• Title/Summary/Keyword: Thrombin inhibitory activity

Search Result 75, Processing Time 0.022 seconds

Inhibitory effects of thromboxane A2 generation by ginsenoside Ro due to attenuation of cytosolic phospholipase A2 phosphorylation and arachidonic acid release

  • Shin, Jung-Hae;Kwon, Hyuk-Woo;Rhee, Man Hee;Park, Hwa-Jin
    • Journal of Ginseng Research
    • /
    • v.43 no.2
    • /
    • pp.236-241
    • /
    • 2019
  • Background: Thromboxane A2 ($TXA_2$) induces platelet aggregation and promotes thrombus formation. Although ginsenoside Ro (G-Ro) from Panax ginseng is known to exhibit a $Ca^{2+}-antagonistic$ antiplatelet effect, whether it inhibits $Ca^{2+}-dependent$ cytosolic phospholipase $A_2$ ($cPLA_{2{\alpha}}$) activity to prevent the release of arachidonic acid (AA), a $TXA_2$ precursor, is unknown. In this study, we attempted to identify the mechanism underlying G-Ro-mediated $TXA_2$ inhibition. Methods: We investigated whether G-Ro attenuates $TXA_2$ production and its associated molecules, such as cyclooxygenase-1 (COX-1), $TXA_2$ synthase (TXAS), $cPLA_{2{\alpha}}$, mitogen-activated protein kinases, and AA. To assay COX-1 and TXAS, we used microsomal fraction of platelets. Results: G-Ro reduced $TXA_2$ production by inhibiting AA release. It acted by decreasing the phosphorylation of $cPLA_{2{\alpha}}$, p38-mitogen-activated protein kinase, and c-Jun N-terminal kinase1, rather than by inhibiting COX-1 and TXAS in thrombin-activated human platelets. Conclusion: G-Ro inhibits AA release to attenuate $TXA_2$ production, which may counteract $TXA_2-associated$ thrombosis.

In-vitro Anti-thrombosis Activities of Different Parts of Nelumbo nucifera Gaertner (다양한 부위별 연 추출물의 항혈전 활성)

  • Ahn, Seon-Mi;Sung, Hwa-Jung;Kim, Jong-Sik;Park, Jong-Yi;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
    • /
    • v.46 no.4
    • /
    • pp.372-376
    • /
    • 2018
  • To investigate the bio-activities of lotus (Nelumbo nucifera Gaertner), ethanol extracts were prepared from different parts of lotus, including lotus root, node of root (NR), leaf, pod of seed (PS), seed (S), and embryo of seed (ES), respectively. Anti-thrombosis activities were evaluated. NR, S, and PS extracts displayed strong anti-coagulation activities, as evidenced by the inhibition of thrombin, prothrombin, and coagulation factors, respectively. NR, leaf, S, and PS extracts displayed strong platelet aggregation inhibitory activities. The aggregation inhibition of S and PS extract was comparable to that of aspirin. The extracts of NR, S, and PS did not show hemolysis activity up to 1.0 mg/ml.

Evaluation of Anti-thrombosis Activities of Different Parts of Cannabis sativa L. (대마 부위별 추출물의 항혈전 활성)

  • Kang, Deok-Gyeong;Kim, Young-Min;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.31 no.6
    • /
    • pp.581-586
    • /
    • 2021
  • The high fatality of COVID-19 (Corona Virus Disease 2019) is closely related to acute pneumonia and severe blood clot formation in brain, heart, kidney and lung. The use of low-molecular weight heparins has been shown to reduce the risk of thrombosis and reduce fatality rates among COVID-19 patients. In this study, we investigated the antithrombotic activity of different parts of C. sativa extracts to determine its potential in preventing blood clots in patients with thromboprophylaxis. The extracts of leaf, stem, root, immature flower and seed of C. sativa showed strong inhibitory activities on blood clot formation. In particular, the flower extract showed the strongest inhibitions against blood coagulation factors and thrombin. Strong hemolysis activities were observed in flower extract and seed extract, suggested that removal of the hemolysis active compounds in th extracts is necessary. This is a first report of anti-thrombosis activities of different parts of C. sativa extracts, and our results suggest that C. sativa extract has potential has a valuable bioresource for high-value products.

