• Title/Summary/Keyword: Antimalarial

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An Isocoumarin with Hepatoprotective Activity in Hep G2 and Primary Hepatocytes from Agrimonia pilosa

  • Ko, Eun-Kyung;Park, Eun-Jeon;Kim, Mi-Hee;Jun, Jung-Yang;Park, Sung-Uk;Sohn, Dong-Hwan;Kim, Youn-Chul
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.383.1-383.1
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    • 2002
  • In connection with our studies on the isolation of hepatoprotective constituents from natural products. we have recently reported hepatoprotective compounds including phenolic bakuchiol. diarylheptanoids. furocoumarins. In the course of continuing efforts. the aqueous extract of the roots of Agrimonia pilosa Ledeb. (Rosaceae) was found to exhibit promising hepatoprotective activity. A. pilosa is a perennial herb distributed throughout South Korea. and its roots have been used as the hemostatic. antimalarial. and antidysenteric agent in oriental medicine. Chemical investigation of the aqueous extract of the roots of this plant. as guided by hepatoprotective active catechin (2). Compound 1 showed hepatoprotective effects on both tacrine-induced cytotoxicity in human level derived Hep G2 cells and tert-hydroperoxide-induced cytotoxicity in rat primary hepatocyles with $EC_{50}$ values of 66.2 $\pm$ 2.8 and 22.9 $\pm$ 2.6 $\mu\textrm{M}$ respectively.

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Autologous Fat Transfer in Lupus Panniculitis Facial Lipoatrophy

  • Kongkunnavat, Natthapong;Prathyajuta, Jirapat;Tonaree, Warangkana
    • Archives of Plastic Surgery
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    • v.49 no.4
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    • pp.527-530
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    • 2022
  • Lupus panniculitis (LP) often presents with tender nodules and intermittent ulcers that then heal with scarring and lipoatrophy. The current mainstay of treatment is medical treatment. Research regarding the treatment of lipoatrophy from LP with autologous fat grafting is limited. We would like to share our experience in this rare case, which was treated with autologous fat transfer. A 48-year-old female presented with erythematous plaque, tender nodules, and ulcers following by a depression of the lesion at the left temporal area. The patient also had indurated erythematous plaque at her left cheek. Both lesions were aggravated by sunlight exposure. After several investigations, she was diagnosed as LP with secondary lipoatrophy and tumid lupus erythematosus at her left temporal and left cheek, respectively. She received antimalarial drug and topical steroids. The patient underwent two sessions of autologous fat transfer. She was satisfied with the volume and contour improvement in the scar following the injection of 8 and 3.7 mL of fat. Furthermore, the patient reported the remission of tender nodules and ulcers since the first fat graft injection. In conclusion, the autologous fat transfer is a simple and effective treatment for lipoatrophy and scar secondary to LP with promising results.

Anti-aggregation Effect of Artemether Through Regulation of PI3K/Akt and MAPK in U46619-induced Platelets (U46619-유도의 혈소판에서 PI3K/Akt 및 MAPK 조절을 통한 Artemether의 응집억제효과)

  • Park, Chang-Eun;Lee, Dong-Ha
    • Korean Journal of Pharmacognosy
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    • v.53 no.2
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    • pp.64-69
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    • 2022
  • When blood vessels are damaged, a rapid hemostatic response should occur in order to lower blood loss and keep normal circulation, and platelet activation and aggregation are essential. Nevertheless, abnormal or excessive platelet aggregation can be a reason of cardiovascular diseases including thrombosis, atherosclerosis, and stroke. Therefore, the screening for a substance which can regulate platelet activation and suppress aggregation reaction is very important for treatment and prevention of cardiovascular diseases. Artemether is a methyl ether derivative of artemisinin, which is isolated from the antimalarial plant Artemisia annua, but research on platelet aggregation or its mechanisms is still insufficient. This study identified the effects of artemether on U46619-induced human platelet aggregation and their granule secretion (ATP and serotonin release). In addition, the effects of artemether on the phosphorylation of PI3K/Akt or MAPK, which are related to signal transduction in platelet aggregation, were studied. As the results, artemether significantly lowered PI3K/Akt and MAPK phosphorylation, which inhibited platelet aggregation through granule secretion (ATP and serotonin release) dose-dependently. Therefore, we suggest that artemether is an antiplatelet substance that regulates PI3K/Akt and MAPK pathway and is of value as a therapeutic and preventive agent for platelet-derived cardiovascular diseases.

