• Title/Summary/Keyword: analgesic agents

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The antinociceptive effect of artemisinin on the inflammatory pain and role of GABAergic and opioidergic systems

  • Dehkordi, Faraz Mahdian;Kaboutari, Jahangir;Zendehdel, Morteza;Javdani, Moosa
    • The Korean Journal of Pain
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    • v.32 no.3
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    • pp.160-167
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    • 2019
  • Background: Pain is a complex mechanism which involves different systems, including the opioidergic and GABAergic systems. Due to the side effects of chemical analgesic agents, attention toward natural agents have been increased. Artemisinin is an herbal compound with widespread modern and traditional therapeutic indications, which its interaction with the GABAergic system and antinoniceptive effects on neuropathic pain have shown. Therefore, this study was designed to evaluate the antinociceptive effects of artemisinin during inflammatory pain and interaction with the GABAergic and opioidergic systems by using a writhing response test. Methods: On the whole, 198 adult male albino mice were used in 4 experiments, including 9 groups (n = 6) each with three replicates, by intraperitoneal (i.p.) administration of artemisinin (2.5, 5, and 10 mg/kg), naloxone (2 mg/kg), bicuculline (2 mg/kg), saclofen (2 mg/kg), indomethacin (5 mg/kg), and ethanol (10 mL/kg). Writhing test responses were induced by i.p. injection of 10 mL/kg of 0.6% acetic acid, and the percentage of writhing inhibition was recorded. Results: Results showed significant dose dependent anti-nociceptive effects from artemisinin which, at a 10 mg/kg dose, was statistically similar to indomethacin. Neither saclofen nor naloxone had antinociceptive effects and did not antagonize antinociceptive effects of artemisinin, whereas bicuculline significantly inhibited the antinocicptive effect of artemisinin. Conclusions: It seems that antinocicptive effects of artemisinin are mediated by $GABA_A$ receptors.

Pain management in periodontal therapy using local anesthetics and other drugs: an integrative review

  • Eduarda Cristina Santos;Daniela Huller;Sabrina Brigola;Marceli Dias Ferreira;Marcia Thais Pochapski;Fabio Andre dos Santos
    • Journal of Dental Anesthesia and Pain Medicine
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    • v.23 no.5
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    • pp.245-256
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    • 2023
  • Background: Surgical and non-surgical periodontal procedures often lead to postoperative pain. Clinicians use pharmacological methods such as anesthetics, anti-inflammatory drugs, and analgesics for relief. However, the multitude of options makes it challenging to select the best approach for routine dental care. Objective: This review aimed to describe previous studies regarding the pharmacological management used for pain control during periodontal procedures as well as factors that may interfere with patients' perception of pain. Methods: We included studies (period of 2000-2023, whose approach corresponded to the pharmacological protocols used for preoperative, trans-operative, and postoperative pain control in adult patients undergoing surgical and non-surgical periodontal therapy. Results: A total of 32 studies were included in the analysis, of which 17 (53%) were related to anesthetic methods and 15 (47%) were related to therapeutic protocols (anti-inflammatory/analgesic agents). These studies predominantly involved nonsurgical periodontal procedures. Studies have reported that factors related to age, type of procedure, and anxiety can influence pain perception; however, only seven of these studies evaluated anxiety. Conclusions: Numerous methods for pain control can be applied in periodontal therapy, which are accomplished through anesthetic methods and/or therapeutic protocols. Factors such as anxiety, age, and type of procedure are related to pain perception in patients. Thus, it is the responsibility of dentists to evaluate each clinical situation and define the best protocol to follow based on the literature.

Lactic Acid Bacteria Increases Hypolipidemic Effect of Crocin Isolated from Fructus of Gardenia jasminoides

  • Lee In-Ah;Min Sung-Won;Kim Dong-Hyun
    • Journal of Microbiology and Biotechnology
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    • v.16 no.7
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    • pp.1084-1089
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    • 2006
  • The fructus of Gardenia jasminoides Ellis (GF) has been widely used as a natural colorant in Asian countries, and also as a Chinese traditional medicine for its homeostatic, antiphlogistic, analgesic, and antipyretic effects. In the present study, its main component, crocin, was fermented with lactic acid bacteria (LAB) and their antihyperlipidemic activity was measured. The GF extract, fermented GF (F-GF), crocin, and fermented crocin (F-crocin) significantly inhibited the increase of serum triglyceride (TG) level in corn oil feeding-induced triglyceridemic mice, as well as that of serum TG and total and LDL cholesterol levels in Triton WR-1339-induced hyperlipidemic mice. These agents also showed hypolipidemic activity in hyperlipidemic mice induced by high fat diet for 5 weeks. F-GF and F-crocin exhibited more potent hyperlipidemic effects than GF and crocin. The results suggest that the hypolipidemic effect of GF and crocin can be synergistically activated by LAB, and that F-GF and F-crocin may improve hyperlipidemia in clinic, compared with GF and crocin.

