Parasites, Hosts and Diseases

"in vivo"

Original Article

Evaluating the activity of N-89 as an oral antimalarial drug: Nagwa S. M. Aly, Hiroaki Matsumori, Thi Quyen Dinh, Akira Sato, Shin-ichi Miyoshi, Kyung-Soo Chang, Hak Sun Yu, Takaaki Kubota, Yuji Kurosaki, Duc Tuan Cao, Gehan A. Rashed, Hye-Sook Kim; Parasites Hosts Dis 2023;61(3):282-291.
Published online August 21, 2023; DOI: https://doi.org/10.3347/PHD.23044

Abstract
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Despite the recent progress in public health measures, malaria remains a troublesome disease that needs to be eradicated. It is essential to develop new antimalarial medications that are reliable and secure. This report evaluated the pharmacokinetics and antimalarial activity of 1,2,6,7-tetraoxaspiro[7.11]nonadecane (N-89) using the rodent malaria parasite Plasmodium berghei in vivo. After a single oral dose (75 mg /kg) of N-89, its pharmacokinetic parameters were measured, and t_1/2 was 0.97 h, T_max was 0.75 h, and bioavailability was 7.01%. A plasma concentration of 8.1 ng/ml of N-89 was maintained for 8 h but could not be detected at 10 h. The dose inhibiting 50% of parasite growth (ED₅₀) and ED₉₀ values of oral N-89 obtained following a 4-day suppressive test were 20 and 40 mg/kg, respectively. Based on the plasma concentration of N-89, we evaluated the antimalarial activity and cure effects of oral N-89 at a dose of 75 mg/kg 3 times daily for 3 consecutive days in mice harboring more than 0.5% parasitemia. In all the N-89- treated groups, the parasites were eliminated on day 5 post-treatment, and all mice recovered without a parasite recurrence for 30 days. Additionally, administering oral N-89 at a low dose of 50 mg/kg was sufficient to cure mice from day 6 without parasite recurrence. This work was the first to investigate the pharmacokinetic characteristics and antimalarial activity of N-89 as an oral drug. In the future, the following steps should be focused on developing N-89 for malaria treatments; its administration schedule and metabolic pathways should be investigated.

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The antimalarial activity of transdermal N-89 mediated by inhibiting ERC gene expression in P. Berghei-infected mice
Hiroaki Matsumori, Thi Quyen Dinh, Shin-ichi Miyoshi, Masayuki Morita, Hye-Sook Kim
Parasitology International.2025; 106: 103026. CrossRef
Evaluating the effect of new antimalarial N-89 for gametocytes in P. berghei-infected mice
Thi Quyen Dinh, Hiroaki Matsumori, Mamoru Niikura, Shin-ichi Miyoshi, Hye-Sook Kim
Parasitology International.2025; 109: 103093. CrossRef

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Brief Communication

Evaluation of the anti-Toxoplasma gondii Activity of Hederagenin in vitro and in vivo: Run-Hui Zhang, Runhao Jin, Hao Deng, Qing-Kun Shen, Zhe-Shan Quan, Chun-Mei Jin; Korean J Parasitol 2021;59(3):297-301.
Published online June 21, 2021; DOI: https://doi.org/10.3347/kjp.2021.59.3.297

Abstract
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Toxoplasma gondii infection is widespread worldwide, not only posing a serious threat to human food safety and animal husbandry, but also endangering human health. The selectivity index was employed to measure anti-T. gondii activity. Hederagenin (HE) exhibited potent anti-T. gondii activity and low cytotoxicity. For this reason, HE was selected for in vivo experiments. HE showed 64.8%±13.1% inhibition for peritoneal tachyzoites in mice, higher than spiramycin 56.8%±6.0%. Biochemical parameters such as alanine aminotransferase, aspartate aminotransferase, glutathione, and malondialdehyde, illustrated that HE was a good inhibitor of T. gondii in vivo. This compound was also effective in relieving T. gondii-induced liver damage. Collectively, it was demonstrated that HE had potential as an anti-T. gondii agent.

Citations

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An updated review of the pharmacological effects and potential mechanisms of hederagenin and its derivatives
Huize Zhang, Yong Li, Yi Liu
Frontiers in Pharmacology.2024;[Epub] CrossRef
Comprehensive Insights into the Development of Antitoxoplasmosis Drugs: Current Advances, Obstacles, and Future Perspectives
Siyang Liu, Minghao Cai, Zhendi Liu, Weixin Gao, Junjie Li, Yuxueqing Li, Xiayire Abudouxukuer, Jili Zhang
Journal of Medicinal Chemistry.2024; 67(23): 20740. CrossRef
Sulfadiazine analogs: anti-Toxoplasma in vitro study of sulfonamide triazoles
Fadwa M Arafa, Doaa Hassan Osman, Mona Mohamed Tolba, Nadjet Rezki, Mohamed R Aouad, Mohamed Hagar, Mervat Osman, Heba Said
Parasitology Research.2023; 122(10): 2353. CrossRef
Synthesis and evaluation of in vitro and in vivo anti -Toxoplasma gondii activity of tetraoxane-substituted ursolic acid derivatives
Ya-Lan Wang, Li-Li Jin, Xu Cheng, Wei-Feng Yan, Hao Deng, Qing-Kun Shen, Zhe-Shan Quan, Chun-Mei Jin, Chang-Hao Zhang
Natural Product Research.2023; 37(21): 3654. CrossRef
Pharmacological overview of hederagenin and its derivatives
Xing Huang, Qing-Kun Shen, Hong-Yan Guo, Xiaoting Li, Zhe-Shan Quan
RSC Medicinal Chemistry.2023; 14(10): 1858. CrossRef
Synthesis and Antitumor Activity of Hederagenin Derivatives
Xing Huang, Changhao Zhang, Hao Deng, Qingkun Shen, Hongyan Guo, Zheshan Quan, Zhiyong Li, Lili Jin
Chinese Journal of Organic Chemistry.2022; 42(9): 2877. CrossRef

