In Vitro Effect of Cryptophycin 52 on Microtubule Assembly and Tubulin: Molecular Modeling of the Mechanism of Action of a New Antimitotic Drug†

Biochemistry ◽  
2001 ◽  
Vol 40 (45) ◽  
pp. 13510-13519 ◽  
Author(s):  
P. Barbier ◽  
C. Gregoire ◽  
F. Devred ◽  
M. Sarrazin ◽  
V. Peyrot
Keyword(s):  
Molecular Modeling ◽  
Mechanism Of Action ◽  
Microtubule Assembly ◽  
Antimitotic Drug ◽  
Cryptophycin 52 ◽  
Vitro Effect

scholarly journals Novel Therapeutic Approach for the Management of Mood Disorders: In Vivo and In Vitro Effect of a Combination of L-Theanine, Melissa officinalis L. and Magnolia officinalis Rehder & E.H. Wilson

Nutrients ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 1803 ◽  
Author(s):  
Vittoria Borgonetti ◽  
Paolo Governa ◽  
Marco Biagi ◽  
Nicoletta Galeotti
Keyword(s):  
Mood Disorders ◽  
Mechanism Of Action ◽  
Neuroprotective Effect ◽  
Endocannabinoid System ◽  
Antidepressant Activity ◽  
Melissa Officinalis ◽  
Magnolia Officinalis ◽  
Vitro Effect

Mood disorders represent one of the most prevalent and costly psychiatric diseases worldwide. The current therapies are generally characterized by several well-known side effects which limit their prolonged use. The use of herbal medicine for the management of several psychiatric conditions is becoming more established, as it is considered a safer support to conventional pharmacotherapy. The aim of this study was to investigate the possible anxiolytic and antidepressant activity of a fixed combination of L-theanine, Magnolia officinalis, and Melissa officinalis (TMM) in an attempt to evaluate how the multiple modulations of different physiological systems may contribute to reducing mood disorders. TMM showed an anxiolytic-like and antidepressant-like activity in vivo, which was related to a neuroprotective effect in an in vitro model of excitotoxicity. The effect of TMM was not altered by the presence of flumazenil, thus suggesting a non-benzodiazepine-like mechanism of action. On the contrary, a significant reduction in the effect was observed in animals and neuronal cells co-treated with AM251, a cannabinoid receptor type 1 (CB1) antagonist, suggesting that the endocannabinoid system may be involved in the TMM mechanism of action. In conclusion, TMM may represent a useful and safe candidate for the management of mood disorders with an innovative mechanism of action, particularly as an adjuvant to conventional therapies.

scholarly journals Synthesis, Molecular Docking and Antiplasmodial Activities of New Tetrahydro-β-Carbolines

2021 ◽  
Vol 22 (24) ◽  
pp. 13569
Author(s):  
Anna Jaromin ◽  
Beata Gryzło ◽  
Marek Jamrozik ◽  
Silvia Parapini ◽  
Nicoletta Basilico ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Molecular Modeling ◽  
Mechanism Of Action ◽  
Blood Cells ◽  
Antiplasmodial Activity ◽  
Drug Resistant ◽  
Human Red Blood Cells ◽  
Molecular Modeling Studies

Malaria is still one of the most dangerous infectious diseases and the emergence of drug resistant parasites only worsens the situation. A series of new tetrahydro-β-carbolines were designed, synthesized by the Pictet–Spengler reaction, and characterized. Further, the compounds were screened for their in vitro antiplasmodial activity against chloroquine-sensitive (D10) and chloroquine-resistant (W2) strains of Plasmodium falciparum. Moreover, molecular modeling studies were performed to assess the potential action of the designed molecules and toxicity assays were conducted on the human microvascular endothelial (HMEC-1) cell line and human red blood cells. Our studies identified N-(3,3-dimethylbutyl)-1-octyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b] indole-3-carboxamide (7) (a mixture of diastereomers) as the most promising compound endowed with the highest antiplasmodial activity, highest selectivity, and lack of cytotoxicity. In silico simulations carried out for (1S,3R)-7 provided useful insights into its possible interactions with enzymes essential for parasite metabolism. Further studies are underway to develop the optimal nanosized lipid-based delivery system for this compound and to determine its precise mechanism of action.

