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Isoeugenol (IEG), a natural component of clove oil, possesses antioxidant, anti-inflammatory, and antibacterial properties. However, the effects of IEG on adipogenesis have not yet been elucidated. Here, we showed that IEG blocks adipogenesis in 3T3-L1 cells at an early stage. IEG inhibits lipid accumulation in adipocytes in a concentration-dependent manner and reduces the expression of mature adipocyte-related factors including PPARγ, C/EBPα, and FABP4. IEG treatment at different stages of adipogenesis showed that IEG inhibited adipocyte differentiation by suppressing the early stage, as confirmed by lipid accumulation and adipocyte-related biomarkers. The early stage stimulates growth-arrested preadipocytes to enter mitotic clonal expansion (MCE) and initiates their differentiation into adipocytes by regulating cell cycle-related factors. IEG arrested 3T3-L1 preadipocytes in the G0/G1 phase of the cell cycle and attenuated cell cycle-related factors including cyclinD1, CDK6, CDK2, and cyclinB1 during the MCE stage. Furthermore, IEG suppresses reactive oxygen species (ROS) production during MCE and inhibits ROS-related antioxidant enzymes, including superoxide dismutase1 (SOD1) and catalase. The expression of cell proliferation-related biomarkers, including pAKT and pERK1/2, was attenuated by the IEG treatment of 3T3-L1 preadipocytes. These findings suggest that it is a potential therapeutic agent for the treatment of obesity. [ABSTRACT FROM AUTHOR]

Abstract Obesity is a major risk to human health. Adipogenesis is blocked by α-tocopherol and conjugated linoleic acid (CLA). However, their effect at preventing obesity is uncertain. The effectiveness of the bioactive agents is associated with their delivery method. Herein, we designed CLA-loaded tocol nanostructured lipid carriers (NLCs) for enhancing the anti-adipogenic activity of α-tocopherol and CLA. Adipogenesis inhibition by the nanocarriers was examined using an in vitro adipocyte model and an in vivo rat model fed a high fat diet (HFD). The targeting of the tocol NLCs into adipocytes and adipose tissues were also investigated. A synergistic anti-adipogenesis effect was observed for the combination of free α-tocopherol and CLA. Nanoparticles with different amounts of solid lipid were developed with an average size of 121‒151 nm. The NLCs with the smallest size (121 nm) showed greater adipocyte internalization and differentiation prevention than the larger size. The small-sized NLCs promoted CLA delivery into adipocytes by 5.5-fold as compared to free control. The nanocarriers reduced fat accumulation in adipocytes by counteracting the expression of the adipogenic transcription factors peroxisome proliferator activated receptor (PPAR)γ and CCAAT/enhancer-binding protein (C/EBP)α, and lipogenic enzymes acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS). Localized administration of CLA-loaded tocol NLCs significantly reduced body weight, total cholesterol, and liver damage indicators in obese rats. The biodistribution study demonstrated that the nanoparticles mainly accumulated in liver and adipose tissues. The NLCs decreased adipocyte hypertrophy and cytokine overexpression in the groin and epididymis to a greater degree than the combination of free α-tocopherol and CLA. In conclusion, the lipid-based nanocarriers were verified to inhibit adipogenesis in an efficient and safe way.

Chamaecostus cuspidatus (Nees & Mart.) C.D.Specht & D.W.Stev and Cheilocostus speciosus (J.Koenig) C.D.Specht contain bioactive compounds that possess many pharmacological activities including antidiabetic and hypolipidemic. These plants are used to treat diabetes by herbal healers. Considering the traditional use of C. cuspidatus and C. speciosus, the present study is designed to perform qualitative and quantitative analysis as well as in-vitro anti-adipogenesis against 3T3-L1 cells to ensure efficacy. A total of thirty-eight compounds were identified using HPLC-QTOF-MS/MS. Quantification of ten bioactive compounds among identified compounds was performed by UPLC-QqQLIT-MS/MS. The quantification method was validated according to ICH guidelines (International conference on harmonization guidelines). Quantification of bioactive compounds of different organs of C. cuspidatus and C. speciosus showed remarkable differences in the content. Microscopic and ORO absorbance confirmed the antiadipogenic potential of leaves (L-02), roots (R-02) of C. cuspidatus and leaves of C. speciosus (L-01) in 3T3-L1 cells. [ABSTRACT FROM AUTHOR]

