INTERACTION OF THROMBOLYTIC PROTEINASES COMPLEX LONGOLITIN AND ITS PRODUCER — MYCELIAL FUNGUS ARTHROBOTRYS LONGA — WITH ANTITHROMBOTIC DRUG PIYAVIT

2018 ◽  
Author(s):  
Т.С. Шаркова ◽  
И.Б. Павлова ◽  
Л.В. Подорольская
Keyword(s):  
Proteolytic Enzymes ◽  
In Vitro Study ◽  
Culture Liquid ◽  
Mycelial Fungus ◽  
Antithrombotic Agents ◽  
Antithrombotic Drug ◽  
Combined Application ◽  
Anamorphic Fungus ◽  
Intact Rats

Цель исследования: изучение взаимодействия комплекса протеолитических ферментов препарата лонголитин из анаморфного гриба Arthrobotrys longa с антикоагулянтным и антитромботическим препаратом пиявитом. Материалы и методы. Препарат пиявит смешивали в разных разведениях с различными концентрациями лонголитина и определяли фибринолитическую активность (ФА) смеси. В другой серии опытов пиявит добавляли в погруженную культуру гриба-продуцента. По окончании эксперимента в пробах культуральной жидкости (КЖ) определяли ФА. Антикоагулянтные свойства КЖ измеряли методом рекальцификации и записи тромбоэластограммы при добавлении КЖ к плазме крови здоровых интактных крыс. Результаты. В опытах in vitro пиявит дозозависимо угнетал ФА лонголитина до полного ее подавления при концентрации 16 мг/мл. Добавление пиявита к культуре гриба-продуцента вызывало усиление биосинтеза препарата с увеличением ФА. КЖ при этом обладала высокой антикоагулянтной активностью. Время рекальцификации и показатель R тромбоэластограммы в КЖ были статистически достоверно удлинены, увеличивалась и антиполимеризационная активность КЖ. Заключение. Совместное применение двух антитромботических средства (лонголитина и пиявита) в исследовании in vitro привело к уменьшению фибринолитических, а значит, и тромболитических свойств лонголитина. Таким образом, одновременное использование этих препаратов требует осторожности. Aim: to study the interaction of Longolitin (complex of proteolytic enzymes from anamorphic fungus Arthrobotrys longa) with anticoagulative and antithrombotic drug Piyavit. Materials and methods. We mixed diff erent dilutions of Piyavit with various concentrations of Longolitin and determined fibrinolytic activity (FA) of the mixture. In other experimental series we added Piyavit to submerged culture of the fungus-producer. At the end of the experiment we determined FA in culture liquid samples (CL). Anticoagulative properties of CL were measured by recalcification method and thromboelastograms recording with CL addition to blood plasma of healthy intact rats. Results. In in vitro experiments Piyavit dose-dependently inhibited FA of Longolitin until it’s completely suppression at concentration of 16 mg/ml. Piyavit addition to the culture of fungus-producer caused the enhancement of drug biosynthesis with FA increasing. At the same time CL had a high anticoagulative activity. Recalcifi cation time and parameter R of thromboelastogram in CL were statistically signifi cant elongated, also CL anti-polymerization activity increased. Conclusion. Combined application of two antithrombotic agents (Longolitin and Piyavit) in in vitro study led to decreasing of fibrinolytic, and so thrombolytic properties of Longolitine. Thus, the simultaneous use of these drugs requires caution. Adding piyavit to the culture of the producer fungus led to an increase in the biosynthesis of the preparation. Thus, caution is needed at simultaneous using of these drugs.

SUSCEPTIBILITY OF PROTEINS USED IN CALF MILK REPLACERS TO HYDROLYSIS BY VARIOUS PROTEOLYTIC ENZYMES

1980 ◽  
Vol 60 (4) ◽  
pp. 907-914 ◽  
Author(s):  
K. J. JENKINS ◽  
S. MAHADEVAN ◽  
D. B. EMMONS
Keyword(s):  
Trichloroacetic Acid ◽  
Proteolytic Enzymes ◽  
Milk Proteins ◽  
In Vitro Study ◽  
Enzyme Treatment ◽  
Protein Hydrolysis ◽  
Protein Substrates ◽  
Optimum Ph ◽  
Milk Replacers

