scholarly journals CHOLESTEROL LOWERING EFFECT OF CHITOSAN NANOPARTICLES USING PARIJOTO FRUITS EXTRACT

2020 ◽  
Vol 17 (2) ◽  
pp. 102-111
Author(s):  
Fania Putri Luhurningtyas ◽  
Rissa Laila Vifta ◽  
Nur Syarohmawati ◽  
Mahardika Adhi Candra
Keyword(s):  
Functional Group ◽  
Chitosan Nanoparticles ◽  
Volume Ratio ◽  
Potential Candidate ◽  
Cholesterol Lowering ◽  
Uniform Particles ◽  
Cholesterol Levels ◽  
Nanoparticle System ◽  
Average Size ◽  
Cholesterol Testing

Parijoto (Medinilla speciosa Reinw. ex Blum) fruit is known to have pharmacological activity as cholesterol lowering levels. Its activity needs to be increased with nanoparticle system so that the active substance can bind 100% to the action target. This study aims to determine the formation of nanoparticles from parijoto fruit (NEBP) and activity test as a decrease in cholesterol levels. The formation of nanoparticles used variations of concentration and volume of chitosan and NaTPP. Anti-cholesterol testing is based on the amount of free cholesterol in the sample that reacted with Lieberman-Burchard into complex green compounds. The best formation of NEBP was 0.2% chitosan, 0.1% NaTPP and volume ratio 5:1. The particle size showed an average size of 269.3 nm (10-1000 nm). The result of the percent transmittance and polydispersity index were 99,379 (close to 100%) and 0.378 (PDI <0.5). The functional group-specific of NEBP was –OH, N-H, PO3. The morphology was round and non-uniform particles. NEBP can decrease 50% cholesterol levels with a smaller EC50 value was 89.08 compared to the extract (EC50 259.98 ppm). Nanoparticles of parijoto fruit is a potential candidate for anti-cholesterol drug.

Quality-by-Design Enabled Chitosan Nanoparticles for Antitubercular Therapy: Formulation, Statistical Optimization, and In vitro Characterization

2020 ◽  
Vol 15 ◽  
Author(s):  
Manasi M. Chogale ◽  
Sujay S. Gaikwad ◽  
Savita P. Kulkarni ◽  
Vandana B. Patravale
Keyword(s):  
Side Effects ◽  
Treatment Regimen ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Antitubercular Therapy ◽  
Prolonged Treatment ◽  
High Dose ◽  
Average Size

Background: Tuberculosis (TB) continues to be among the leading causes for high mortality among developing countries. Though a seemingly effective treatment regimen against TB is in place, there has been no significant improvement in the therapeutic rates. This is primarily owing to the high drug doses, their associated sideeffects, and prolonged treatment regimen. Discontinuation of therapy due to the severe side effects of the drugs results in the progression of the infection to the more severe drug-resistant TB. Objectives: Reformulation of the current existing anti TB drugs into more efficient dosage forms could be an ideal way out. Nanoformulations have been known to mitigate the side effects of toxic, high-dose drugs. Hence, the current research work involves the formulation of Isoniazid (INH; a first-line anti TB molecule) loaded chitosan nanoparticles for pulmonary administration. Methods: INH loaded chitosan nanoparticles were prepared by ionic gelation method using an anionic crosslinker. Drugexcipient compatibility was evaluated using DSC and FT-IR. The formulation was optimized on the principles of Qualityby-Design using a full factorial design. Results: The obtained nanoparticles were spherical in shape having an average size of 620±10.97 nm and zeta potential +16.87±0.79 mV. Solid state characterization revealed partial encapsulation and amorphization of INH into the nanoparticulate system. In vitro release study confirmed an extended release of INH from the system. In vitro cell line based safety and efficacy studies revealed satisfactory results. Conclusion: The developed nanosystem is thus an efficient approach for antitubercular therapy.

Targeting the Cholesterol Paradigm in the Risk Reduction for Atherosclerotic Cardiovascular Disease: Does the Mechanism of Action of Pharmacotherapy Matter for Clinical Outcomes?

2021 ◽  
pp. 107424842110236
Author(s):  
Ruihai Zhou ◽  
George A. Stouffer ◽  
Sidney C. Smith
Keyword(s):  
Cardiovascular Disease ◽  
Clinical Outcomes ◽  
Mechanism Of Action ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Blood Cholesterol ◽  
Atherosclerotic Cardiovascular Disease ◽  
Pcsk9 Inhibitors ◽  
Cholesterol Lowering ◽  
Cholesterol Levels

