
Secondary Infection ◽  
Surface Protein ◽  
Extracellular Polysaccharide ◽  
Assay Method ◽  
Inhibitory Effects ◽  
Active Components ◽  
Salvadora Persica

Background: Enterococcus faecalis (E. faecalis) is one of the most persistent gram positive bacteria in root canal, resulting in secondary infection after endodontic treatment. E. faecalis pathogenicity is caused by overgrowth of E. faecalis planktonics and biofilms. E. faecalis planktonics produce lipoteichoid acid (LTA) as a virulence factor that can defend their permeability cell. On the other hand, E. faecalis biofilms produce protease, such as Esp (enterococcal surface protein), GelE (gelatinase), and SprE (serin protease), that have quorum-sensing mechanism as an adhesion factor to form extracellular polysaccharide substance (EPS) and increase the growth of the biofilms themselves. Siwak (Salvadora persica L.) has active components, namely benzylisothio-cyanate, trimethylamine, and salvadorine that can inhibit the growth of E. faecalis planktonics and biofilms. Purpose: This study aimed to measure inhibitory effects of siwak extract on the growth of E. faecalis planktonics and biofilms. Method: This research was an antimicrobial research on the culture of E.faecalis incubated in a TSB medium. Siwak extract was diluted into different concentrations, namely 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, and 100%. The extract then was placed into the E. faecalis’s colony and planted into Trypticase Soy Agar medium. After incubated for 24 hours at 37°C, the colony would be measured and compared with the control (+) and control (-). As an antibiofilm research, this research used biofilm microtitter assay method to form E. faecalis biofilms incubated in a well-plate medium containing TSB and 0.1 % glucose. Siwak extract then was diluted into the same range concentration as in first method, and placed into the colony of E. faecalis to form biofilms. The biofilms were measured and compared to the control (+) given siwak extract and the control (-) given 0.1% chlorhexidine. After the incubation, they were washed three times, and staining process was conducted using Chrystal violet. The optical density then was measured by ELISA Reader 595 nm. Result: Siwak extract could inhibit the growth of E. faecalis planktonics at the concentration of 35% as a minimum inhibitory concentration as well as the growth of E. faecalis biofilms at the concentration of 45% as a minimum biofilm inhibitory concentration. Conclusion: Siwak extract has an inhibitory effect, particularly at a concentration of 35% on the growth of E. faecalis planktonics and at the concentration of 45% on the growth of E. faecalis biofilms.

scholarly journals A ten-year (2000–2009) study of antimicrobial susceptibility of bacteria that cause bovine respiratory disease complex—Mannheimia haemolytica, Pasteurella multocida, and Histophilus somni—in the United States and Canada

2012 ◽  
Vol 24 (5) ◽  
pp. 932-944 ◽  
Author(s):  
Ellen Portis ◽  
Cynthia Lindeman ◽  
Lacie Johansen ◽  
Gillian Stoltman
Keyword(s):  
Pasteurella Multocida ◽  
Inhibitory Concentration ◽  
The United States ◽  
Mannheimia Haemolytica ◽  
In Vitro Susceptibility ◽  
Histophilus Somni ◽  
Bovine Respiratory Disease Complex ◽  
Year 2000 ◽  
Over Time

Bovine isolates of Mannheimia haemolytica, Pasteurella multocida, and Histophilus somni, collected from 2000 to 2009, were tested for in vitro susceptibility to ceftiofur, penicillin, danofloxacin, enrofloxacin, florfenicol, tetracycline, tilmicosin, and tulathromycin. Ceftiofur remained very active against all isolates. Penicillin retained good activity against P. multocida and H. somni isolates with no appreciable changes in susceptibility or minimal inhibitory concentration (MIC) distributions with time. While there was no obvious trend, the percent of M. haemolytica that were susceptible to penicillin ranged from 40.9% to 66.7%. Danofloxacin MIC50 and MIC90 values for M. haemolytica and P. multocida did not change beyond a single dilution over the 6 years it was included in the testing panel. The MIC90 for H. somni increased beyond 1 dilution. Enrofloxacin MIC50 values for the 3 pathogens also did not change over time, unlike the MIC90 values, which increased by at least 4-doubling dilutions. Ninety percent or more of M. haemolytica and H. somni isolates were susceptible to florfenicol, while susceptibility among P. multocida was 79% or greater. Less than 50% of the isolates tested as susceptible to tetracycline in many of the years. All 3 organisms showed declines in tilmicosin and tulathromycin MIC50 and MIC90 values over the years in which they were tested.