Anticoagulant Activity of Sulfated Polysaccharides Isolated from Codium fragile (청각 산추출물에서 정제한 함황다당류의 항응고활성)

  • Park, Mee-Kyung;Kweon, Mee-Hyang;Cho, Hong-Yon;Yang, Han-Chul
    • Applied Biological Chemistry
    • /
    • v.42 no.2
    • /
    • pp.140-146
    • /
    • 1999
  • We have isolated two anticoagulant polysaccharides from an acidic extract of Codium fragile. The purification was conducted using three consecutive chromatographies of DEAE-Toyopearl 650C, Sephadex G-100 (G-75), and Sepharose CL-6B by measuring activated partial thromboplastin time (APTT). The two purified anticoagulant polysaccharides, CF-1-VIa-1 and CF-1-VIIa-1, were found to be nearly homogenous on HPLC using a gel permeation column and appeared to have molecular weights of about 80,000 Da and 40,000 Da, respectively. The polysaccharides consisted mainly of arabinose and galactose in a molar ratio of about 2 : 1, and also comprised 12-13% of sulfates at their constituent sugars. CF-1-VIa-1 and CF-1-VIIa-1 inhibited blood coagulation via both the intrinsic and the extrinsic pathways. The polysaccharides unlike heparin showed an inhibitory activity on thrombin when a pure fibrinogen without antithrombin III was used as a substrate. Structural modifications using sulfation and desulfation affected the anticoagulant activities directly, suggesting that the content of sulfate plays an important role in the blood coagulation cascade. The polysaccharides may inhibit some proteases involved in the blood coagulation cascade, judging from the independence of calcium concentrations in their anticoagulant activity.

  • PDF

Anti-coagulation and Anti-platelet Aggregation Activities of Black Ginger (Kaempferia parviflora) (흑생강(Kaempferia parviflora)의 항응고 및 혈소판 응집저해 활성)

  • Lee, Man-Hyo;Sung, Hwa-Jung;Kwon, Chong Suk;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.28 no.9
    • /
    • pp.1068-1075
    • /
    • 2018
  • Kaempferia parviflora, an herbaceous plant in the family Zingiberaceae, is popular in many tropical regions. It is called as black ginger or krachaidum in Thailand and Laos, and its raw or dried root have been used as spices and teas. The rhizomes also have been traditionally used to treat gastrointestinal disorders, ulcers, gout, dysentery, allergies and to improve physical work capacity. Recently, its anti-obesity, anti-oxidant, anti-inflammatory and blood clot-lysis activities were reported. In this study, the anti-thrombosis activity of black ginger was investigated, since improvement in blood fluidity leads to the prevention of various lifestyle-related diseases. The hot water and ethanol extract and their subsequent solvent fractions (hexane, ethylacetate, butanol fractions and water residue) were prepared, and their anti-coagulation and platelet aggregation inhibitory activities were determined, respectively. Among the black ginger extracts and their fractions, the ethylacetate fraction (EAF) of ethanol extract only showed significant extensions of blood coagulation time determined by thrombin time (TT), prothrombin time (PT), and activated partial thromboplastin time (aPTT). At 5 mg/ml concentration, TT, PT and aPTT were extended to 1.22, 1.49 and >15-folds compared to non-treatment. The EAFs of ethanol and hot water extract showed strong inhibitions against collagen-induced platelet aggregations, which are comparable to inhibitions of aspirin. Also the EAFs from black ginger did not show any hemolysis activity against human RBC up to 0.5 mg/ml. Our results suggest that the EAF of black ginger has a potential as novel anti-coagulation and ant-platelet aggregation agent. This report provides the first evidence of anti-coagulation activity of black ginger.

Antithrombotic Activity of Hermetia illucens (Black Soldier Fly) (동애등에의 항혈전 활성)