Hypercholesterolemia is a well-established risk factor for atherosclerotic cardiovascular disease (ASCVD). Low-density lipoprotein cholesterol (LDL-C) has been labeled as “bad” cholesterol and high-density lipoprotein cholesterol (HDL-C) as “good” cholesterol. The prevailing hypothesis is that lowering blood cholesterol levels, especially LDL-C, reduces vascular deposition and retention of cholesterol or apolipoprotein B (apoB)-containing lipoproteins which are atherogenic. We review herein the clinical trial data on different pharmacological approaches to lowering blood cholesterol and propose that the mechanism of action of cholesterol lowering, as well as the amplitude of cholesterol reduction, are critically important in leading to improved clinical outcomes in ASCVD. The effects of bile acid sequestrants, fibrates, niacin, cholesteryl ester transfer protein (CETP) inhibitors, apolipoprotein A-I and HDL mimetics, apoB regulators, acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitors, cholesterol absorption inhibitors, statins, and proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors, among other strategies are reviewed. Clinical evidence supports that different classes of cholesterol lowering or lipoprotein regulating approaches yielded variable effects on ASCVD outcomes, especially in cardiovascular and all-cause mortality. Statins are the most widely used cholesterol lowering agents and have the best proven cardiovascular event and survival benefits. Manipulating cholesterol levels by specific targeting of apoproteins or lipoproteins has not yielded clinical benefit. Understanding why lowering LDL-C by different approaches varies in clinical outcomes of ASCVD, especially in survival benefit, may shed further light on our evolving understanding of how cholesterol and its carrier lipoproteins are involved in ASCVD and aid in developing effective pharmacological strategies to improve the clinical outcomes of ASCVD.

Increased Superoxide Anion Production by Platelets in Hypercholesterolemic Patients

2002 ◽  
Vol 87 (05) ◽  
pp. 796-801 ◽  
Author(s):  
Valerio Sanguigni ◽  
Pasquale Pignatelli ◽  
Daniela Caccese ◽  
Fabio Pulcinelli ◽  
Luisa Lenti ◽  
...  
Keyword(s):  
Superoxide Anion ◽  
Ldl Cholesterol ◽  
Experimental Studies ◽  
Human Platelets ◽  
Superoxide Anion Production ◽  
Cholesterol Lowering ◽  
Platelet Production ◽  
Cholesterol Levels ◽  
Anion Production ◽  
O2 Production

SummaryThe purpose of this study was to investigate the relationship between hypercholesterolemia and superoxide anion production.Experimental studies demonstrated that hypercholesterolemia is associated with enhanced cellular superoxide anion (O2 −) production. Aim of the study was to assess whether the same phenomenon occurs in humans.Lipid profile and platelet O2 − production were measured in 28 patients with hypercholesterolemia, compared with 25 age- and sexmatched healthy subjects, and in 21 out of the 28 patients after 8-week treatment with 10 mg/day atorvastatin (a HMGCoA reductase inhibitor). In order to assess the mechanism by which LDL cholesterol interferes with platelet production of O2 −, human platelets were incubated with LDL cholesterol in the presence of either an inhibitor of the phospholipaseA2 enzyme, AACOCF3, or an inhibitor of NADH/NADPH oxidases, DPI.O2 − platelet generation was significantly higher (p <0.001) and significantly related to LDL cholesterol (p < 0.001 ) in patients as compared to controls. 8-week treatment with 10 mg/day atorvastatin significantly reduced both LDL cholesterol and O2 − platelet production. This effect was partially related to the cholesterol-lowering, in that three days of treatment with atorvastatin significantly decreased platelet O2 − production, while no significant change in LDL-cholesterol levels was observed. Platelets incubated with LDL cholesterol showed O2 − release by atorvastatin is partially related to cholesterol lowering effect, suggesting that other mechanisms could be responsible for the antioxidant activity of the drug.

Cholesterol, Cholesterol-Lowering Medication Use, and Breast Cancer Outcome in the BIG 1-98 Study

2017 ◽  
Vol 35 (11) ◽  
pp. 1179-1188 ◽  
Author(s):  
Signe Borgquist ◽  
Anita Giobbie-Hurder ◽  
Thomas P. Ahern ◽  
Judy E. Garber ◽  
Marco Colleoni ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Endocrine Therapy ◽  
Early Stage ◽  
Cancer Recurrence ◽  
Disease Free Survival ◽  
Distant Recurrence ◽  
Cholesterol Lowering ◽  
Hormone Receptor Positive ◽  
Cholesterol Levels ◽  
Free Interval