4,727 View
106 Download
8 Web of Science
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Original Article

Construction of In Vivo Fluorescent Imaging of Echinococcus granulosus in a Mouse Model: Sibo Wang, Tao Yang, Xuyong Zhang, Jie Xia, Jun Guo, Xiaoyi Wang, Jixue Hou, Hongwei Zhang, Xueling Chen, Xiangwei Wu; Korean J Parasitol 2016;54(3):291-299.
Published online June 30, 2016; DOI: https://doi.org/10.3347/kjp.2016.54.3.291

Abstract
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Human hydatid disease (cystic echinococcosis, CE) is a chronic parasitic infection caused by the larval stage of the cestode Echinococcus granulosus. As the disease mainly affects the liver, approximately 70% of all identified CE cases are detected in this organ. Optical molecular imaging (OMI), a noninvasive imaging technique, has never been used in vivo with the specific molecular markers of CE. Thus, we aimed to construct an in vivo fluorescent imaging mouse model of CE to locate and quantify the presence of the parasites within the liver noninvasively. Drug-treated protoscolices were monitored after marking by JC-1 dye in in vitro and in vivo studies. This work describes for the first time the successful construction of an in vivo model of E. granulosus in a small living experimental animal to achieve dynamic monitoring and observation of multiple time points of the infection course. Using this model, we quantified and analyzed labeled protoscolices based on the intensities of their red and green fluorescence. Interestingly, the ratio of red to green fluorescence intensity not only revealed the location of protoscolices but also determined the viability of the parasites in vivo and in vivo tests. The noninvasive imaging model proposed in this work will be further studied for long-term detection and observation and may potentially be widely utilized in susceptibility testing and therapeutic effect evaluation.

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Dihydroartemisinin-sodium taurocholate-PLGA nanoparticles: a novel therapeutic approach against cystic echinococcosis
Aierpati Moheteer, Jiang Zhu, Dongming Pang, Xue Rao, Nijiati Aini, Kalibixiati Aimulajiang, Zhenping Zhang, Saifuding Abula, Adelijiang Wusiman
Frontiers in Pharmacology.2025;[Epub] CrossRef
Imaging as a (pre)clinical tool in parasitology
Clarize Maria de Korne, Lisette van Lieshout, Fijs Willem Bernhard van Leeuwen, Meta Roestenberg
Trends in Parasitology.2023; 39(3): 212. CrossRef
Autoimmunity in human CE: Correlative with the fertility status of the CE cyst
E. A. EL Saftawy, A. Abdelraouf, M. A. Elsalam, P. Zakareya, A. Fouad, E. A. Albadawi, A. H. S. Abobakr Ali, N. M. Amin
Helminthologia.2022; 59(1): 1. CrossRef
Small animal in vivo imaging of parasitic infections: A systematic review
Adam Novobilský, Johan Höglund
Experimental Parasitology.2020; 214: 107905. CrossRef
Lethal effects of gold nanoparticles on protoscolices of hydatid cyst: in vitro study
Sara Napooni, Mohsen Arbabi, Mahdi Delavari, Hossein Hooshyar, Sima Rasti
Comparative Clinical Pathology.2019; 28(1): 143. CrossRef
Combination of TiO2 nanoparticles and Echinometra mathaeis gonad extracts: In vitro and in vivo scolicidal activity against hydatid cysts
Azita Navvabi, Ahmad Homaei, Shahram Khademvatan, Mohammad Hassan Khadem Ansari, Mousa Keshavarz
Biocatalysis and Agricultural Biotechnology.2019; 22: 101432. CrossRef
Macrophage Activation and Functions during Helminth Infection: Recent Advances from the Laboratory Mouse
Marion Rolot, Benjamin G. Dewals
Journal of Immunology Research.2018; 2018: 1. CrossRef
Improved experimental model of hepatic cystic hydatid disease resembling natural infection route with stable growing dynamics and immune reaction
Rui-Qing Zhang, Xin-Hua Chen, Hao Wen
World Journal of Gastroenterology.2017; 23(45): 7989. CrossRef

