• Title/Summary/Keyword: Pharmacological properties

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Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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Lepidium sativum (Garden cress): a review of contemporary literature and medicinal properties

  • Mali, Ravindra G;Mahajan, Shailaja G;Mehta, Anita A
    • Advances in Traditional Medicine
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    • v.7 no.4
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    • pp.331-335
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    • 2007
  • The utility of Lepidium sativum Linn (Garden cress) as a medicinal plant has increased many fold over a period of time. A survey of literature relating to the medicinal uses of L.sativum reveals it to be one of the widely used medicinal plants. It finds place in folklore medicine, Ayurveda, Unani and other indigenous systems of medicine. Following a large number of claims on the wide range of traditional medicinal properties of the plant, considerable efforts have been made to verify its efficacy as a curative agent through pharmacological investigations and clinical trials. In this article, a comprehensive account of the traditional uses, phytochemical investigation and therapeutic potential of Lepidium sativum is presented.

A Review on Phytochemistry and Pharmacology of Sparassis crispa (꽃송이버섯의 구성성분과 약리효과에 대한 리뷰)

  • Bang, Rodae;Lee, Young-Jong
    • The Korea Journal of Herbology
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    • v.34 no.6
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    • pp.131-138
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    • 2019
  • Objective : Sparassis crispa has been recognized for its therapeutic value since the late 20th century because of its high β-glucan content. Since then, researches have been conducted on the pharmacological effects but most of these are individual studies on the effects of β-glucan from S. crispa and the comprehensive reviews are lacking. The purpose of this study was to review the compounds composition and pharmacological effects of S. crispa. Methods : This review analyzes the papers about chemical and nutritional composition and pharmacological effects of S. crispa. The data in this review is based on selected papers after reviewing all studies containing the keyword "sparassis crispa" for PubMed, NDSL, and J-Stage published before February 2019. Results : S. crispa is composed of protein, lipids, and carbohydrates. Most of the compounds are carbohydrates and the highest content is β-glucan. More than 40% of the dried fruiting body of S. crispa is composed of β-glucan. In addition, it contains polyphenols, flavonoids, terpenoids and phthalide-based compounds. Broad spectrum of its pharmacological actions have been established which include immunomodulatory, anticancer, antiinflammatory, antioxidant, hypoglycemic, antiobesic and neuroprotective effects. Conclusion : The most studied fields have been shown to have immunomodulatory and anticancer effects by inhibiting the proliferation of cancer cells and angiogenesis and increasing hematopoitic responses. Unique structure and characteristic of high molecular weight β-glucan are considered to have high immunomodulatory effects of S. crispa. And low molecular fractions or phthalides of S. crispa also have antioxidant, immunomodulatory and anticancer effects.

Natural radioprotectors and their impact on cancer drug discovery

  • Kuruba, Vinutha;Gollapalli, Pavan
    • Radiation Oncology Journal
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    • v.36 no.4
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    • pp.265-275
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    • 2018
  • Cancer is a complex multifaceted illness that affects different patients in discrete ways. For a number of cancers the use of chemotherapy has become standard practice. Chemotherapy is a use of cytostatic drugs to cure cancer. Cytostatic agents not only affect cancer cells but also affect the growth of normal cells; leading to side effects. Because of this, radiotherapy gained importance in treating cancer. Slaughtering of cancerous cells by radiotherapy depends on the radiosensitivity of the tumor cells. Efforts to improve the therapeutic ratio have resulted in the development of compounds that increase the radiosensitivity of tumor cells or protect the normal cells from the effects of radiation. Amifostine is the only chemical radioprotector approved by the US Food and Drug Administration (FDA), but due to its side effect and toxicity, use of this compound was also failed. Hence the use of herbal radioprotectors bearing pharmacological properties is concentrated due to their low toxicity and efficacy. Notably, in silico methods can expedite drug discovery process, to lessen the compounds with unfavorable pharmacological properties at an early stage of drug development. Hence a detailed perspective of these properties, in accordance with their prediction and measurement, are pivotal for a successful identification of radioprotectors by drug discovery process.

Mesenchymal stem cells in the treatment of osteonecrosis of the jaw

  • Nifosi, Gianfilippo;Nifosi, Lorenzo;Nifosi, Antonio Fabrizio
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.47 no.2
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    • pp.65-75
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    • 2021
  • Medication-related osteonecrosis of the jaw (MRONJ) has recently associated to the increase in antiresorptive and anti-angiogenic drugs prescriptions in the treatment of oncologic and osteoporotic patients. The physiopathogenesis of MRONJ remains unclear and available treatments are unsatisfactory. Newer pharmacological treatments have shown good results, but are not curative and could have major side effects. At the same time as pharmacological treatments, mesenchymal stem cells (MSCs) have emerged as a promising therapeutic modality for tissue regeneration and repair. MSCs are multipotential non-hematopoietic progenitor cells capable to differentiating into multiple lineages of the mesenchyme. Bone marrow MSCs can differentiate into osteogenic cells and display immunological properties and secrete paracrine anti-inflammatory factors in damaged tissues. The immunomodulatory, reparative, and anti-inflammatory properties of bone marrow MSCs have been tested in a variety of animal models of MRONJ and applied in specific clinical settings. The aim of this review is to discuss critically the immunogenicity and immunomodulatory properties of MSCs, both in vitro and in vivo, the possible underlying mechanisms of their effects, and their potential clinical use as modulators of immune responses in MRONJ, and to identify clinical safety and recommendations for future research.