An in vitro study was conducted to assess the hydrolytic susceptibility of various milk and non-milk proteins (soybean, rapeseed, fish) used in calf milk replacers to endogenous and commercial proteolytic enzymes. Extent of protein hydrolysis (%) was calculated from the reduced amount of protein precipitated by 10% trichloroacetic acid following enzyme treatment. All of the enzymes tested hydrolyzed the milk proteins more extensively than the non-milk proteins both at their optimum pH, and at the pH (6.1) of calf abomasal contents immediately after feeding. At both optimum pH and pH 6.1, the highest average hydrolysis value for all protein substrates was obtained with pronase followed by papain, trypsin, pancreatin, chymotrypsin, Mucor miehei rennet andchymosin (calf rennet). All substrates were hydrolyzed extensively by pepsin at pH 2.0 but, as expected, very little hydrolysis occurred with this enzyme atpH6.1.

scholarly journals In Vitro Study of Combined Application of Bevacizumab and 5-Fluorouracil or Bevacizumab and Mitomycin C to Inhibit Scar Formation in Glaucoma Filtration Surgery

2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Yuanyuan Zhang ◽  
Shaopin Zhu ◽  
Xun Xu ◽  
Lei Zuo
Keyword(s):  
Mitomycin C ◽  
In Vitro Study ◽  
Drug Combinations ◽  
Vitro Study ◽  
Type I ◽  
Subconjunctival Injection ◽  
Filtration Surgery ◽  
Glaucoma Filtration Surgery ◽  
Combined Application

This is an in vitro study conducted to observe the safety and antiscarring effects of combined application of bevacizumab (BVZ) and 5-fluorouracil (5-Fu) or BVZ and mitomycin C (MMC) during glaucoma filtration surgery (GFS). The cytotoxicity of drug combinations in human Tenon’s fibroblasts (HTFs) and human umbilical vein endothelial cells (HUVECs) was evaluated. Their effects on the levels of vascular endothelial growth factor (VEGF) in HUVECs, cell proliferation and migration in HTFs, and the expression of collagen type I alpha 1 (Col1A1) gene in HTFs were evaluated. In addition, the effects of combined drugs on VEGF(R) mRNA in HTFs were detected to explore the possible underlying drug mechanisms. The results showed that BVZ combined with 5-Fu demonstrated more significant antiscarring effects than BVZ or 5-Fu alone. However, the inhibitory effects of BVZ combined with MMC were similar to those of MMC alone. The cytotoxicity of the drug combinations was significantly greater than that of single drug, suggesting that combined application of BVZ and antimetabolites after GFS was safer when applied at different sites (such as subconjunctival injection at bilateral sides of the filtering bleb) or at varied time points.

Effect of 1-Methyl-2-Mercapto-5-(3-Pyridyl)-Imidazole (KC-6141) on Rabbit Platelet Aggregation in Vitro and Rat Platelet Retention

1978 ◽  
Vol 39 (01) ◽  
pp. 167-176 ◽  
Author(s):  
Teruhiko Umetsu ◽  
Tadakatsu Kato
Keyword(s):  
Arachidonic Acid ◽  
Platelet Aggregation ◽  
Response Curve ◽  
In Vitro Study ◽  
Rabbit Platelet ◽  
Antithrombotic Drug ◽  
Method Effects ◽  
Induced Aggregation ◽  
Retention Study

SummaryEffect of l-methyl-2-mercapto-5-(3-pyridyl)-imidazole (KC-6141) on rabbit platelet aggregation in vitro and rat platelet retention were investigated.In the in vitro study, KC-6141 inhibited ADP-induced aggregation by 27% at 5× 10−4M, being more active than dipyridamole but much less than adenosine. Inhibition of arachidonic acid-and collagen-induced aggregation by KC-6141 was more effective than that of ADP-induced one and its ED50 was 2.1×10−5 and 8×10−5M, respectively. KC-6141 was 10 and 4 times more potent than aspirin in arachidonic acid-and collagen-induced aggregation, respectively. The dose-response curve of KC-6141 was parallel to that of aspirin, suggesting it is an aspirin-like compound.In the platelet retention study, a method for determining platelet retention in rats was devised so that platelet retention can be measured with a volume of blood as small as possible. By use of the method, effects of KC-6141, aspirin and dipyridamole were compared. When administered intraperitoneally at 100 mg/kg, KC-6141 indicated 54.8% inhibition of platelet retention, whereas aspirin and dipyridamole showed only 23.5 and 5.2% inhibition, respectively. On the oral administration at 200 mg/kg, KC-6141 inhibited by 60.8% and its ED50 was 125 mg/kg. The activity lasted over 32 hr.The above results demonstrated that KC-6141 is a compound with more potent action on the platelet aggregation, as well as on the platelet retention than aspirin and dipyridamole – a known antithrombotic drug.

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