1, 5 - bis (4 - methoxyphenyls) - 6, 7 - Dioxa-bicyclo [3.2.2] nonane's Anti-toxoplasmosis Effect that was Separated in Artemisin annula (개똥쑥에서 분리 확인된 endoperoxide ring 구조를 갖는 1,5-bis(4-methoxyphenyl)-6,7-dioxa-bicyclo[3.2.2]nonane의 항톡소포자충 효과)

  • Jiang, Jing-Hua;Kim, Hwa-Kyoung;Kim, Hye-Sook;Kamata, Masaki;Wataya, Yusuke;Park, Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.21 no.1
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    • pp.82-85
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    • 2007
  • The Chinese medicinal plant Artemisia annua is the source of the antimalarial compound artemisinin. By the way, Artemisin annula was known have endoperoxide ring structure is included and has anti-malarial effect. Malaria and Toxoplasma gondii (T. gondii) is belong to Apicomplexa genera. So, confirmed whether we go compound 1,5-bis(4-methoxyphenyl)-6,7-dioxa-bicyclo[3.2.2]nonane that have endoperoxide ring structure and there is anti-toxoplasmosis effect. The efficacy of 1,5-bis(4-methoxyphenyl)-6,7-dioxa-bicyclo[3.2.2] nonane alone was examined in vitro and in a murine model of acute toxoplasmosis. In vitro studies were peformed with HeLa cell cultures, with quantification of Toxoplasma growth by a cell proliferation assay. Selectivity of 1,5-bis(4-methoxyphenyl)-6,7-dioxa-bicyclo[3.2.2]nonane was 4.9 in vitro cell proliferation assay, this is higher than sulfadiazine (selectivity was 1.63). For in vivo studies, mice were acutely infected intraperitoneally with 10$^5$ tachyzoites of the virulent RH strain and then treated perorally for 4 days from 6 hours postinfection. Efficacy was assessed by sequential determination of parasite burdens in peritoneal cavity. in vitro, 1,5-bis(4-methoxyphenyl)-6,7-dioxa-bicyclo[3.2.2]nonane inhibited Toxoplasma growth at a concentration of 150mg/kg of body weight per day, the inhibition ratio was estimated to be 85.72%.

Review on the ethnomedicinal, phytochemical and pharmacological properties of Piper sarmentosum: scientific justification of its traditional use

  • Seyyedan, Atefeh;Yahya, Farhana;Kamarolzaman, Mohammad Fauzi Fahmi;Suhaili, Zarizal;Desa, Mohd Nasir Mohd;Khairi, Hussain Mohd;Somchit, Muhammad Nazrul;Fatimah, Corazon Abdullah;Teh, Lay Kek;Salleh, Mohd Zaki;Zakaria, Zainul Amiruddin
    • CELLMED
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    • v.3 no.3
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    • pp.19.1-19.32
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    • 2013
  • Piper sarmentosum is a creeping herb belongs to the family of Piperaceae. It is locally known to the Malays as 'Pokok kadok' and can be found in different regions of South-East Asia including Malaysia. Ethnopharmacologically, various parts of the plant (e.g. leave, fruit and root) are widely used in Asian countries for centuries to treat different types of diseases and ailments such as hypertension, diabetes, joint aches, muscle pain, coughs, influenza, toothaches and rheumatism. Scientific findings also demonstrated different pharmacological actions of various parts of P. sarmentosum such as adulticidal, antitermite, antioxidant, antifungal, antituberclosis, antiplasmoid, antimalarial, hypoglycemia, antiinflammatory, antinoceptive, antipyretic, antibacterial, anticancer, antituberculosis, antiangiogenesis, antimicrobial, antifeedant and cytotoxic activities. Different types of phytochemical constituents have been successfully identified and isolated from various parts of P. sarmentosum. Therefore, the information related to the botany, ethnomedicinal uses, phytochemical constituents and pharmacological activities of P. sarmentosum were reviewed here.