THE IN VITRO EFFECT OF PROGESTERONE AND OESTROGENS ON THE SPONTANEOUS AND OXYTOCIN-INDUCED ACTIVITY OF THE HUMAN MYOMETRIUM

1974 ◽  
Vol 76 (1) ◽  
pp. 172-177 ◽  
Author(s):  
L. Barnafi ◽  
R. Larraguibel
Keyword(s):  
Mechanism Of Action ◽  
Inhibitory Effect ◽  
Human Myometrium ◽  
Vitro Effect ◽  
Dose Dependent

ABSTRACT The in vitro effect of progesterone and oestrogens on the spontaneous and oxytocin-induced activity of the pregnant and non-pregnant human myometrium was studied. Oestrogens as well as progesterone blocked the spontaneous and oxytocininduced contractions 10–20 min after the steroids were added to the bath. The inhibitory effect was dose-dependent and reversible. Oestradiol-17β and diethylstilboestrol were approximately 10 times more active than progesterone. The possible mechanism of action of oestrogens and progesterone are discussed.

Effects “in Vitro” of Some Cardiovascular Drugs and Other Agents on Human Platelet Aggregation

1973 ◽  
Vol 29 (01) ◽  
pp. 190-195 ◽  
Author(s):  
G Sacchetti ◽  
D Bellani ◽  
C Montanari ◽  
A Gibelli
Keyword(s):  
Platelet Aggregation ◽  
Mechanism Of Action ◽  
Human Platelet ◽  
Cardiovascular Drugs ◽  
Blocking Drug ◽  
Human Platelet Aggregation ◽  
Vitro Effect ◽  
Induced Aggregation

SummaryThe in vitro effect of the following substances on human platelet aggregation is studied: K 4423 (a ß-blocking drug), isoproterenol, phentolamine, papaverine, methamidoline (a myolytic agent).None of these substances causes aggregation. All inhibit aggregation induced by ADP or noradrenaline, except for phentolamine, which is active only on noradrenaline- induced aggregation.Hypothesis on the mechanism of action of the compounds tested are proposed.

Multi-mode light microscopy of microtubule assembly dynamics and chromosome movement in vivo and In vitro

1996 ◽  
Vol 54 ◽  
pp. 730-731
Author(s):  
E. D. Salmon ◽  
J. C. Waters ◽  
C. Waterman-Storer
Keyword(s):  
Imaging System ◽  
Ccd Camera ◽  
Transmitted Light ◽  
Microtubule Assembly ◽  
Live Cells ◽  
Optical Efficiency ◽  
Multiple Band ◽  
Multi Mode

We have developed a multi-mode digital imaging system which acquires images with a cooled CCD camera (Figure 1). A multiple band pass dichromatic mirror and robotically controlled filter wheels provide wavelength selection for epi-fluorescence. Shutters select illumination either by epi-fluorescence or by transmitted light for phase contrast or DIC. Many of our experiments involve investigations of spindle assembly dynamics and chromosome movements in live cells or unfixed reconstituted preparations in vitro in which photodamage and phototoxicity are major concerns. As a consequence, a major factor in the design was optical efficiency: achieving the highest image quality with the least number of illumination photons. This principle applies to both epi-fluorescence and transmitted light imaging modes. In living cells and extracts, microtubules are visualized using X-rhodamine labeled tubulin. Photoactivation of C2CF-fluorescein labeled tubulin is used to locally mark microtubules in studies of microtubule dynamics and translocation. Chromosomes are labeled with DAPI or Hoechst DNA intercalating dyes.

In vitro effect of an aqueous extract of Artocarpus lakoocha on the intestinal parasites in cattle

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
N Saowakon ◽  
P Chaichanasak ◽  
C Wanichanon ◽  
V Reutrakul ◽  
P Sobhon
Keyword(s):  
Aqueous Extract ◽  
Intestinal Parasites ◽  
Vitro Effect

In vitro effect of purified plumbagin of Plumbago indica against motility of Paramphistomum cervi

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
N Saowakon ◽  
P Kueakhai ◽  
N Changklungmoa ◽  
N Lorsuwannarat ◽  
P Sobhon
Keyword(s):  
Plumbago Indica ◽  
Vitro Effect ◽  
Paramphistomum Cervi

In vitro effect on myometrial contractility by a combination of Bryophyllum pinnatum juice and atosiban

2017 ◽  
Author(s):  
S Santos ◽  
C Haslinger ◽  
M Hamburger ◽  
M Mennet ◽  
O Potterat ◽  
...  
Keyword(s):  
Myometrial Contractility ◽  
Vitro Effect ◽  
Bryophyllum Pinnatum
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