scholarly journals Is In Vitro Antibiotic Combination More Effective than Single-Drug Therapy against Anthrax?

2005 ◽  
Vol 49 (4) ◽  
pp. 1323-1325 ◽  
Author(s):  
Abed Athamna ◽  
Muhammad Athamna ◽  
Aburashed Nura ◽  
Eli Shlyakov ◽  
Darrin J. Bast ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Antibacterial Efficacy ◽  
Bacterial Killing ◽  
Single Drug ◽  
Development Of Resistance ◽  
Single Drug Therapy ◽  
Time Kill ◽  
Synergistic Combinations ◽  
Over Time

ABSTRACT Antibiotic combinations are used to enhance antibacterial efficacy and to prevent the development of resistance. We have tested a possible synergistic effect of several antibacterial combinations on Bacillus anthracis. The in vitro activities of antibiotic combinations against two strains of B. anthracis, strain Sterne and the Russian anthrax vaccine strain STi, were tested by the fractional inhibitory concentration (FIC) method, derived from the MICs of the agents in combination, and by measuring the rate of bacterial killing over time by several antibiotic combinations. The FIC results showed that synergism against both B. anthracis strains was observed only with the combination of rifampin and clindamycin. The telithromycin-amoxicillin combination showed synergism against strain Sterne only. All other combinations were either indifferent or antagonistic. The results of the bacterial time-kill study demonstrated indifferent effects for all combinations. These in vitro results demonstrate the difficulties in obtaining synergistic combinations of antibiotics against B. anthracis.

scholarly journals APPLICATION OF ELICITOR FOR PRODUCTION OF SAPONINS FROM IN VITRO PANAX CULTURES

2018 ◽  
Vol 16 (2) ◽  
pp. 211-221
Author(s):  
Nguyen Thi Nhat Linh ◽  
Nguyen Hoang Loc ◽  
Duong Tan Nhut
Keyword(s):  
Metabolic Engineering ◽  
Large Scale ◽  
Optimal Solution ◽  
Scale Production ◽  
Triterpene Saponins ◽  
Active Components ◽  
Triterpene Saponin ◽  
Saponin Content ◽  
Pharmacologically Active

The Panax ginseng species are traditional medicinal herbs having high value. The major pharmacologically active components are the ginsenosides of saponin group, which are dammarane type triterpene glycosides containing a tetracyclic glycose. Ginseng saponin, one of the secondary metabolites, is necessary for the growth and development of Panax genus plants. In pharmaceutical industry, triterpene saponins were purified to produce drugs for its promising healing and restorative properties. However, commercial applications are still obstacle for practical problems, because ginseng natural resources are rarely precious; and ginseng resources from field have low and variable yields dependent on season or quality of soil. Moreover, triterpene saponins have complex structures, making chemical synthesis an economically uncompetitive option for large-scale production. A current alternative optimal solution that is popular in the world is the application of cell and tissue culture to produce a large of cell or root yield in short time. But the difficulty in producing triterpene saponins from in vitro culture is that the triterpene saponin content is much lower than natural. To increase the triterpene saponin content, elicitors are added to the culture medium. Based on the effect of the elicitor, metabolic engineering in vitro is also able to enhance the overexpression of genes which translated enzymes or signals producing saponin in the isoprenoid pathway. Application of elicitor researches could improve triterpene saponin yields or adjust specific desired triterpene saponins from in vitro ginseng culture. Therefore, we review the recent studies of elicitor in Panax genus cultures and saponin biosynthetic gene to study and assess the efficiency of elicitors in triterpene saponin production and metabolic engineering of triterpene saponins.