  • Pyo, Su-Jin;Won, Jun;Kang, Deok-Gyeong;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.30 no.4
    • /
    • pp.386-393
    • /
    • 2020
  • Insect industry has been focused as production of food, animal feed, pollinator and for environmental remediation. Hermetia illicens, called as black soldier fly (BSF) is famous as nutritive feed. In this study, to evaluate the antithrombotic activities of BSF, the larvae (instar 2~6), pupae, residue after adult emergence [RAAE] and adult of Hermetia illicens [black soldier fly, BSF] were collected and their ethanol extracts were prepared. Growth of BSF larvae was very rapid and the weight of larvae was increased to 25-folds during 10 days cultivation. The ethanol extraction ratios showed from 1.0% (pupae) to 18.5%(adults). The highest total polyphenol, total flavonoid, and total sugar contents were observed in RAEE (17.2 mg/g), pupae (3.4 mg/g), and instar 6 (37.6 mg/g), suggesting that metabolic changes occur during the life cycle of the BSF. Anti-coagulation assay showed that extracts of RAEE, instar 6 and pupa of BSF significantly inhibited thrombin, prothrombin, and blood coagulation factors. Furthermore, the extracts of RAEE, instar 3 and adult of BSF showed a strong platelet aggregation inhibitory activity. Our results suggest that pupae and RAEE of BSF have potential as antithrombotic agents. This is the first study to provide evidence of the antithrombotic activity of the BSF and bioactivity alterations during its life cycle.

Anti-coagulation and Platelet Aggregation Inhibitory Activities of the Ethanol Extract of Aerial Bulbils of Dioscorea alata L. (열대마 영여자 추출물의 항응고 및 혈소판 응집저해 활성)

  • Su-Gyeong Jeon;So-Young Choe;Kyung-Ran Im;Jong-Pil Lee;Jun-Hong Park;Ho-Yong Sohn
    • Journal of Life Science
    • /
    • v.34 no.3
    • /
    • pp.153-159
    • /
    • 2024
  • Dioscorea alata L, commonly known as "tropical yam" is the most widely consumed yam species among the 650 yam species belonging to the Dioscoreacea family. It is extensively cultivated in tropical and subtropical regions and is a major food source in Africa and India. Also, it is used for medicinal purposes, particularly in China and Taiwan, for its anti-inflammatory properties. In comparison to other yam varieties such as D. batatas or D. opposita, the tropical yam has gained popularity in Korea due to its higher yield per unit area. In this study, the nutritional characteristics and anti-thrombosis activity of the aerial bulbils of D. alata L. tropical yam were compared to those of D. opposita. The results showed that the aerial bulbils of tropical yam exhibited nutritional characteristics and potent anticoagulant activity compared to those of domestic yam varieties. The bulbils extract of tropical yam showed superior anticoagulant activities against thrombin, prothrombin and blood coagulation factors. Furthermore, the bulbils extract of tropical yam exhibited strong platelet aggregation inhibition at 0.25 mg/ml and showed no hemolytic activity up to a concentration of 2.5 mg/ml. These findings suggest the potential development of high-value anti-thrombosis agents utilizing the aerial bulbils of tropical yam.

A Comparison of the Components and Biological Activities in Raw and Boiled Red Beans (Phaseolus radiatus L.) (생팥과 증자팥의 성분 및 생리활성 비교)

  • Lee, Ryun Kyung;Kim, Mi-Sun;Lee, Ye-Seul;Lee, Man-Hyo;Lee, Jong Hwa;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
    • /
    • v.42 no.2
    • /
    • pp.162-169
    • /
    • 2014
  • In the course of study for the development of functional food using red beans (azuki beans, Phaseolus radiatus L.), the ethanol extracts from raw-red bean (RRB) and boiled-red bean (BRB) were prepared, and the components and various biological activities of both were compared. It was observed that the extraction yield, and the total polyphenol content, of the BRB were 1.2 times higher than that of the RRB. However, the contents of total flavonoid, total sugar and reducing sugar in the BRB were 30, 27.9 and 30.8% respectively when compared with those of RRB. In relation to antioxidative activity, both RRB and BRB exhibited moderate DPPH anion, ABTS cation, and nitrite scavenging activities and reducing power, though in all cases RRB demonstrated stronger activities than BRB. The extracts of RRB and BRB did not reveal any antimicrobial activities. In a ${\alpha}$-amylase inhibitory activity assay, RRB was higher than BRB, while BRB showed higher ${\alpha}$-glucosidase inhibitory activity than RRB. A strong and particular activity was observed in an anti-thrombosis activity assay of RRB. The extract of RRB demonstrated strong inhibitions against prothrombin and blood coagulation factors, with moderate thrombin inhibition. However, the extract of BRB did not exhibit any significant anti-thrombosis activity. Our results indicate that RRB has different, but useful biological activities, and loss or elimination of the biologically active substances in RRB occurs during the production of BRB. Therefore, to develop more functional foods from red beans, a study of suitable boiling, heating and drying processes is essential, and the efficient re-use of boiled waste water from the boiling process is necessary. These results could be applied to the further development of functional red bean beverages and sweat red bean pastes.

