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Oral cavity: An open horizon for nanopharmaceuticals
Nguyen Oanh Oanh Thi,Tran Khue Dan,Ha Nhan Thi,Doan Sang Minh,Dinh Thi Thanh Hai,Tran Tuan Hiep 한국약제학회 2021 Journal of Pharmaceutical Investigation Vol.51 No.4
Background Oral administration is the primary route employed for drug delivery. In addition to the gastrointestinal tract, the oral cavity has been drawing considerable attention owing to its physiological properties and advances in drug carrier development. Notably, nanotechnology has made immense contributions to enhancing drug bioavailability, stability, and efficacy, both in research and clinical settings. Area covered The present review comprises lessons from physiological characteristics to fundamental material science knowledge, summarizing the pros and cons of nanotechnology applications in therapeutic drug delivery. The oral cavity presents inherent challenges, including oral cancer, dental caries, oral infection, or oral inflammation, that necessitate local solutions. Simultaneously, the vascular system under the tongue and in the buccal region offers a portal for systemic drug absorption. Expert opinion Among available delivery systems, nanoparticle-based drug delivery, with the oral cavity as the action or absorption site, can be developed as a principal dosage formulation. Although convenience and fast onset might be advantageous, additional studies are warranted for preclinical characterization, especially in animal models, and for determining manufacturing competence, prior to human trials to meet standards in clinical settings.
Hoang Thai Hoa,Nguyen Thi Thu,Nguyen Thuong Dong,Tran Thi Oanh,Tran Thi Hien,Do Thi Ha 한국생약학회 2020 Natural Product Sciences Vol.26 No.3
The ability of the total extract from Physalis angulata; three fractions after partitioning with n-hexane, ethyl acetate (TBE), and water; and four withanolides (compounds 1 – 4) to phosphorylate 5'-adenosine monophosphate-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC) in HepG2 cells was evaluated. The TBE fraction (50 μg/mL) activated p-ACC and p-AMPK expression most strongly. Compounds 1 – 4 (10 μM) upregulated p-ACC expression at different levels. Compound 4 induced the most significant changes in p-AMPK expression, followed by 1 and 2. Sterol regulatory element-binding proteins (SREBPs) play a functional role in the transcriptional regulation of the lipogenic pathway, including fatty acid synthase (FAS) and ACC. The effects of compounds 2 and 4 (10 μM) on FAS and SREBP-1c expression under high glucose conditions (30 mM) in HepG2 cells were evaluated further. Both dose-dependently inhibited FAS and SREBP-1c expression as well as lipid accumulation (1 – 10 μM) were compared to high-concentration glucose control, which upregulated FAS and SREBP-1c. These results suggest that compounds 2 and 4 upregulate AMPK, suppress FAS and SREBP-1c, and have potential effects on glucose and lipid metabolism.
Nguyen Phuong Thao,이영숙,Bui Thi Thuy Luyen,Ha Van Oanh,Irshad Ali,Madeeha Arooj,고영상,양서영,김영호 한국생약학회 2018 Natural Product Sciences Vol.24 No.3
Inflammation is a biological response caused by overactivation of the immune system and is controlled by immune cells via a variety of cytokines. The overproduction of pro-inflammatory cytokines enhances abnormal host immunity, resulting in diseases such as rheumatoid arthritis, cardiovascular disease, Alzheimer's disease, and cancer. Inhibiting the production of pro-inflammatory cytokines such as interleukin (IL)-12p40, IL-6, and tumor necrosis factor (TNF)-a might be one way to treat these conditions. Here, we investigated the anti-inflammatory activity of compounds isolated from Cimicifuga dahurica (Turcz.) Maxim., which is traditionally used as an antipyretic and analgesic in Korea. In primary cell culture assays, 12 compounds were found to inhibit the production of pro-inflammatory cytokines (IL-12p40, IL-6, and TNF-a) in vitro in bone marrow-derived dendritic cells stimulated with LPS.
Kim, Jang Hoon,Thao, Nguyen Phuong,Han, Yoo Kyong,Lee, Young Suk,Luyen, Bui Thi Thuy,Oanh, Ha Van,Kim, Young Ho,Yang, Seo Young TaylorFrancis 2018 Journal of enzyme inhibition and medicinal chemist Vol.33 No.1
<P><B>Abstract</B></P><P>Cholinesterases (ChEs) are enzymes that break down neurotransmitters associated with cognitive function and memory. We isolated cinnamic acids (<B>1</B> and <B>2</B>), indolinones (<B>3</B> and <B>4</B>), and cycloartane triterpenoid derivatives (<B>5</B>–<B>19</B>) from the roots of <I>Cimicifuga dahurica</I> (Turcz.) Maxim. by chromatography. These compounds were evaluated for their inhibitory activity toward ChEs. Compound <B>1</B> was determined to have an IC<SUB>50</SUB> value of 16.7 ± 1.9 μM, and to act as a competitive inhibitor of acetylcholinesterase (AChE). Compounds <B>3</B>, <B>4</B> and <B>14</B> were found to be noncompetitive with IC<SUB>50</SUB> values of 13.8 ± 1.5 and 6.5 ± 2.5 μM, and competitive with an IC<SUB>50</SUB> value of 22.6 ± 0.4 μM, respectively, against butyrylcholinesterase (BuChE). Our molecular simulation suggested each key amino acid, Tyr337 of AChE and Asn228 of BuChE, which were corresponded with potential inhibitors <B>1</B>, and <B>3</B> and <B>4</B>, respectively. Compounds <B>1</B> and <B>4</B> were revealed to be promising compounds for inhibition of AChEs and BuChEs, respectively.</P>