The Development of Homologous (Canine/Anti-Canine) Antibodies in Dogs with Haemophilia A (Factor VIII Deficiency): A Ten-Year Longitudinal Study

1993 ◽  
Vol 69 (01) ◽  
pp. 021-024 ◽  
Author(s):  
Shawn Tinlin ◽  
Sandra Webster ◽  
Alan R Giles
Keyword(s):  
Factor Viii ◽  
Canine Model ◽  
Significant Inhibition ◽  
Human Condition ◽  
Haemophilia A ◽  
Variable Expression ◽  
The Family ◽  
Over Time

SummaryThe development of inhibitors to factor VIII in patients with haemophilia A remains as a serious complication of replacement therapy. An apparently analogous condition has been described in a canine model of haemophilia A (Giles et al., Blood 1984; 63:451). These animals and their relatives have now been followed for 10 years. The observation that the propensity for inhibitor development was not related to the ancestral factor VIII gene has been confirmed by the demonstration of vertical transmission through three generations of the segment of the family related to a normal (non-carrier) female that was introduced for breeding purposes. Haemophilic animals unrelated to this animal have not developed functionally significant factor VIII inhibitors despite intensive factor VIII replacement. Two animals have shown occasional laboratory evidence of factor VIII inhibition but this has not been translated into clinical significant inhibition in vivo as assessed by clinical response and F.VIII recovery and survival characteristics. Substantial heterogeneity of inhibitor expression both in vitro and in vivo has been observed between animals and in individual animals over time. Spontaneous loss of inhibitors has been observed without any therapies designed to induce tolerance, etc., being instituted. There is also phenotypic evidence of polyclonality of the immune response with variable expression over time in a given animal. These observations may have relevance to the human condition both in determining the pathogenetic factors involved in this condition and in highlighting the heterogeneity of its expression which suggests the need for caution in the interpretation of the outcome of interventions designed to modulate inhibitor activity.

Metal-organic Nanopharmaceuticals

2020 ◽  
Vol 8 (3) ◽  
pp. 163-190
Author(s):  
Benjamin Steinborn ◽  
Ulrich Lächelt
Keyword(s):  
Metal Ions ◽  
Coordination Polymers ◽  
Active Agent ◽  
Lewis Base ◽  
High Loading ◽  
Active Components ◽  
Base Functions ◽  
Metal Organic ◽  
Theranostic Applications ◽  
Pharmacologically Active

: Coordinative interactions between multivalent metal ions and drug derivatives with Lewis base functions give rise to nanoscale coordination polymers (NCPs) as delivery systems. As the pharmacologically active agent constitutes a main building block of the nanomaterial, the resulting drug loadings are typically very high. By additionally selecting metal ions with favorable pharmacological or physicochemical properties, the obtained NCPs are predominantly composed of active components which serve individual purposes, such as pharmacotherapy, photosensitization, multimodal imaging, chemodynamic therapy or radiosensitization. By this approach, the assembly of drug molecules into NCPs modulates pharmacokinetics, combines pharmacological drug action with specific characteristics of metal components and provides a strategy to generate tailorable multifunctional nanoparticles. This article reviews different applications and recent examples of such highly functional nanopharmaceuticals with a high ‘material economy’. : Lay Summary: Nanoparticles, that are small enough to circulate in the bloodstream and can carry cargo molecules, such as drugs, imaging or contrast agents, are attractive materials for pharmaceutical applications. A high loading capacity is a generally aspired parameter of nanopharmaceuticals to minimize patient exposure to unnecessary nanomaterial. Pharmaceutical agents containing Lewis base functions in their molecular structure can directly be assembled into metal-organic nanopharmaceuticals by coordinative interaction with metal ions. Such coordination polymers generally feature extraordinarily high loading capacities and the flexibility to encapsulate different agents for a simultaneous delivery in combination therapy or ‘theranostic’ applications.

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