FURTHER STUDIES WITH THE MITOCHONDRIAL INHIBITOR OF CHOLESTEROL SYNTHESIS

1964 ◽  
Vol 42 (1) ◽  
pp. 105-110 ◽  
Author(s):  
B. B. Migicovsky
Keyword(s):  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Protein Fraction ◽  
Cholesterol Synthesis ◽  
Liver Homogenate ◽  
Liver Mitochondria ◽  
Active Principle ◽  
Mitochondrial Extract ◽  
Mitochondrial Inhibitor

The inhibitory activity of an aqueous extract of liver mitochondria (I.C.S.) was observed with Triton-treated rats. Fractionation of I.C.S. on Sephadex indicated that the active principle comes off the Sephadex with the protein fraction. Inhibitory activity was shown to be present in the 100,000 × g supernate of the liver homogenate of a starved rat, indicating that the active principle moves from the mitochondrion to the surrounding cytoplasm.Electrodialysis of the mitochondrial extract revealed that the inhibitor is permeable and moves to the cathode. The electrodialyzed material was found to be active as an inhibitor of cholesterol synthesis in vitro and in vivo.It is concluded that the active principle is associated with protein and may be separated therefrom by electrodialysis.

IN VIVO INHIBITION OF CHOLESTEROL BIOSYNTHESIS BY A MITOCHONDRIAL EXTRACT

1961 ◽  
Vol 39 (4) ◽  
pp. 747-755 ◽  
Author(s):  
B. B. Migicovsky
Keyword(s):  
Cholesterol Synthesis ◽  
Cholesterol Biosynthesis ◽  
Liver Mitochondria ◽  
Blood Cholesterol ◽  
Active Principle ◽  
Aqueous Extracts ◽  
Inhibitory Substance ◽  
Cholesterol Levels ◽  
Mitochondrial Extract

Aqueous extracts of liver mitochondria were administered to rats by intraperitoneal, subcutaneous, and oral routes, and C14-acetate or mevalonate was injected intraperitoneally 3 hours later. Cholesterol synthesis in vivo from C14-acetate was depressed by the inhibitory substance in the mitochondrial extracts. Synthesis from C14-mevalonate was not inhibited.Active extracts were prepared from livers of rat, rabbit, pig, and sheep. An inhibitory substance is present in blood serum and administration of active mitochondrial extracts depressed blood cholesterol levels. Pending its identification, the active principle has been provisionally termed I.C.S. (inhibitor of cholesterol synthesis).

Agents affecting lipid metabolism. XXXI. Properties of an inhibitor of cholesterol synthesis present in rabbit liver mitochondria

1968 ◽  
Vol 46 (2) ◽  
pp. 179-187 ◽  
Author(s):  
M. N. Cayen ◽  
D. Dvornik
Keyword(s):  
Cholesterol Synthesis ◽  
Liver Mitochondria ◽  
Aqueous Extracts ◽  
Hepatic Cholesterol ◽  
Large Molecules ◽  
Hepatic Cholesterol Synthesis ◽  
Significant Enrichment ◽  
Liver Homogenates ◽  
Mitochondrial Extract

Aqueous extracts of mitochondria from livers of starved animals have been reported to inhibit hepatic cholesterol synthesis. Some properties of a mitochondrial extract prepared from starved rabbits have been studied. The extract depressed the incorporation of both 2-14C-acetate and 3H-mevalonate into cholesterol by rat liver homogenates, giving concentration–dependent responses. The active factor was unstable to heat, but stable under in vitro incubation conditions, to pH changes, and to storage in the dark and cold. It was cationic and associated with one or more large molecules (mol. wt. 50 000–150 000); it was not cleaved by trypsin digestion. Fractionation experiments did not result in any significant enrichment of inhibitory activity.

scholarly journals In Vitro α-Amylase and Protein Glycation Inhibitory Activity of the Aqueous Extract of Flueggea leucopyrus Willd

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Vishmi Sachindra Thrikawala ◽  
Srianthie A. Deraniyagala ◽  
Chamira Dilanka Fernando ◽  
Dinusha Nishani Udukala
Keyword(s):  
Aqueous Extract ◽  
Diabetic Complications ◽  
Inhibitory Activity ◽  
Radical Scavenging ◽  
Vital Role ◽  
Protein Glycation ◽  
Total Phenolic ◽  
Chronic Hyperglycemia ◽  
Body Tissues