Medicinal plants traditionally used for the management of female reproductive health dysfunction in Tana River County, Kenya

  • Kaingu, Catherine Kaluwa;Oduma, Jemimah Achieng;Mbaria, James Mucunu;Kiama, Stephen Gitah
    • CELLMED
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    • v.3 no.2
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    • pp.17.1-17.10
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    • 2013
  • Reproductive dysfunction is a major health concern amongst the inhabitants of Tana River County. An ethno botanical study was conducted in Garsen, Itsowe and Ngao sub divisions of Tana River County to document the utilization of medicinal plants for the management of female reproductive ailments. The target population was practicing herbalists from Pokomo, Ormo and Giryama communities in the study area. Structured questionnaires and focussed group discussions were used to collect data. Forty eight plant species distributed in 40 genera and 29 families were documented as being important for the management of pregnancy related complications, menstrual disorders, infertility, fibroids and as contraceptives. The species most frequently cited by the herbalists were fourteen. Fifty two percent of the plant species were probably being mentioned for the first time as being useful in reproductive health management. In conclusion, Tana River has a pool of TMPs with a wealth of indigenous knowledge that needs to be exploited. The plants used to treat dysmenorrhea for example may be important analgesic agents that need further investigation while those with anti-fertility properties may contain steroidal phyto chemical compounds. Such species therefore need further investigation to establish their efficacy and mechanism of action.

Influence of Aspirin on Pilocarpine-Induced Epilepsy in Mice

  • Jeong, Kyoung Hoon;Kim, Joo Youn;Choi, Yun-Sik;Lee, Mun-Yong;Kim, Seong Yun
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.1
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    • pp.15-21
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    • 2013
  • Aspirin (acetylsalicylic acid) is one of the most widely used therapeutic agents based on its pharmacological actions, including anti-inflammatory, analgesic, anti-pyretic, and anti-thrombotic effects. In this study, we investigated the effects of aspirin on seizure susceptibility and hippocampal neuropathology following pilocarpine-induced status epilepticus (SE). SE was induced by pilocarpine hydrochloride (280 mg/kg, i.p.) administration in C57BL/6 mice (aged 8 weeks). Aspirin was administered daily (15 mg/kg or 150 mg/kg, i.p.) for 10 days starting 3 days before SE, continuing until 6 days after SE. After pilocarpine injection, SE onset time and mortality were recorded. Neuronal cell death was examined using cresyl violet and Fluoro-Jade staining, and glial responses were observed 7 days post SE using immunohistochemistry. In the aspirin-treated group, the onset time of SE was significantly shortened and mortality was markedly increased compared to the control group. However, in this study, aspirin treatment did not affect SE-induced neuronal cell death or astroglial and microglial responses in the hippocampus. In conclusion, these results suggest that the safety of aspirin should be reevaluated in some patients, especially with neurological disorders such as temporal lobe epilepsy.

Aromatherapy of Patients with Arthritis (관절염 환자를 위한 아로마테라피)

  • Kim, Myung-Ja;Nam, Eun-Sook
    • Journal of muscle and joint health
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    • v.11 no.1
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    • pp.7-17
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    • 2004
  • In this paper, we checked health problems of patients who suffered from arthritis. After assessing each patients condition, in order to alleviate their sufferings, we introduced several methods of aromatherapy as a holistic approach to these health problems. Aromatherapy is used of essential oils, which are obtained from aromatic plants, can be defined as a nature-friendly complementary/alternative method, has its great merit in its each way of application. If the arthritis condition is localized, massage,compress or poultices, and hand or foot baths are most effective. Many of essential oils in the recipe have dual benefits, as anti-inflammative and analgesic agents. The Juniper and carrot seed aid in eliminating fluid and toxin accumulation in the joint and surrounding tissue. There are many different courses available and health professional should choose one that is relevant to clinical practice. Considering the future of nursing as a major contribution in the consumer-centered structure of medical health service, aromatherapy as a complementary/alternative method is expected to contribute not only to establishing more effective health service but also to resolving chronic health problems of arthritis.

