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1.
Biosci Biotechnol Biochem ; 87(12): 1523-1531, 2023 Nov 21.
Article in English | MEDLINE | ID: mdl-37709570

ABSTRACT

We focused on Piper longum L., a herbal drug produced in Myanmar, which has a renoprotective effect. Thus, we attempted to isolate and identify compounds that enhance the expression of the ABCG2 gene from the aerial parts of the plant except for the fruit. Among the various P. longum extracts, we isolated and identified the components. Using Caco-2 cells, the hABCG2 mRNA expression-enhancing effects of the isolated compounds were compared with the positive reference compound (3-methylcholanthrene [3MC]) using real-time polymerase chain reaction. Six compounds were isolated and identified from the methanol extract of P. longum. Among the isolated compounds, licarin A and neopomatene had lower toxicity and higher hABCG2 mRNA expression-enhancing effects in Caco-2 cells. Suppression of hAhR expression by siRNA reduced the activity of licarin A and neopomatene, as well as the hAhR agonist 3MC, suggesting that these 2 compounds may act as hAhR agonists to promote hABCG2 expression.


Subject(s)
Lignans , Piper , Humans , Plant Extracts/pharmacology , Caco-2 Cells , Lignans/pharmacology , Gene Expression , RNA, Messenger/genetics , ATP Binding Cassette Transporter, Subfamily G, Member 2/genetics , Neoplasm Proteins
2.
Virusdisease ; 32(3): 446-466, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34631974

ABSTRACT

Hepatitis B is one of the major burdens for health services and is the leading cause of morbidity and mortality from cirrhosis of liver and hepatocellular carcinoma. Current treatment strategies using nucleos(t)ide analogue reverse-transcriptase inhibitors or interferons are targeted for the long-term suppression of hepatitis B DNA. However, functional cure of hepatitis B infection (HBsAg clearance) was difficult to attain with such treatments. Therefore, new treatment strategies or innovative treatments are urgently needed. The new treatments should focus on the potential therapeutic targets such as covalently closed circular DNA which may be important for the HBsAg clearance. Plant based medicines have been used in different traditional medicine practices and these natural products/compounds serve as a good source of information or clues for use in drug discovery and design. Many natural products were found to be effective against hepatitis B virus and some even have better therapeutic activities than currently used compounds. This review summarizes the current evidence of Myanmar medicinal plants in basic and clinical research which shows promising potential for the development of novel therapeutic agents for the treatment of hepatitis B.

3.
Chem Biodivers ; 18(7): e2100243, 2021 Jul.
Article in English | MEDLINE | ID: mdl-34128328

ABSTRACT

Non-alcoholic fatty liver disease (NAFLD) is currently the most common chronic liver disease in the world, with a prevalence of 25 % in many countries. To date, no drug has been approved to treat NAFLD, therefore, the use of phytochemicals to prevent this disease is meaningful. In this study, we focused on the effects of Moringa oleifera Lam. on diabetes, attempted to isolate compounds that regulate NAFLD. Compounds 1 and 2 were isolated from the ethyl acetate fraction of M. oleifera. Spectral data revealed that they were 1-hydroxy-3-phenylpropan-2-yl benzoate (1) and benzyl benzylcarbamate (2), respectively. The three-dimensional structure of compound 1 was determined by single crystal X-ray structural analysis. Neither compound was toxic to HepG2 cells, and compound 1 was found to have a concentration-dependent inhibitory effect on intracellular lipid accumulation induced by stimulation of linoleic acid (LA). As a result of measuring the effects of compound 1 on the intracellular lipid production-related protein, it was found that compound 1 enhanced protein expression that promotes lipolysis. On the other hand, since the action of compound 1 was similar to that of PPARα agonists, it is deduced that compound 1 enhanced the activity of PPARα and further enhanced the expression of lipolytic proteins, which is related to the suppression of intracellular lipid accumulation. Furthermore, as the result of docking simulation, compound 1 had a higher binding affinity to the ligand binding site of PPARα than fenofibrate, which is a PPARα agonist, and thus compound 1 was considered to be promising as an agonist of PPARα.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Moringa oleifera/chemistry , Non-alcoholic Fatty Liver Disease/drug therapy , Plant Extracts/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Proliferation/drug effects , Cell Survival/drug effects , Density Functional Theory , Drug Screening Assays, Antitumor , Hep G2 Cells , Humans , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Tumor Cells, Cultured
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