Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
Volume 16, Issue 6
Displaying 1-11 of 11 articles from this issue
Review
  • Bo Zhang, Wenjian Pei, Pingping Cai, Zhixue Wang, Fanghua Qi
    Article type: review-article
    2022 Volume 16 Issue 6 Pages 258-272
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 21, 2022
    JOURNAL FREE ACCESS

    As an indispensable part of Traditional Chinese medicine (TCM), Chinese patent medicines have played an important role in preventing and treating diseases in China. Since they are easy to use, easy to store, and cost-effective, Chinese patent medicines have been generally accepted and widely used in Chinese clinical practice as a vital medical resource. In recent years, as TCM has developed and it has been accepted around the world, many Chinese patent medicine companies have gained international market access and successfully registered several Chinese patent medicines as over-the-counter (OTC) or prescription drugs in regions and countries that primarily use Western medicine such as the EU, Russia, Canada, Singapore, and Vietnam. Moreover, several Chinese patent medicines have been obtained the US Food and Drug Administration (FDA) approval conducting phase II or III clinical trials in the US. The current work has focused on several Chinese patent medicines that have been successfully registered or that have been submitted for registration abroad. Summarized here are recent advances in the efficacy and molecular mechanisms of these Chinese patent medicines to treat respiratory infectious diseases (Lianhua Qingwen capsules, Jinhua Qinggan granules, and Shufeng Jiedu Capsules), cardiovascular and cerebrovascular diseases (Compound Danshen Dripping Pills, Huatuo Zaizao pills, and Tongxinluo Capsules), cancers (a Kanglaite injection and a Shenqi Fuzheng Injection), and gynecological diseases (Guizhi Fuling Capsules). The hope is that this review will contribute to a better understanding of Chinese patent medicines by people around the world.

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Original Article
  • Elyza Aiman Azizah Nur, Keisuke Kobayashi, Satoshi Ohte, Hiroshi Tomod ...
    Article type: research-article
    2022 Volume 16 Issue 6 Pages 273-279
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 01, 2022
    JOURNAL FREE ACCESS

    A cell-based assay was conducted to screen microbial culture broths for potentiators of neutral lipid degradation in Chinese Hamster Ovary K1 cells. A total of 5,363 microbial cultures from fungi and actinomycetes were screened in this assay. Brefeldin A (1) from fungal cultures was found to promote the degradation of triacylglycerol (TG) with an EC50 of 2.6 µM. Beauveriolides I (2), III (3), beauverolides A (4), B (5), and K (6) from fungal cultures showed potentiating effect on cholesteryl ester (CE) degradation with EC50s ranging from 0.02 to 0.13 µM. Among these compounds, 2 and 6 exhibited the strongest activities (EC50, 0.02 µM). From actinomycete cultures, oxohygrolidin (7) (EC50 for TG and CE, > 1.7 and 0.8 µM, respectively) and hygrolidin (8) (EC50 for TG and CE, 0.08 and 0.004 µM, respectively) promoted degradation of CE more preferably than TG.

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  • Hiroshi Hamamoto, Atsushi Miyashita, Koushirou Kamura, Ryo Horie, Kazu ...
    Article type: research-article
    2022 Volume 16 Issue 6 Pages 280-285
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 01, 2022
    JOURNAL FREE ACCESS

    We found the activity of arylsulfatase in the midgut contents of the silkworm, Bombyx mori. We identified a 60-kDa protein that comigrates with the activity on a column chromatography following ammonium sulfate precipitation. Based on its partial amino acid sequence, we searched for its coding gene using Basic Local Alignment Search Tool (BLAST) and identified KWMTBOMO05106. Transcriptional data suggest a specific expression of the gene in middle silk glands. The majority (80%) of arylsulfatase activity was found in the silk glands, concurring the specific transcription in the silk gland. Observing the feeding behaviour of the silkworm, we found that silkworms smear a mucus secretes from the spinneret on the food pellet as they feed on. Arylsulfatase activity was also detected in the food pellet bitten by the silkworm as well as in the gut content. Furthermore, arylsulfatase activity was not detected either in the food pellet and in the gut content when silkworms had obstructed the spinneret. These results suggest that arylsulfatase is secreted from the silk glands and may contribute to digestive function.