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The Novel Synthetic Substance MR-387C[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-L-leucine] as an Aminopeptidase M Inhibitor

  • Chung, Myung-Chul;Chun, Hyo-Kon;Lee, Ho-Jae;Kho, Yung-Hee
    • BMB Reports
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    • v.28 no.1
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    • pp.83-86
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    • 1995
  • In the course of screening for new aminopeptidase M inhibitors which were expected to be analgesic, immunopotentiating, or anti-metastatic agents, the novel synthetic substance MR-387C[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-L-leucine] (M.W. 504 daltons) was obtained. It was competitive with the substrate and had an $IC_{50}$ value of $0.04\;{\mu}m/ml$ ($7.9{\times}10^{-8}\;M$) and an inhibition constant ($K_i$) of $3.8{\times}10^{-8}\;M$. This novel MR-387C was compared with various known inhibitors of aminopeptidase M. It inhibited the enzyme more strongly than any other microorganism-originated inhibitor, except probestin.

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Adenosine Kinase Inhibitor Design Based on Pharmacophore Modeling

  • Lee, Yun-O;Bharatham, Nagakumar;Bharatham, Kavitha;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
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    • v.28 no.4
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    • pp.561-566
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    • 2007
  • Adenosine kinase (AK) is a ubiquitous intracellular enzyme, which catalyzes the phosphorylation of adenosine (ADO) to adenosine monophosphate (AMP). AK inhibitors have therapeutic potential as analgesic and antiinflammatory agents. A chemical feature based pharmacophore model has been generated from known AK inhibitors (26 training set compounds) by HypoGen module implemented in CATALYST software. The top ranked hypothesis (Hypo1) contained four features of two hydrogen-bond acceptors (HBA) and two hydrophobic aromatics (Z). Hypo1 was validated by 124 test set molecules with a correlation coefficient of 0.905 between experimental and estimated activity. It was also validated by CatScramble method. Thus, the Hypo1 was exploited for searching new lead compounds over 238,819 chemical compounds in NCI database and then the selected compounds were screened based on restriction estimated activity and Lipinski's rules to evaluate their drug-like properties. Finally we could obtain 72 new lead candidates and the two best compound structures from them were posted.

Inclusion Complex of Analgesic and Antiinflammatory agents with Cyclodextrins (I): Enhancement of Dissolution of Ibuprofen by $2-Hydroxypropyl-{\beta}-cyclodextrin$ (시클로덱스트린과 소염진통제 간의 포접복합체에 관한 연구(I): 2-히드록시프로필-${\beta}$-시클로덱스트린에 의한 이부프로펜의 용출 증가)

  • Oh, In-Joon;Park, Jeong-Gyu;Lee, Yong-Bok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • v.23 no.1
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    • pp.11-18
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    • 1993
  • Inclusion complex of ibuprofen with $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP-{\beta}-CD)$ in aqueous solution and in the solid state was evaluated by the solubility method and the instrumental analysis such as infrared spectroscopy, thermal analysis and x-ray diffractometry. The aqueous solubility of ibuprofen was increased linearly with the increase in the concentration of $HP-{\beta}-CD$, showing an $A_L$ type phase solubility diagram. The results showed that the dissolution rate of ibuprofen was significantly increased by complexation with $HP-{\beta}-CD$. $Ibuprofen-HP-{\beta}-CD$ complex enhanced the mean plasma concentration levels and the area under plasma concentration-time curve after oral administration compared to those of the drug alone. It is concluded that the complex of ibuprofen with $HP-{\beta}-CD$ increases the dissolution rate and improves the bioavailability of the ibuprofen by the formation of a water-soluble complex.

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Synthesis of Methylated Anthranilate Derivatives Using Engineered Strains of Escherichia coli

  • Lee, Hye Lim;Kim, Song-Yi;Kim, Eun Ji;Han, Da Ye;Kim, Bong-Gyu;Ahn, Joong-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.29 no.6
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    • pp.839-844
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    • 2019
  • Anthranilate derivatives have been used as flavoring and fragrant agents for a long time. Recently, these compounds are gaining attention due to new biological functions including antinociceptive and analgesic activities. Three anthranilate derivatives, N-methylanthranilate, methyl anthranilate, and methyl N-methylanthranilate were synthesized using metabolically engineered stains of Escherichia coli. NMT encoding N-methyltransferase from Ruta graveolens, AMAT encoding anthraniloyl-coenzyme A (CoA):methanol acyltransferase from Vitis labrusca, and pqsA encoding anthranilate coenzyme A ligase from Pseudomonas aeruginosa were cloned and E. coli strains harboring these genes were used to synthesize the three desired compounds. E. coli mutants (metJ, trpD, tyrR mutants), which provide more anthranilate and/or S-adenosyl methionine, were used to increase the production of the synthesized compounds. MS/MS analysis was used to determine the structure of the products. Approximately, $185.3{\mu}M$ N-methylanthranilate and $95.2{\mu}M$ methyl N-methylanthranilate were synthesized. This is the first report about the synthesis of anthranilate derivatives in E. coli.