Identification of bioactive heterocyclic compounds from mulberry and their protective effect against streptozotocin-induced apoptosis in INS-1 cells

Song, Ji Hoon; Lee, Dahae; Lee, Seoung Rak; Yu, Jae Sik; Jang, Tae Su; Nam, Joo‐Won; Kim, Ki‐Hyun; Kang, Ki Sung

doi:10.3892/mmr.2018.8582

Cited by 5 publications

(6 citation statements)

References 26 publications

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“…These findings are inconsistent with previous findings on STZ treated INS-1 cells. On the other hand, treating the INS-1 cells with 2.5 and 5 µM of CA acid reversed the STZ effect and protected against apoptosis [ 34 ].…”

Section: Discussionmentioning

confidence: 99%

Carnosic Acid Protects INS-1 β-Cells against Streptozotocin-Induced Damage by Inhibiting Apoptosis and Improving Insulin Secretion and Glucose Uptake

et al. 2022

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Carnosic acid (CA), a natural polyphenolic diterpene derived from Rosmarinus officinalis, has been proven to possess a broad spectrum of medicinal properties. Nevertheless, no studies on its impact on pancreatic β-cells have been conducted to date. Herein, clonal rat INS-1 (832/13) cells were pretreated with CA for 24 h and then incubated with streptozotocin (STZ) for 3 h. Several functional experiments were performed to determine the effect of CA on STZ-induced pancreatic β-cell damage, including cell viability assay, apoptosis analysis, and measurement of the level of insulin secretion, glucose uptake, malondialdehyde (MDA), reactive oxygen species (ROS), and proteins expression. STZ treatment decreased cell survival, insulin secretion, glucose uptake, and increased apoptosis, MDA, and ROS production in INS-1 cells. Furthermore, protein expression/phosphorylation analysis showed significant down-regulation in insulin, PDX-1, PI3K, AKT/p-AKT, and Bcl2. On the other hand, expression of BAX and BAD and cleaved PARP were significantly increased. Interestingly, preincubation with CA reversed the adverse impact of STZ at the cellular and protein expression levels. In conclusion, the data indicate that CA protects β-cells against STZ-induced damage, presumably through its modulatory effect on the different pathways, including the Pi3K/AKT/PDX-1/insulin pathway and mitochondria-mediated apoptosis.

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Section: Discussionmentioning

confidence: 99%

Carnosic Acid Protects INS-1 β-Cells against Streptozotocin-Induced Damage by Inhibiting Apoptosis and Improving Insulin Secretion and Glucose Uptake

et al. 2022

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“…((R)-5-hydroxypyrrolidin-2-one, methyl(R)-pyroglutamate, loliolide, 3-benzofuran carboxaldehyde and odisolane, which protected pancreatic INS-1 cells from streptozotocin-induced cytotoxicity. 25 2.1 | Five and six-membered ring synthetic heterocycles…”

Section: Five-membered Ring Natural Heterocyclicsmentioning

confidence: 99%

Advancement in chiral heterocycles for the antidiabetic activity

Gupta,

Rani,

Nainwal

et al. 2024

Chirality

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For the synthesis and development of pharmaceuticals, chirality is an important structural component. Chiral heterocyclic compounds have annoyed the interest of synthetic chemists who are working to create useful and efficient techniques for these molecules. As indicated by the expanding number of chiral drugs created in the last two decades, the link between chirality and pharmacological activity has become more important in the pharmaceutical and biopharmaceutical industries. Approximately 65% of currently used drugs are chiral, and many of them are promoted as racemates in many circumstances. There are a growing number of new chiral heterocyclic compounds with important biological properties and intriguing uses in medical chemistry and drug discovery. In this study, we review current breakthroughs in chiral heterocycles and their different physiological activities that have been published in the last year (from 2010 to early 2023). This study focuses on the current trends in the use of chiral heterocycles in drug design and the creation of several powerful and competent candidates for diabetic illnesses.

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“…We also identified butyl pyroglutamate from M. alba fruits as a nephroprotective agent against cisplatin-induced kidney cell death in LLC-PK1, and its effect was found to be mediated by attenuation of the phosphorylation of c-Jun N-terminal kinase, MAPK, ERK, p38, and caspase-3 [41]. In particular, we recently found that loliolide, a heterocyclic compound in M. alba fruits, showed a protective effect against streptozotocin-induced apoptosis of INS-1 cells via inhibition of the caspase signaling pathway and induction of B-cell lymphoma-2 (Bcl-2) protein expression, suggesting that the active compound could be effective in preventing diabetes mellitus [42]. In the present study, the ethanol extract of M. alba fruits was further investigated to identify potential antidiabetic natural compounds, as there have been few studies on the antidiabetic compounds identified from M. alba and their underlying mechanisms of action, although it has been used in traditional medicine to lower blood sugar levels [36], and M. alba extracts are known to exhibit antidiabetic properties [37,38].…”

Section: Introductionmentioning

confidence: 99%

Antidiabetic Flavonoids from Fruits of Morus alba Promoting Insulin-Stimulated Glucose Uptake via Akt and AMP-Activated Protein Kinase Activation in 3T3-L1 Adipocytes

Lim

Lee

et al. 2021

Pharmaceutics

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Morus alba (Moraceae), known as white mulberry, has been used to treat fever, protect against liver damage, improve eyesight, and lower blood sugar levels in traditional oriental medicine. Few studies have been conducted on the antidiabetic compounds identified from M. alba and their underlying mechanisms of action. Consequently, in this study, the fruits of M. alba were investigated for potential antidiabetic natural products using 3T3-L1 adipocytes. Phytochemical analysis of the ethanolic extract of M. alba fruits, followed by high-performance liquid chromatography (HPLC), purification led to the isolation of two main compounds: rutin and quercetin-3-O-β-d-glucoside (Q3G). Long-term use of available drugs for treating type 2 diabetes ((T2D) is often accompanied by undesirable side effects, which have generated increased interest in the development of more effective and safer antidiabetic agents. Examination of the isolated compounds, rutin and Q3G, for antidiabetic or anti-obesity properties or both in 3T3-L1 adipocytes demonstrated that they both improved glucose uptake via Akt-mediated insulin signaling pathway or AMP-activated protein kinase (AMPK) activation in 3T3-L1 adipocytes. The compounds also showed a positive effect on lipid accumulation in adipocytes, suggesting that glucose uptake occurred through activation of the Akt and AMPK signaling pathway without inducing adipogenesis. Taken together, our findings suggest that rutin and Q3G in M. alba fruits have the potential to induce fewer side effects such as weight gain, and these active compounds could be potential therapeutic candidates for the management of T2D.

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Identification of bioactive heterocyclic compounds from mulberry and their protective effect against streptozotocin-induced apoptosis in INS-1 cells

Cited by 5 publications

References 26 publications

Carnosic Acid Protects INS-1 β-Cells against Streptozotocin-Induced Damage by Inhibiting Apoptosis and Improving Insulin Secretion and Glucose Uptake

Carnosic Acid Protects INS-1 β-Cells against Streptozotocin-Induced Damage by Inhibiting Apoptosis and Improving Insulin Secretion and Glucose Uptake

Advancement in chiral heterocycles for the antidiabetic activity

Antidiabetic Flavonoids from Fruits of Morus alba Promoting Insulin-Stimulated Glucose Uptake via Akt and AMP-Activated Protein Kinase Activation in 3T3-L1 Adipocytes

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