Comparative evaluation of the efficacy of wound healing with and without dehydrated human amniotic/chorionic membrane in alveoloplasty: a pilot study

  • Gajul, Monica;Bhate, Kalyani;Awate, Sayali;Kakodkar, Pradnya;Shah, Sonal
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.47 no.4
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    • pp.279-285
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    • 2021
  • Objectives: Wound healing is an integral part of any surgical procedure. Appropriate wound closure is critical to any successful surgical procedure, especially intraoral procedures. Various factors aid in wound healing, both pharmacological and non-pharmacological. Dehydrated human amniotic/chorionic membrane (dHACM) is an emerging bioinert material that contains anti-inflammatory properties, angiogenetic properties, osteogenic potential, and various growth factors. The purpose of this study was to evaluate the efficacy of wound healing properties of dHACM in bilateral alveoloplasty patients. Materials and Methods: A prospective split-mouth study was conducted on 10 patients. Site A received sutures with dHACM and site B was sutured without dHACM. Wound healing was assessed with the Landry, Turnbull, and Howley Index. Results: Sites A and site B were compared. A P<0.05 and a test value of 22 was obtained, indicating a statistical difference between the two sites. Conclusion: Our study showed better healing with dHACM than without.

Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay

  • Kim, Young-Hoon;Bae, Young-Ji;Kim, Hyung Soo;Cha, Hey-Jin;Yun, Jae-Suk;Shin, Ji-Soon;Seong, Won-Keun;Lee, Yong-Moon;Han, Kyoung-Moon
    • Biomolecules & Therapeutics
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    • v.23 no.5
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    • pp.486-492
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    • 2015
  • Drug metabolism mostly occurs in the liver. Cytochrome P450 (CYP) is a drug-metabolizing enzyme that is responsible for many important drug metabolism reactions. Recently, the US FDA and EU EMA have suggested that CYP enzyme induction can be measured by both enzymatic activity and mRNA expression. However, these experiments are time-consuming and their interassay variability can lead to misinterpretations of the results. To resolve these problems and establish a more powerful method to measure CYP induction, we determined CYP induction by using luminescent assay. Luminescent CYP assays link CYP enzyme activity to firefly luciferase luminescence technology. In this study, we measured the induction of CYP isozymes (1A2, 2B6, 2C9, and 3A4) in cryopreserved human hepatocytes (HMC424, 478, and 493) using a luminometer. We then examined the potential induction abilities (unknown so far) of mesalazine, a drug for colitis, and mosapride citrate, which is used as an antispasmodic drug. The results showed that mesalazine promotes CYP2B6 and 3A4 activities, while mosapride citrate promotes CYP1A2, 2B6, and 3A4 activities. Luminescent CYP assays offer rapid and safe advantages over LC-MS/MS and qRT-PCR methods. Furthermore, luminescent CYP assays decrease the interference between the optical properties of the test compound and the CYP substrates. Therefore, luminescent CYP assays are less labor intensive, rapid, and can be used as robust tools for high-throughput CYP screening during early drug discovery.

Pharmacological Actions of $\imath$--Muscone on Cerebral Ischemia and Central Nervous System ($\imath$-Muscone의 뇌허혈 및 중추신경계에 관한 약효연구)

  • 조태순;이선미;이은방;조성익;김용기;신대희;박대규
    • Biomolecules & Therapeutics
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    • v.5 no.3
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    • pp.306-315
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    • 1997
  • In order to investigate pharmacological properties of ι -muscone, effects of ι-muscone and musk on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in Mongolian gerbils. The histological observations showed a preventive effect of the ι-muscone treatment with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by the ι-muscone treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils.˙ This elevation was prevented by the ι-muscone treatment. While ι-muscone had no effects on the hexobarbital-induced sleeping time and the convulsions induced by electric shock, pentetrazol and strychnine, it had effect on rotarod test and spontaneous activity test. Respiration rate and depth were increased by the ι-muscone treatment. Furthermore, ι-muscone showed anti-stress effect. Our findings suggest that the pharmacological profile of ι-muscone on cerebral ischemia and central nervous system are similar to that of musk.

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Pharmacological Actions of New Woohwangchungsimwon Liquid on Cerebral Ischemia and Central Nervous System (신우황청심원액의 뇌허혈 및 중추신경계에 관한 약효연구)

  • 조태순;이선미;이은방;조성의;김용기;신대희;박대규
    • Biomolecules & Therapeutics
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    • v.5 no.4
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    • pp.402-411
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    • 1997
  • ln order to investigate pharmacological properties of New Woohwangchungsimwon Liquid (NCL) and Woohwangchungsimwon Liquid (CL), effects of NCL and CL on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in Mongolian gerbils. The histological observations showed a preventive effect of NCL and CL treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by CL treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils. This elevation was inhibited by NCL and CL treatments. While NCL and CL had no effects on the hexobarbital-induced sleeping time, they prevented the seizures induced by electric shock and pentetrazol. NCL and CL showed sedative effect in rotarod and spontaneous activity test. Respiration rate and depth were increased at the high dose of NCL and CL. Furthermore, NCL and CL showed anti-stress effect. Our findings suggest that the pharmacological profile of NCL on cerebral ischemia and central nervous system are similar to that of CL.

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