There is much interest in plant-based medicine with antidiabetic and antiglycation properties. Chronic hyperglycemia plays a vital role in the development of long-term diabetic complications by inducing protein glycation and the gradual formation of advanced glycation end products (AGEs) in various body tissues. The main objectives of this study were to investigate the aqueous extract of the whole plant of Flueggea leucopyrus Willd (FLAE), a medicinal plant used in traditional medicine in Sri Lanka for its in vitro α-amylase inhibitory activity and its inhibitory potential on the formation of AGEs. α-Amylase inhibitory activity determined by 3,5-dinitrosalicylic acid method revealed that FLAE possesses 29%–91% inhibitory activity at a concentration range of 2.5–400 μg/mL, respectively. Nonenzymatic protein glycation inhibitory capacity assessed by bovine serum albumin-fructose fluorescence spectrometric assay showed that FLAE at 15.6–250.0 μg/mL inhibited AGE formation by 0.9%–98%, respectively. Radical scavenging ability of FLAE using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and total phenolic and flavonoid contents of FLAE were also determined. This study shows that Flueggea leucopyrus Willd not only inhibits α-amylase enzyme, which is known to break starch to glucose, but also inhibits the formation of AGEs, which occur due to chronic hyperglycemia that leads to the onset of diabetic complications.

THEVETIA PERUVIANA ROOTS EXTRACT MEDICATED GOLD NANOPARTICLES AND ITS UREASE INHIBITORY ACTIVITY

2021 ◽  
pp. 79-82
Author(s):  
SAUD BAWAZEER
Keyword(s):  
Gold Nanoparticles ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Enzyme Inhibitor ◽  
Research Work ◽  
Thevetia Peruviana ◽  
Urease Enzyme ◽  
Urease Inhibitory ◽  
Microscopy Techniques

Objective: The main objective of the current research work was synthesized of gold nanoparticles (AuNPs) of Thevetia peruviana aqueous extract,characterization, and screening for urease enzyme inhibitory activity.Methods: AuNPs were synthesized by mixing 1 mM gold salt solution with T. peruviana aqueous extract without any reducing agents. The preparedAuNPs were characterized using UV–visible spectroscopy, Fourier transform infrared spectroscopy, and scanning electron microscopy techniques. Thesynthesized AuNPs were assessed for in vitro urease enzyme inhibitory activity at 0.2 μg in comparison with the aqueous extract.Results: In this finding, we synthesized the AuNPs of T. peruviana aqueous extract for the 1st time. The AuNPs exhibited significant stability atroom temperature. The AuNPs showed significant urease inhibitory activity with IC50 67.56±1.67 at 0.2 μg as compared to aqueous extract whichexhibited good activity with IC50 39.21±1.32 μ at 0.2 mg, against standard thiourea (IC50=21.00±1.16). The formation of AuNPs correlates due to activephytochemical present in extract which is responsible for synthesizing NPs.Conclusion: T. peruviana extract and prepared AuNPs are an outstanding urease enzyme inhibitor and are capable of making fine NPs. Application:The synthesized AuNPs of T. peruviana aqueous extract which significant urease inhibitory activity may allow us to discover NPs for potentiallyeffective and safe nanoherbal therapy.

scholarly journals Antioxidant Properties and Digestive Enzyme Inhibitory Activity of the Aqueous Extract from Leafy Stems of Cissus polyantha

2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Mahamad Abba Talba ◽  
David Miaffo ◽  
Sylviane Laure Poualeu Kamani ◽  
Albert Kamanyi ◽  
Sylvie Léa Wansi
Keyword(s):  
Traditional Medicine ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Antiradical Activity ◽  
Digestive Enzyme ◽  
Antioxidant Properties ◽  
Antioxidant Potential ◽  
Antioxidant Power ◽  
Treatment Of Diabetes