Purpose Cholesterol-lowering medication (CLM) has been reported to have a role in preventing breast cancer recurrence. CLM may attenuate signaling through the estrogen receptor by reducing levels of the estrogenic cholesterol metabolite 27-hydroxycholesterol. The impact of endocrine treatment on cholesterol levels and hypercholesterolemia per se may counteract the intended effect of aromatase inhibitors. Patients and Methods The Breast International Group (BIG) conducted a randomized, phase III, double-blind trial, BIG 1-98, which enrolled 8,010 postmenopausal women with early-stage, hormone receptor–positive invasive breast cancer from 1998 to 2003. Systemic levels of total cholesterol and use of CLM were measured at study entry and every 6 months up to 5.5 years. Cumulative incidence functions were used to describe the initiation of CLM in the presence of competing risks. Marginal structural Cox proportional hazards modeling investigated the relationships between initiation of CLM during endocrine therapy and outcome. Three time-to-event end points were considered: disease-free-survival, breast cancer–free interval, and distant recurrence–free interval. Results Cholesterol levels were reduced during tamoxifen therapy. Of 789 patients who initiated CLM during endocrine therapy, the majority came from the letrozole monotherapy arm (n = 318), followed by sequential tamoxifen-letrozole (n = 189), letrozole-tamoxifen (n = 176), and tamoxifen monotherapy (n = 106). Initiation of CLM during endocrine therapy was related to improved disease-free-survival (hazard ratio [HR], 0.79; 95% CI, 0.66 to 0.95; P = .01), breast cancer–free interval (HR, 0.76; 95% CI, 0.60 to 0.97; P = .02), and distant recurrence–free interval (HR, 0.74; 95% CI, 0.56 to 0.97; P = .03). Conclusion Cholesterol-lowering medication during adjuvant endocrine therapy may have a role in preventing breast cancer recurrence in hormone receptor–positive early-stage breast cancer. We recommend that these observational results be addressed in prospective randomized trials.

scholarly journals Community based cholesterol testing has a favorable effect short term follow up cholesterol levels

1990 ◽  
Vol 15 (2) ◽  
pp. A184
Author(s):  
Thomas C. Hilton ◽  
Carolyn Burt ◽  
Stephen C. Smith ◽  
Harold L. Kennedy
Keyword(s):  
Favorable Effect ◽  
Short Term ◽  
Community Based ◽  
Cholesterol Levels ◽  
Cholesterol Testing

Are recent statin recommendations to employ fixed doses and abandon targets effective for treatment of hypercholesterolaemia? Investigation based on number needed to treat

2016 ◽  
Vol 24 (1) ◽  
pp. 76-83 ◽  
Author(s):  
Handrean Soran ◽  
Safwaan Adam ◽  
Paul N Durrington
Keyword(s):  
Secondary Prevention ◽  
Moderate Intensity ◽  
Fixed Dose ◽  
Dose Titration ◽  
Number Needed To Treat ◽  
Atherosclerotic Cardiovascular Disease ◽  
Cvd Risk ◽  
Cholesterol Lowering ◽  
Cholesterol Levels ◽  
Lowering Therapy

Background Assessed by number needed to treat (NNT) to prevent one event, it was previously shown that for those at similar atherosclerotic cardiovascular disease (CVD) risk, the benefit accruing from treating people with higher cholesterol levels with statins is greater than for those with lower levels. Method By estimating NNT from both the absolute atherosclerotic cardiovascular risk and the pre-treatment low density lipoprotein cholesterol (LDL-C) concentration, recent recommendations for fixed dose high and moderate intensity statin treatment in the primary and secondary prevention of CVD were compared with cholesterol-lowering therapy aimed at a target LDL-C. Results We report that the USA and UK recommendations to employ a fixed dose of atorvastatin 20 mg daily for primary prevention will produce good results in people with low cholesterol levels, but are a disadvantage for those with higher levels who benefit more from a therapeutic target and statin dose titration and, where necessary, adjunctive cholesterol-lowering therapy to achieve this target. The higher dose of atorvastatin 80 mg daily with no target recommended for secondary prevention is generally more effective than aiming for a LDL-C goal except in people with particularly high cholesterol. Conclusion For optimum clinical effectiveness, initial LDL-C concentration must be considered in deciding whether a target will allow a greater decrease in LDL-C and thus a lower NNT than a fixed dose regimen. Individual variation in the LDL-C response to statins also makes post-treatment cholesterol measurement essential.

THE ANATOMY AND FUNCTION OF A SEGMENT OF THE X CHROMOSOME OF DROSOPHILA MELANOGASTER

Genetics ◽  
1972 ◽  
Vol 71 (1) ◽  
pp. 139-156
Author(s):  
B H Judd ◽  
M W Shen ◽  
T C Kaufman
Keyword(s):  
Drosophila Melanogaster ◽  
X Chromosome ◽  
Functional Group ◽  
Deletion Mapping ◽  
Mutant Type ◽  
Functional Units ◽  
Average Size ◽  
And Function

ABSTRACT An average size chromomere of the polytene X chromosome of Drosophila melanogaster contains enough DNA in each haploid equivalent strand to code for 30 genes, each 1,000 nucleotides long. We have attempted to learn about the organization of chromosomes by asking how many functional units can be localized within a chromomere. This was done by 1) recovery of mutants representative of every cistron in the 3A2-3C2 region; 2) the characterization of the function of each mutant type and grouping by complementation tests; 3) the determination of the genetic and cytological position of each cistron by recombination and deletion mapping. The data clearly show one functional group per chromomere. It is postulated that a chromomere is one cistron within which much of the DNA is regulatory in function.

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