Therapeutic effects of dihydroartemisinin and transferrin against glioblastoma

  • Kim, Suk Hee;Kang, Seong Hee;Kang, Bo Sun
    • Nutrition Research and Practice
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    • v.10 no.4
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    • pp.393-397
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    • 2016
  • BACKGROUND/OBJECFTIVES: Artemisinin, a natural product isolated from Gaeddongssuk (artemisia annua L.) and its main active derivative, dihydroartemisinin (DHA), have long been used as antimalarial drugs. Recent studies reported that artemisinin is efficacious for curing diseases, including cancers, and for improving the immune system. Many researchers have shown the therapeutic effects of artemisinin on tumors such as breast cancer, liver cancer and kidney cancer, but there is still insufficient data regarding glioblastoma (GBM). Glioblastoma accounts for 12-15% of brain cancer, and the median survival is less than a year, despite medical treatments such as surgery, radiation therapy, and chemotherapy. In this study, we investigated the anti-cancer effects of DHA and transferrin against glioblastoma (glioblastoma multiforme, GBM). MATERIALS/METHODS: This study was performed through in vitro experiments using C6 cells. The toxicity dependence of DHA and transferrin (TF) on time and concentration was analyzed by MTT assay and cell cycle assay. Observations of cellular morphology were recorded with an optical microscope and color digital camera. The anti-cancer mechanism of DHA and TF against GBM were studied by flow cytometry with Annexin V and caspase 3/7. RESULTS: MTT assay revealed that TF enhanced the cytotoxicity of DHA against C6 cells. An Annexin V immune-precipitation assay showed that the percentages of apoptosis of cells treated with TF, DHA alone, DHA in combination with TF, and the control group were $7.15{\pm}4.15%$, $34.3{\pm}5.15%$, $66.42{\pm}5.98%$, and $1.2{\pm}0.15%$, respectively. The results of the Annexin V assay were consistent with those of the MTT assay. DHA induced apoptosis in C6 cells through DNA damage, and TF enhanced the effects of DHA. CONCLUSION: The results of this study demonstrated that DHA, the derivative of the active ingredient in Gaeddongssuk, is effective against GBM, apparently via inhibition of cancer cell proliferation by a pharmacological effect. The role of transferrin as an allosteric activator in the GBM therapeutic efficacy of DHA was also confirmed.

A Case of Vivax Malaria Complicated by Adult Respiratory Distress Syndrome and Successful Management with Extracorporeal Membrane Oxygenation

  • Lee, Hyun-Jung;Baek, Ji-Hyeon;Chae, Myoung-Hun;Joo, Hoyeon;Lee, Jin-Soo;Chung, Moon-Hyun;Park, Yun-Kyu;Kim, Joung-Teak
    • Parasites, Hosts and Diseases
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    • v.51 no.5
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    • pp.551-555
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    • 2013
  • Complicated malaria is mainly caused by Plasmodium falciparum, but, increasingly, Plasmodium vivax is also being reported as a cause. Since the reemergence of indigenous vivax malaria in 1993, cases of severe malaria have been steadily reported in Korea. Herein, we report a case of vivax malaria complicated by adult respiratory distress syndrome (ARDS) that was successfully managed with extracorporeal membrane oxygenation (ECMO). A 59-year-old man presented at our hospital with fever and abdominal pain, which had persisted for 10 days. On admission, the patient had impaired consciousness, shock, hypoxia and haziness in both lungs, jaundice, thrombocytopenia and disseminated intravascular coagulation, metabolic acidosis, and acute kidney injury. A peripheral blood smear and a rapid diagnostic test verified P. vivax mono-infection. Ten hours after admission, hypoxia became more severe, despite providing maximal ventilatory support. The administration of antimalarial agents, ECMO, and continuous venovenous hemofiltration resulted in an improvement of his vital signs and laboratory findings. He was discharged from the hospital 7 weeks later, without any sequelae.

A relapsed case of imported tertian malaria after a standard course of hydroxychloroquine and primaquine therapy (Hydroxych1oroquine과 primaquine 통상 용량으로 치료한 후 재발한 유입 삼일열 말라리아 1예)

  • 이경주;정문현
    • Parasites, Hosts and Diseases
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    • v.36 no.2
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    • pp.143-146
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    • 1998
  • Resistance of Plcsmodium species to antimalarial agents has become increasingly challenging to the management and prevention of malaria. We experienced an imported case of tertian malaria due to Plasmodum viuax relapsed after a seemingly successful treatment with conventional course of hydroxychloroquine and primaquine. A 35-year-old man developed fever three days after return from India and mainland China. After his illness was diagnosed as tertian malaria, he was managed with hydroxy- chloroquine and then primaquine (primaquine base 15 mg/day for 14 days). Thereafter peripheral blood smears showed no malarial parasites, and there was no relapse of symptom until the 55th post-treatment day, however, six months after the above treatment tertian malaria relapsed. He was managed with the same medications again un malaria did not relapse for 10 months.