Cissus polyantha (Vitaceae) is a plant used in Cameroonian traditional medicine for the treatment of diabetes. The aims of this study were to evaluate the in vitro antioxidant and antidiabetic activities of the aqueous extract of Cissus polyantha leafy stems. The enzyme inhibitory activity was determined in vitro on α-amylase and α-glucosidase enzymes, followed by confirmative study in vivo on normal rats (oral starch and sucrose tolerance tests at doses of 111, 222, and 444 mg/kg). The ferric reducing antioxidant power and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) antiradical activity of the extract were examined to evaluate the antioxidant potential of the extract. The total content of phenols, flavonoids, and tannins of the extract were also determined. The results showed an inhibitory effect of the extract on the α-amylase and α-glucosidase activities with IC50 values of 216.14 and 182.40 μg/mL, respectively. The extract at doses of 222 and 444 mg/kg induced a significant decrease in postprandial glycaemia during the starch and sucrose tolerance tests. A remarkable antiradical activity of the extract was obtained although lower than that of the standard product. The aqueous extract of leafy stems of Cissus polyantha has an interesting inhibitory activity on the α-amylase and α-glucosidase enzymes, as well as an antioxidant potential, thus validating its use in traditional medicine for the treatment of diabetes mellitus and its complications.

scholarly journals Antibacterial Efficacies of Extracts of Lemon Grass (Cymbopogon citratus) on Some Clinical Microbial Isolates

2021 ◽  
Vol 10 (1) ◽  
Author(s):  
Kamoldeen Ajijolakewu ◽  
Muinat Olanike Kazeem ◽  
Risikat Nike Ahmed ◽  
Rahmat Folashade Zakariyah ◽  
Tariq Oluwakunmi Agbabiaka ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Aqueous Extract ◽  
Ethanolic Extract ◽  
Multidrug Resistant ◽  
Clinical Isolates ◽  
Active Principle ◽  
Cymbopogon Citratus ◽  
Lemon Grass

The spread of new infections and the emergence of multidrug resistant strains of microorganisms necessitate the search for new antimicrobials with focus on plant extracts. In this study, the antimicrobial activity of the extracts (aqueous and ethanolic) of lemon grass known usually for bioactive essential oil (Cymbopogon citratus) was investigated in-vitro, against selected clinical isolates (Staphylococcus aureus, Escherichia coli, Enterococcus faecalis, Pseudomonas aeruginosa and Candida albicans). Antimicrobial efficacy of the extracts was assessed using the agar-well diffusion and broth-dilution techniques. The aqueous extract of C. citratus was more efficacious as it showed higher antimicrobial activity against all the test isolates at all tested concentrations. In contrast, only two of the test isolates; P. aeruginosa and S. aureus were susceptible to the ethanolic extract with minimum inhibitory (MIC) concentrations of 2 mg/ml (against S. aureus) and 12.5 mg/ml (against P. aeruginosa). The MIC of the aqueous extract were (mg/ml): 2, 6.25, 12.5, 25 and 50 against S. aureus, E. faecalis, P. aeruginosa, E. coli and C. albicans respectively. Meanwhile, both the aqueous and ethanolic extracts of C. citratus exerted only a bacteriostatic effect against the five test isolates at all concentrations. Quantitative phytochemical screening of the two extracts revealed the presence of more concentration of active compounds in the aqueous extract than the ethanolic extract which plausibly accounts for its greater antimicrobial activity. This study has shown that, in difference to the use of its conventional essential oil, solvent extraction of Cymbopogon citratus is also a potent source of efficacious antimicrobials. Further works to determine the respective mechanisms of action(s) of the extracts’ active principle is being projected. Keywords: Lemon grass, clinical isolates, antimicrobial efficacies, bioactive compounds

EFFECT OF STARVATION ON CHOLESTEROL BIOSYNTHESIS IN VITRO

1955 ◽  
Vol 33 (1) ◽  
pp. 858-866 ◽  
Author(s):  
B. B. Migicovsky ◽  
J. D. Wood
Keyword(s):  
Particulate Matter ◽  
Cholesterol Synthesis ◽  
Cholesterol Biosynthesis ◽  
Liver Homogenate ◽  
Normal Liver ◽  
Synthetic Activity ◽  
Liver Homogenates

The components of centrifugal fractionation of liver homogenates from normal and starved rats were examined for cholesterol synthesis and inhibition thereof. Normal liver particulate matter fractions obtained between 700 to 9000 × g and 9000 to 140,000 × g were active with respect to cholesterol synthesis in the presence of clear supernate obtained by centrifugation at 140,000 × g. The particles alone did not synthesize cholesterol. Particles from liver homogenate of starved rats, recombined with clear supernate from starved rats, lacked synthetic activity but clear supernate from liver homogenate of starved rats showed some activity in the presence of normal particles. Degradation of cholesterol occurred with liver particles (700–9000 × g) from both normal and starved rats: the latter preparation also inhibited cholesterol synthesis. Preliminary incubation of clear supernate from normal rats with particles from starved rats, followed by recentrifugation at 140,000 × g, produced a supernate with synthetic activity equal to that obtained with untreated supernate. Preliminary incubation with normal particles gave a supernate with less synthetic activity. This indicated another difference between particulate matter from normal and starved rats.