Anti-oxidation and Anti-thrombosis Activities of Polyphenol-enriched Fraction of Acorn Pollen Extract (도토리 화분 추출물의 폴리페놀 고함유 분획물의 항산화 및 항혈전 활성)

  • Lee, Yun-Jin;Kang, Deok-Gyeong;Pyo, Su-Jin;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.32 no.7
    • /
    • pp.501-509
    • /
    • 2022
  • Pollen corrected from Quercus species is abundant in Korea and has been used to treat anemia and inflammation of the prostate gland. It is also used for hemostasis in oriental medicine. In this study, the ethanol extract of the acorn pollen and its subsequent organic solvent fractions using hexane, ethylacetate, butanol, and water residue were prepared, and their antioxidant, anti-thrombosis, and hemolysis activities were evaluated. The ethylacetate fraction of acorn pollen (EF-AP) showed the highest polyphenol content (225.0 mg/g) and strong antioxidant activity among the solvent fractions. The RC50 of EF-AP against DPPH, ABTS, and nitrite radicals was 72.2, 27.7, and 62.6 ㎍/ml, respectively. The blood coagulation activities of the all-solvent fractions determined by thrombin time, prothrombin time, and activated partial thromboplastin time were negligible up to 5 mg/ml. Platelet aggregation inhibitory activities were observed in the EF-AP, butanol fraction, and water residue, whereas hexane fraction induced strong platelet aggregation. The EF-AP has no hemolysis activity against human RBC up to 1 mg/ml. UPLC/MS/MS analysis of the EF-AP revealed that rutin, isoquercitrin, and astragalin are major compounds for antioxidant and anti-thrombosis activities. Our results suggest that EF-AP could be developed as a noble antioxidant and anti-thrombosis agent.

Changes in the in vitro Antioxidant and Antithrombosis Activities of Salicornia europaea According to Harvest Time (수확시기에 따른 함초의 항산화 및 항혈전 활성의 변화)

  • Kim, Mi-Sun;Lee, Jung-Nam;Seong, Ha-Jung;Kim, Deuk Hoi;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.26 no.9
    • /
    • pp.1033-1040
    • /
    • 2016
  • In Korea, the aerial parts of the halophyte Salicornia europaea, known as hamcho, are used in salads in April–June and in oriental medicine in September–October In this study, with the aim of developing functional foods to aid blood circulation, hot water extract (HWE) and ethanol extract (EE) were prepared using hamcho harvested from the fields of Shinan, Jeonnam, Korea on 5th April (HWE-04, EE-04), 5th July (HWE-06, EE-06), 5th August (HWE-08, EE-08), 5th September (HWE-09, EE-09), and 5th October (HWE-10, EE-10), and their antioxidant and antithrombosis activities were evaluated. Among the HWEs, HWE-10 showed the highest concentration of total polyphenols and total flavonoids (22.4 and 17.6 mg/ml, respectively), and EE-09 had the highest concentration among the EEs (20.1 and 19.3 mg/ml, respectively). Among the HWEs and EEs, HWE-08 and EE-08 had the highest total sugar and reducing sugar content. In the antioxidation assay, HWE-10 and EE-09 showed strong reducing power, as well as DPPH, ABTS, and nitrite scavenging activities. The calculated RC50s of EE-09 against DPPH, ABTS, and nitrite were 578, 277, and 68.8 μg/ml, respectively. The antithrombosis activity assay revealed that HWE-04, HWE-06, EE-04, and EE-06 had anticoagulation activity against coagulation factors and that HWE-08, HWE-09, EE-08, and EE-09 expressed strong thrombin inhibitory activity, which was comparable to the antithrombosis activity of aspirin. In addition, EE-06 and HWE-08 exhibited strong aggregation inhibitory activities against human platelets. The results suggest that extract from hamcho harvested in particular periods and prepared using a defined solvent has strong potential as a novel food ingredient and an antioxidant and antithrombosis agent.