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Brief Report
  • Ruquan Wang, Yongliang Li, Jianjun Gao, Yepeng Luan
    Article type: brief-report
    2022 Volume 16 Issue 6 Pages 286-292
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 16, 2022
    JOURNAL FREE ACCESS

    Gemcitabine is widely used in the clinic as a first-line antitumor agent. However, intrinsic and acquired resistance hinders its wide clinical application. In this study, a gemcitabine prodrug nominated as WRQ-2 was designed and synthesized by conjugating gemcitabine with the indole-3-methanol analogue OSU-A9 through a carbamate linkage. WRQ-2 exhibited high cytotoxicity against six cancer cell lines (HeLa, A549, MDA-MB-231, HuH-7, MGC-803, and HCT-116) with IC50 values in low micromolar range. WRQ-2 reversed the resistance of HeLa cells to gemcitabine caused by hENT1 inhibition. Compared to gemcitabine, WRQ-2 induced a higher degree of DNA damage and apoptosis in the presence of hENT1 inhibitor. Our study suggests that compound WRQ-2 is a potential gemcitabine prodrug and worth of further antitumor activity investigation.

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  • Hiroyuki Yamamoto, Chiho Tanaka, Momo Okada, Yoshikazu Sawaguchi, Tosh ...
    Article type: brief-report
    2022 Volume 16 Issue 6 Pages 293-296
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 16, 2022
    JOURNAL FREE ACCESS

    Skin pigmentation is among the defenses against ultraviolet (UV) radiation. During formation of skin pigmentation, melanosomes that are transported to the cell membrane and released are internalized by keratinocytes. We here examined whether vinculin, the origin of actin fibers, is involved in this intracellular transport of melanosomes by using melanocytes with suppressed vinculin expression. Using fluorescence immunostaining, the migration of vinculin to the cell membrane due to exposure to 365-nm LED light was examined. The intracellular distribution of melanosomes after irradiation was weighted toward the pericellular region compared with non-irradiated cells. With the suppression of vinculin expression, the amount of extracellularly released melanin decreased. We conclude that the membrane migration of vinculin after UVA exposure is involved in the intracellular transport of melanosomes.

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Correspondence
  • Fangzhou Dou, Zhenxue Tian, Xu Yang, Jing Li, Ruquan Wang, Jianjun Gao
    2022 Volume 16 Issue 6 Pages 297-299
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: October 28, 2022
    JOURNAL FREE ACCESS

    Adult T-cell leukemia/lymphoma (ATL) is a mature T-cell lymphoma with a poor prognosis. Accumulating trimethylation of histone H3 lysine 27 (H3K27me3) caused by upregulated function of either enhancer of zeste homologue 2 (EZH2) or its homolog EZH1 plays an essential role in the maintenance of transcriptional repression in ATL. Selective inhibition of EZH2 may complementarily induce EZH1 activation, so dual targeting EZH1/2 is a rational strategy in developing potent antitumor agents. Valemetostat is the first dual EZH1/2 inhibitor approved for treatment of aggressive ATL in Japan in September 2022. Several other dual EZH1/2 inhibitors such as HH2853, HM97594, and HM97662 have also demonstrated potential in treating malignant tumors. Dual targeting EZH1/2 may have promising antitumor action in hematological malignancies and solid tumors.

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  • Hao Liao, Jiuxin Qu, Hongzhou Lu
    2022 Volume 16 Issue 6 Pages 300-304
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 18, 2022
    JOURNAL FREE ACCESS

    The 2022 monkeypox outbreak outside Africa is ongoing. Cases have been reported in Hong Kong and Chongqing, China. In order to better prevent and control the potential spread of monkeypox virus in China, the development of sensitive and reliable detection commercial kits is imminent. This correspondence reviews the existing laboratory assays and related technologies for nucleic acid (PCR) and serological assays for the diagnosis of monkeypox virus to provide reference for the management and decision-making departments. Due to the serological cross-reactivity of orthopoxviruses, PCR is the laboratory test of choice to confirm monkeypox virus infection. We recommend a dual-target PCR approach in which one assay targets a conserved sequence of the Orthopoxvirus genus and the other targets a monkeypox virus specific sequence.

