Clinical Application Potential of Small Molecules that Induce Brown Adipose Tissue Thermogenesis by Improving Fat Metabolism

Lu, Kang; Dass, Kingsley Theras Primus; Tsai, Shin‐Fu; Chuang, Hong-Meng; Lin, Shinn‐Zong; Liu, Shih‐Ping; Harn, Horng‐Jyh

doi:10.1177/0963689720927394

Cited by 5 publications

(4 citation statements)

References 49 publications

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“…PPAPs might therefore represent a new scaffold of thermogenic inducers. Several clinical trials that aimed to promote BAT thermogenesis and browning of WAT have been carried out, but there are no effective and safe drugs that can increase the amounts of BAT or activate BAT, in clinical settings, for the treatment of metabolic diseases (Lu et al, 2020). Thus, more specific targets and drug delivery systems to WAT need to be developed to enhance browning-inducing activity and reduce the effects on other tissues.…”

Section: Discussionmentioning

confidence: 99%

Bioactivity‐based molecular networking‐guided identification of guttiferone J from Garcinia cambogia as an anti‐obesity candidate

Chen

et al. 2022

British J Pharmacology

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Background and Purpose: Pharmacological intervention to induce browning of white adipose tissue provides a promising anti-obesity therapy. The fruits of Garcinia cambogia (Clusiaceae) have been widely applied to manage body weight; however, the chemical principles remain unclear. The current study aims to discover browning inducers from the fruits of G. cambogia and investigate the underlying mechanisms.Experimental Approach: The bioactivity-based molecular networking and Oil Red O staining on 3T3-L1 and C3H10T1/2 adipocytes were applied for guided isolation.High-fat diet-induced obese mice were recruited to evaluate the anti-obesity activity.

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Section: Discussionmentioning

confidence: 99%

Bioactivity‐based molecular networking‐guided identification of guttiferone J from Garcinia cambogia as an anti‐obesity candidate

Chen

et al. 2022

British J Pharmacology

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“…Aside from controlling energy intake, novel drugs that aim to boost energy expenditure through stimulating thermogenesis are receiving more attention nowadays. , For instance, recent studies have revealed the crucial role of brown adipose tissue in dissipating energy by producing heat. Thus, research has been striving to induce the transformation of adipose tissue from white to beige, achieving the “browning effect” to suppress obesity .…”

Section: Pharmaceuticals and Polymeric Biomaterials Carriersmentioning

confidence: 99%

Current Role and Potential of Polymeric Biomaterials in Clinical Obesity Treatment

2023

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The rise of obesity and associated fatal diseases has taken a massive toll worldwide. Despite the existing pharmaceuticals and bariatric surgeries, these approaches manifest limited efficacy or accompany various side effects. Therefore, researchers seek to facilitate the prolonged and specific delivery of therapeutics. Or else, to mimic the essential part of "gastric bypass" by physically blocking excessive absorption via less invasive methods. To achieve these goals, polymeric biomaterials have gained tremendous interest recently. They are known for synthesizing hydrogels, microneedle patches, mucoadhesive coatings, polymer conjugates, and so forth. In this Review, we provide insights into the current studies of polymeric biomaterials in the prevention and treatment of obesity, inspiring future improvements in this regime of study.

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“…In this context, significant advancements have been made in unraveling white adipose tissue (WAT) mechanisms to reveal potential approaches for reducing fat accumulation [4]. Recently, there has been an emphasis on the approaches that are centered around brown adipose tissue (BAT) due to its unique inherent ability to modulate global energy expenditure in the form of heat [5]. This exceptional feature of BAT, to dissipate energy through non-shivering thermogenesis, underscores its importance as a crucial target in combating obesity [6].…”

Section: Introductionmentioning

confidence: 99%

High-Fat-High-Fructose Diet Elicits Brown Adipocyte Dysfunction through miRNA-103 Induced miRNA Biogenesis Pathway

Shree,

Meruvu,

Park

et al. 2024

Obesities

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Background: Obesity is a critical public health concern with its prevalence growing at an alarming rate worldwide. The Western diet that typically includes high-fat or high-fructose components is one of the leading contributing factors of obesity. Recent findings demonstrate the essential role of BAT in regulating whole-body metabolism. However, the explicit mechanism through which BAT maintains homeostasis is still unknown. Methods: Six-week-old C57BL/6 male mice were fed either a low-fat diet (LFD) or a high-fat high-fructose diet (HFHFD) for 4, 12, and 20 weeks. Results: We observed a significant increase in BAT weight under HFHFD along with BAT whitening in a time-dependent manner. This was also accompanied by a significant decrease in UCP1 and PGC1α protein, as well as a significant increase in the Bax/Bcl-2 ratio as early as 12 weeks, indicating increased apoptosis under HFHFD. Interestingly, miRNA-103 expression that holds a seed sequence within the miRNA biogenesis machinery, Dicer, was significantly upregulated after 12 and 20 weeks of HFHFD. Dicer and another biogenesis regulator, TRBP2, exhibited significant upregulation at 4 weeks of HFHFD. Conversely, those gene expressions were significantly downregulated at 12 and 20 weeks of HFHFD, followed by a significant decrease in the protein level at 12 weeks. To confirm the mechanistic connection, miRNA-103 knockdown in vitro significantly upregulated Dicer and the TRBP2 gene. However, only Dicer exhibited a significant increase at the translational level. Conclusion: Overall, we conclude that HFHFD may elicit BAT dysfunction by inhibiting Dicer via miRNA-103.

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Clinical Application Potential of Small Molecules that Induce Brown Adipose Tissue Thermogenesis by Improving Fat Metabolism

Cited by 5 publications

References 49 publications

Bioactivity‐based molecular networking‐guided identification of guttiferone J from Garcinia cambogia as an anti‐obesity candidate

Bioactivity‐based molecular networking‐guided identification of guttiferone J from Garcinia cambogia as an anti‐obesity candidate

Current Role and Potential of Polymeric Biomaterials in Clinical Obesity Treatment

High-Fat-High-Fructose Diet Elicits Brown Adipocyte Dysfunction through miRNA-103 Induced miRNA Biogenesis Pathway

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