Agents affecting lipid metabolism. XXXII. Effect of a liver mitochondrial extract on cholesterol synthesis in the rat

1968 ◽  
Vol 46 (2) ◽  
pp. 189-191
Author(s):  
M. N. Cayen ◽  
P. Hill ◽  
D. Dvornik
Keyword(s):  
Body Weight ◽  
Lipid Metabolism ◽  
Crude Extract ◽  
Cholesterol Synthesis ◽  
Liver Mitochondria ◽  
Liver Cholesterol ◽  
Acetate Incorporation ◽  
Hepatic Cholesterol ◽  
Experimental Conditions ◽  
Mitochondrial Extract

A lyophilized extract was prepared from liver mitochondria of rabbits starved for 24 h. Rats were fed single oral (1–4 g/kg body weight) and intraperitoneal (1.5 g/kg) doses of the crude extract. After 3 h, the livers of one group were removed and 2-14C-acetate incorporation into cholesterol was measured. In the second group, rats received an interperitoneal dose of 2-14C-acetate 1 h after administration of the mitochondrial extract; animals were sacrificed 2 h later and the incorporation into hepatic cholesterol was measured. Under these experimental conditions, administration of the mitochondrial extract did not decrease the incorporation of 2-14C-acetate into liver cholesterol.

scholarly journals Sambiloto (Andrographis paniculata Nees.) leaf extract activity as an α-Amylase enzyme inhibitor

2021 ◽  
pp. 305-308
Author(s):  
Yustina Sri Hartini ◽  
Dewi Setyaningsih ◽  
Maria Josephine Vivian Chang ◽  
Maria Cyrilla Iglesia Adi Nugrahanti
Keyword(s):  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Enzyme Inhibitor ◽  
Statistical Tests ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Andrographis Paniculata ◽  
Activity Test ◽  
Ic50 Value

Introduction: Sambiloto (Andrographis paniculata) is an antidiabetic medicinal plant that acts by inhibiting the α-amylase enzyme. Andrographolide, the active compound of sambiloto leaf, is insoluble in water but dissolves in ethanol. Aim: This study compared the in vitro activity of aqueous extract and ethanolic extract of sambiloto leaf with the α-amylase enzyme. Methods: The inhibitory activity test of the α-amylase enzyme was carried out using the ultraviolet-visible spectrophotometric method by measuring the absorbance of the remaining starch, which forms a blue complex with iodine-iodide. Results: The inhibitory activity of the α-amylase enzyme of the aqueous extract of sambiloto leaf (with the IC50 value of 14.203 ± 0.112 mg/mL) was lower than that of the ethanol extract (with the IC50 value of 9.253 ± 0.116 mg/mL). The results of the statistical tests showed significant differences (p <0.05) between the inhibitory activity of the α-amylase enzyme acarbose and the activity of both extracts.

INHIBITION OF CHOLESTEROL BIOSYNTHESIS BY A MITOCHONDRIAL EXTRACT

1960 ◽  
Vol 38 (4) ◽  
pp. 339-346 ◽  
Author(s):  
B. B. Migicovsky
Keyword(s):  
Cholesterol Synthesis ◽  
Cholesterol Biosynthesis ◽  
Inhibitory Effect ◽  
Homeostatic Mechanism ◽  
Heat Labile ◽  
Mitochondrial Extract

Cholesterol biosynthesis was effectively inhibited by an extract of mitochondria disrupted with sonic oscillations. The inhibitory effect occurred both in vivo and in vitro. The inhibitor substance was heat-labile, and could be prepared from mitochondria from livers of normal or starved rats. The inhibition appeared to be of the competitive type. The locus of the inhibition in the chain of reactions from acetate to cholesterol appeared to be between acetoacetate and mevalonate. It is suggested that the inhibitor substance present in the mitochondrion represents, in part, the homeostatic mechanism that controls cholesterol synthesis by the liver.

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