著者
Kosuke Shimizu Miki Takada Tomohiro Asai Kenji Irimura Kazuhiko Baba Naoto Oku
出版者
The Pharmaceutical Society of Japan
雑誌
Biological and Pharmaceutical Bulletin (ISSN:09186158)
巻号頁・発行日
vol.25, no.6, pp.783-786, 2002 (Released:2002-06-01)
参考文献数
19
被引用文献数
10 13

To enhance the therapeutic efficacy as well as to reduce the side effect, we attempted to liposomalize 4β-aminoalkyl-4′-O-demethyl-4-desoxypodophyllotoxin (TOP-53), a novel and effective topoisomerase II inhibitor. More than 90% of TOP-53 was efficiently incorporated into the liposomes composed of dipalmitoylphosphatidylcholine and cholesterol by remote-loading method. Anti-tumor activity of liposomal TOP-53 against solid tumor was examined in vivo using colon26 NL-17 carcinoma model mice. Three doses of liposomal TOP-53 (12 mg/kg/dose) showed significant tumor growth suppression (97.5% reduction determined at day 25) and the increase in life span (33%) of tumor-bearing mice. Furthermore, one mouse out of 5 was completely cured after treatment. Since similar efficacy was observed in the free TOP-53 treated group, liposomalization does not contribute much to the enhancement of therapeutic efficacy. However, a slight but measurable damage at the injection site was observed when free TOP-53 was injected, and the damage was diminished by the liposomalization. Taken together, liposomalization reduces the side effect rather than enhancing the therapeutic efficacy when TOP-53 is used.
著者
Kosuke SHIMIZU Taizo SUZUKI Keisuke KAMEYAMA
出版者
The Institute of Electronics, Information and Communication Engineers
雑誌
IEICE Transactions on Fundamentals of Electronics, Communications and Computer Sciences (ISSN:09168508)
巻号頁・発行日
vol.E101.A, no.11, pp.1815-1822, 2018-11-01 (Released:2018-11-01)
参考文献数
24
被引用文献数
1

We propose the cube-based perceptual encryption (C-PE), which consists of cube scrambling, cube rotation, cube negative/positive transformation, and cube color component shuffling, and describe its application to the encryption-then-compression (ETC) system of Motion JPEG (MJPEG). Especially, cube rotation replaces the blocks in the original frames with ones in not only the other frames but also the depth-wise cube sides (spatiotemporal sides) unlike conventional block-based perceptual encryption (B-PE). Since it makes intra-block observation more difficult and prevents unauthorized decryption from only a single frame, it is more robust than B-PE against attack methods without any decryption key. However, because the encrypted frames including the blocks from the spatiotemporal sides affect the MJPEG compression performance slightly, we also devise a version of C-PE with no spatiotemporal sides (NSS-C-PE) that hardly affects compression performance. C-PE makes the encrypted video sequence robust against the only single frame-based algorithmic brute force (ABF) attack with only 21 cubes. The experimental results show the compression efficiency and encryption robustness of the C-PE/NSS-C-PE-based ETC system. C-PE-based ETC system shows mixed results depending on videos, whereas NSS-C-PE-based ETC system shows that the BD-PSNR can be suppressed to about -0.03dB not depending on videos.
著者
Kosuke Shimizu Miki Takada Tomohiro Asai Koichi Kuromi Kazuhiko Baba Naoto Oku
出版者
The Pharmaceutical Society of Japan
雑誌
Biological and Pharmaceutical Bulletin (ISSN:09186158)
巻号頁・発行日
vol.25, no.10, pp.1385-1387, 2002 (Released:2002-10-01)
参考文献数
19
被引用文献数
6 8

A novel anti-tumor agent, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride (TAS-103), effectively inhibits both topoisomerase I and II activities. To enhance anti-tumor efficacy and to reduce the side effects of the agent, liposomalization of TAS-103 was performed. TAS-103 was effectively entrapped in liposomes by a remote-loading method, and was stable at 4 °C and in the presence of 50% serum. To evaluate the anti-tumor efficacy of liposomal TAS-103, the growth inhibition against Lewis lung carcinoma cells in vitro and the therapeutic efficacy against solid tumor-bearing mice in vivo were examined. Liposomal TAS-103 showed strong cytotoxic effect against Lewis lung carcinoma cells in a dose dependent manner and effectively suppressed solid tumor growth accompanying longer survival time of tumor-bearing mice in comparison with the mice treated with free TAS-103. These results suggest that liposomal TAS-103 is useful for cancer therapy.