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Drug Resistance and in Vitro Susceptibility of Plasmodium falciparum in Thailand during 1988-2003

  • Suwandittakul, Nantana;Chaijaroenkul, Wanna;Harnyuttanakorn, Pongchai;Mungthin, Mathirut;Bangchang, Kesara Na
    • Parasites, Hosts and Diseases
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    • v.47 no.2
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    • pp.139-144
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    • 2009
  • The aim of the present study was to investigate antimalarial drug pressure resulting from the clinical use of different antimalarials in Thailand. The phenotypic diversity of the susceptibility profiles of antimalarials, i.e., chloroquine (CQ), quinine (QN), mefloquine (MQ), and artesunate (ARS) in Plasmodium falciparum isolates collected during the period from 1988 to 2003 were studied. P. falciparum isolates from infected patients were collected from the Thai-Cambodian border area at different time periods (1988-1989, 1991-1992, and 2003), during which 3 different patterns of drug use had been implemented: MQ+sulphadoxine (S)+pyrimethamine (P), MQ alone and MQ+ARS, respectively. The in vitro drug susceptibilities were investigated using a method based on the incorporation of $[^3H]$ hypoxanthine. A total of 50 isolates were tested for susceptibilities to CQ, QN, MQ, and ARS. Of these isolates, 19, 16, and 15 were adapted during the periods 1988-1989, 1991-1993, and 2003, respectively. P. falciparum isolates collected during the 3 periods were resistant to CQ. Sensitivities to MQ declined from 1988 to 2003. In contrast, the parasite was sensitive to QN, and similar sensitivity profile patterns were observed during the 3 time periods. There was a significantly positive but weak correlation between the $IC_{50}$ values of CQ and QN, as well as between the $IC_{50}$, values of QN and MQ. Drug pressure has impact on sensitivity of P. falciparum to MQ. A combination therapy of MQ and ARS is being applied to reduce the parasite resistance, and also increasing the efficacy of the drug.

Chemical Constituents from the Aerial Parts of Vernonia cinerea L. and Their Anti-Inflammatory Activity (베르노니아 시네레아 지상부의 화학 성분 및 항염증 활성)

  • Youn, Ui Joung;Chang, Leng Chee
    • Korean Journal of Medicinal Crop Science
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    • v.24 no.6
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    • pp.437-443
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    • 2016
  • Background: Previous phytochemical studies of whole Vernonia cinerea L. plants have identified sesquiterpene lactones, sterols, and triterpenes, which possess anticancer, antifeedant, and antimalarial activities. However, there are no reports of other types of bioactive metabolites. Therefore, the present study aimed to identify phenolic compounds with anti-inflammatory activity in the aerial parts of the plant. Methods and Results: Compounds were isolated from the aerial parts of V. cinerea using a silica and C-18 gel columns and semi-preparative HPLC instrument, and the structures of the compounds were determined using one- and two- dimension nuclear magnetic resonance spectroscopy and mass spectroscopy. The chloroform soluble extracts and isolated compounds were evaluated for their anti-inflammatory potential based on their ability to inhibit nitric oxide production and $TNF-{\alpha}$ induced $NF-{\kappa}B$ activity. Conclusions: Phytochemical study of the aerial parts of V. cinerea led to the isolation of six phenolic compounds. Compound 1 was a major metabolite, and to the best of our knowledge, compounds 2 - 6 were isolated from V.cinerea for the first time. Among the isolates, compounds 1 and 3 exhibited $TNF-{\alpha}$-induced $NF-{\kappa}B$ activity with $IC_{50}$ values of 7.5 and 11.5 M, respectively, and the inhibitory activity of phenyl propanoid compound 3 on $TNF-{\alpha}$-induced $NF-{\kappa}B$ was evaluated for the first time.