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  • Cheng Wang, Liqin Sun, Qian Li, Hongzhou Lu
    2022 Volume 16 Issue 6 Pages 305-308
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 16, 2022
    JOURNAL FREE ACCESS

    Clinical diagnosis of tuberculosis (TB) in people living with the human immunodeficiency virus (HIV) poses a challenge. The Xpert MTB/RIF Ultra (Ultra) has displayed greater sensitivity at diagnosing tuberculosis and rifampicin resistance compared to the Xpert MTB/RIF (Xpert). However, whether Ultra is able to facilitate an auxiliary diagnosis of TB in patients with an HIV-TB co-infection remains unclear. Accordingly, the current study evaluated the use of Ultra in patients with an HIV-TB co-infection by summarizing relevant studies. The sensitivity and specificity of Ultra and Xpert at diagnosing patients with an HIV-TB co-infection have been summarized and compared. The performance of Ultra in diagnosing extrapulmonary tuberculosis was also summarized. Although a large-cohort, multi-center study needs to be conducted to assess Ultra's ability to detect TB in AIDS patients in the future, the current evidence supports the use of Ultra for the assessment of patients with an HIV-TB co-infection.

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  • Hiroki Iwata, Keisuke Nakamura, Noriko Kobayashi, Kazuko Fujimoto, Nao ...
    2022 Volume 16 Issue 6 Pages 309-312
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 19, 2022
    JOURNAL FREE ACCESS

    Community pharmacies are required to play a role in maintaining the health of local residents. Since September 2015, a national policy in Japan has allowed saliva tests to be used for oral health check-ups at community pharmacies. In the present study, we aimed to reveal dentists' perceptions and expectations for oral health check-ups provided at community pharmacies. A questionnaire survey was administered to dentists at 1,000 randomly selected dental clinics in Tokyo, Japan; 257 responses (25.7%) were included in the analysis and 85.2% of respondents approved of oral health check-ups at community pharmacies. Most respondents who approved of oral health check-ups expected that community pharmacists would recommend that local residents visit a dental clinic (85.8%) and provide a report to dentists (60.3%) after the check-up. Furthermore, 79.0% of respondents desired collaboration with community pharmacies. These findings suggested the potential for oral health check-ups to facilitate collaboration between community pharmacies and dental clinics aimed at maintaining and improving oral health of local residents.

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Letter
  • Yuesi Zhong, Manhang Cai, Zaomao Zhong, Yi Zhang, Meihai Deng, Nan Lin
    Article type: letter
    2022 Volume 16 Issue 6 Pages 313-315
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: December 18, 2022
    JOURNAL FREE ACCESS

    Cholestasis and obstructive jaundice can be extrahepatic or intrahepatic. Here we present one case with calculous cholecystitis who presenting with repeated obstructive jaundice and without bile duct dilation. The patient received laparoscopic cholecystectomy, and cystohepatic duct was identified intraoperatively, there was no cholestasis or obstructive jaundice postoperatively. Cystohepatic duct is a rare biliary anomaly observed in 0.7% of all surgical cases and in 1.5% of all cadaveric dissections. The cystohepatic duct can be the bridge of calculous cholecystitis complicating cholangitis and obstructive jaundice, here we for the first time presented this entity.

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  • Kenji Karako
    Article type: letter
    2022 Volume 16 Issue 6 Pages 316-317
    Published: December 25, 2022
    Released on J-STAGE: December 26, 2022
    Advance online publication: September 06, 2022
    JOURNAL FREE ACCESS

    Japan is facing the largest outbreak of COVID-19 in history in 2022. The number of new infections per day surpassed 200,000 for the first time in July and peaked in August. Japan has required the reporting of information on all infected persons, but maintaining this system is difficult. Starting in September 2, 2022, four prefectures have implemented a trial policy to limit the infected that must be reported in order to reduce the burden on medical personnel. The policy obliges medical facilities to report only people with a high-risk infection, but the number of the infected will continue to be counted regardless of whether they have a high-risk or low-risk infection. More prefectures are expected to adopt this policy in the future.

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