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Brief Communication

A Rapid and Convenient Method for in Vivo Fluorescent Imaging of Protoscolices of Echinococcus multilocularis: Tao Yang, Sibo Wang, Xuyong Zhang, Jie Xia, Jun Guo, Jixue Hou, Hongwei Zhang, Xueling Chen, Xiangwei Wu; Korean J Parasitol 2016;54(2):225-231.
Published online April 30, 2016; DOI: https://doi.org/10.3347/kjp.2016.54.2.225

Abstract
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Human and animal alveolar echinococcosis (AE) are important helminth infections endemic in wide areas of the Northern hemisphere. Monitoring Echinococcus multilocularis viability and spread using real-time fluorescent imaging in vivo provides a fast method to evaluate the load of parasite. Here, we generated a kind of fluorescent protoscolices in vivo imaging model and utilized this model to assess the activity against E. multilocularis protoscolices of metformin (Met). Results indicated that JC-1 tagged E. multilocularis can be reliably and confidently used to monitor protoscolices in vitro and in vivo. The availability of this transient in vivo fluorescent imaging of E. multilocularis protoscolices constitutes an important step toward the long term bio-imaging research of the AE-infected mouse models. In addition, this will be of great interest for further research on infection strategies and development of drugs and vaccines against E. multilocularis and other cestodes.

Citations

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NIR-II fluorescence microscopic bioimaging for intrahepatic angiography and the early detection of Echinococcus multilocularis microlesions
Nuernisha Alifu, Ting Yan, Jun Li, Lijun Zhu, Abudusalamu Aini, Siyiti Amuti, Juan Wu, Wenjing Qi, Gang Guo, Wenbao Zhang, Xueliang Zhang
Frontiers in Bioengineering and Biotechnology.2023;[Epub] CrossRef
In Vitro and In Vivo Efficacy of Albendazole Chitosan Microspheres with Intensity-Modulated Radiation Therapy in the Treatment of Spinal Echinococcosis
Sibo Wang, Shan Wang, Weishan Wang, Yi Dai, Zhongpeng Qiu, Wei Ke, Minghao Geng, Jing Li, Ke Li, Qingyuan Ma, Feng Li
Antimicrobial Agents and Chemotherapy.2021;[Epub] CrossRef
Small animal in vivo imaging of parasitic infections: A systematic review
Adam Novobilský, Johan Höglund
Experimental Parasitology.2020; 214: 107905. CrossRef

8,485 View
89 Download
3 Web of Science
Crossref

Original Article

Sensitivity of Plasmodium falciparum to Antimalarial Drugs in Hainan Island, China: Shan-Qing Wang, Guang-Ze Wang, Yu-Chun Li, Feng Meng, Shi-Gan Lin, Zhen-Hu Zhu, Ding-Wei Sun, Chang-Hua He, Xi-Min Hu, Jian-Wei Du; Korean J Parasitol 2015;53(1):35-41.
Published online February 27, 2015; DOI: https://doi.org/10.3347/kjp.2015.53.1.35

Abstract
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Pyronaridine and artesunate have been shown to be effective in falciparum malaria treatment. However, pyronaridine is rarely used in Hainan Island clinically, and artesunate is not widely used as a therapeutic agent. Instead, conventional antimalarial drugs, chloroquine and piperaquine, are used, explaining the emergence of chloroquine-resistant Plasmodium falciparum. In this article, we investigated the sensitivity of P. falciparum to antimalarial drugs used in Hainan Island for rational drug therapy. We performed in vivo (28 days) and in vitro tests to determine the sensitivity of P. falciparum to antimalarial drugs. Total 46 patients with falciparum malaria were treated with dihydroartemisinin/piperaquine phosphate (DUO-COTECXIN) and followed up for 28 day. The cure rate was 97.8%. The mean fever clearance time (22.5±10.6 hr) and the mean parasite clearance time (27.3±12.2 hr) showed no statistical significance with different genders, ages, temperatures, or parasite density (P>0.05). The resistance rates of chloroquine, piperaquine, pyronarididine, and artesunate detected in vitro were 71.9%, 40.6%, 12.5%, and 0%, respectively (P<0.0001). The resistance intensities decreased as follows: chloroquine>piperaquine>pyronarididine>artesunate. The inhibitory dose 50 (IC₅₀) was 3.77×10^-6 mol/L, 2.09×10^-6 mol/L, 0.09×10^-6 mol/L, and 0.05×10^-6 mol/L, and the mean concentrations for complete inhibition (CIMC) of schizont formation were 5.60×10^-6 mol/L, 9.26×10^-6 mol/L, 0.55×10^-6 mol/L, and 0.07×10^-6 mol/L, respectively. Dihydroartemisinin showed a strong therapeutic effect against falciparum malaria with a low toxicity.

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Evaluation Algorithm of Volleyball Players’ Competitive Ability Based on the Random Matrix Model
Tailin Wang, Hua Zheng, Fangshu Li, Nian Jia, Zengliang Cai, Ning Cao
Mathematical Problems in Engineering.2022; 2022: 1. CrossRef