School of Integrated Traditional Chinese and Western Medicine, Binzhou Medical University, Yantai 264003, China.
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
Molecules. 2018 Aug 27;23(9):2158. doi: 10.3390/molecules23092158.
Deoxyschizandrin (DS) is a bioactive benzocyclooctadiene lignan found in the fruit of . However, poor bioavailability and non-specificity of DS frequently caused low therapeutic efficacy. In the present study, DS-liposome (DS-lipo) was implemented to enhance the hepatic targeting and inhibition effects on adipocyte differentiation in 3T3-L1 cells. The formulations enabled encapsulation of as much as 24.14% DS. The DS-lipo prepared was about 73.08 nm, as measured by laser light scattering (LLS) morphology. In the visual field of a scanning electron microscope (SEM), the liposomes were spherical with similar size and uniform dispersion. Fluorescence live imaging study exhibited hepatic targeting of liposomes in vivo. Furthermore, High-Content Analysis (HCS) imaging microassay analyses revealed DS-lipo and DS reduced cytoplasmic lipid droplet in 3T3-L1 adipocytes, with the IC value of 8.68 μM and 31.08 μM, respectively. The lipid droplet accumulation inhibition rate of 10 μM DS-lipo was above 90%, which was even superior to the effect of 30 μM DS solution. The current findings suggest that DS-lipo was a therapeutic strategy for alleviating lipid-associated diseases and nonalcoholic fatty liver disease (NAFLD).
五味子甲素（DS）是一种生物活性苯丙素类木脂素，存在于五味子果实中。然而，DS 的生物利用度差且特异性低，常导致治疗效果低。在本研究中，采用 DS-脂质体（DS-lipo）提高 DS 的肝靶向性，并抑制 3T3-L1 细胞中的脂肪细胞分化。该制剂可将多达 24.14%的 DS 包封。通过激光光散射（LLS）形态学测量，制备的 DS-lipo 的直径约为 73.08nm。在扫描电子显微镜（SEM）的视野中，脂质体呈球形，具有相似的大小和均匀的分散性。荧光活体成像研究显示了脂质体在体内的肝靶向性。此外，高内涵分析（HCS）成像微分析表明，DS-lipo 和 DS 降低了 3T3-L1 脂肪细胞中的细胞质脂滴，其 IC 值分别为 8.68 μM 和 31.08 μM。10 μM DS-lipo 的脂滴积累抑制率超过 90%，甚至优于 30 μM DS 溶液的效果。目前的研究结果表明，DS-lipo 是一种治疗与脂质相关疾病和非酒精性脂肪肝（NAFLD）的策略。