[Display omitted] • Two undescribed stilbenes were isolated from Cajanus cajan. • PPAR γ was identified as the key target for blocking differentiation of adipocytes by CAB and CAC. • Molecular docking was performed to find the possible binding mode of compounds to PPAR γ. • A potential mechanism on anti-adipogenic effects of CAB and CAC in 3 T3-L1 adipocytes was proposed. Two new stilbenes, denominated Cajanotone B (CAB) and Cajanotone C (CAC), were isolated from the leaves of Cajanus cajan. In this study, the structures of CAB and CAC were unambiguously elucidated by a combination of various spectral methods. Both compounds significantly inhibited the adipogenesis in 3T3-L1 adipocytes by reducing the lipid accumulation, triglyceride content and FFA secretion. CAB and CAC also substantially inhibit the mRNA expression of HSL, ATGL, C/EBPα and PPARγ as deciphered based by RT-PCR assay. Down-regulation of PPAR is believed to be the primary mechanism underlying which CAB and CAC inhibited adipogenic differentiation because the lipid-promoting activity of PPAR agonists can be counteracted by these compounds. The molecular interaction between CAB/CAC and PPAR γ was revealed with the help of molecular docking. Taken together, CAB and CAC could serve as new lead compounds with the potential to speed up the development of novel lipid-lowering and weight-control therapies. [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of Oroxylum indicum fruit extract on high-fat diet-induced hyperlipidemic mice. Methods: The phytochemical composition of Oroxylum indicum fruit extract was determined by liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) and gas chromatography-mass spectrometry. Forty-two male mice were used. The mice were divided into six groups: normal control, high-fat diet control, simvastatin treatment (20 mg/kg BW/day), and Oroxylum indicum fruit extract (100, 200, 300 mg/kg BW/day) treatment groups. Food intake, body weight, serum parameters, lipid profile, and histopathological lesions of the kidney, liver, and epididymal fat were observed. Results: LC-MS/MS results revealed four major components of Oroxylum indicum fruit extract: luteolin, apigenin, baicalein, and oroxylin A. Twenty-seven volatile oils were identified from Oroxylum indicum fruit extract. Daily oral administration of Oroxylum indicum fruit extract at 100 to 300 mg/kg BW/day significantly reduced the body weight, total cholesterol, triglyceride, and low-density lipoprotein cholesterol level (P

Non-alcoholic fatty liver disease (NALFD) is a disease characterized by liver steatosis. The liver is a key organ involved in the metabolism of fat, protein, and carbohydrate, enzyme activation, and storage of glycogen, which is closely related to the intestine by the bidirectional relation of the gut-liver axis. Abnormal intestinal microbiota composition can affect energy metabolism and lipogenesis. In this experiment, we investigated the beneficial effect of Lactobacillus reuteri MJM60668 on lipid metabolism and lipogenesis. C57BL/6 mice were fed a high-fat diet (HFD) and orally administrated with MJM60668. Our results showed that mice treated with MJM60668 significantly decreased liver weight and liver/body weight ratio, without affecting food intake. Serum levels of ALT, AST, TG, TCHO, and IL-1β in mice fed with MJM60668 were decreased compared to the HFD group. Investigation of gene and protein expression on the lipogenesis and lipid metabolism showed that the expression of ACC, FAS, and SREBP was decreased, and PPARα and CPT was increased. Furthermore, an increase of adiponectin in serum was shown in our experiment. Moreover, serum IL-1β level was also significantly decreased in the treated mice. These results suggested that MJM60668 can strongly inhibit lipogenesis, enhance fatty acid oxidation, and suppress inflammation. Additionally, supplementation of MJM60668 increased the proportion of Akkermansiaceae and Lachnospiracea, confirming a potential improvement of gut microbiota, which is related to mucus barrier and decrease of triglycerides levels. [ABSTRACT FROM AUTHOR]

Obesity and overweight have serious health outcomes. "Phikud Tri-Phon" (PTP) is a traditional Thai medicine comprising three dried fruits from Aegle marmelos L., Morinda citrifolia L., and Coriandrum sativum L. Whether this medicine impacts on metabolic disease is unclear. This study aimed to investigate the phenolic and flavonoid contents of PTP and each of its herbal components, and further assess their antioxidant and anti-adipogenetic activities. Oil-red O staining was measured for lipid accumulation in 3T3-L1 adipocytes. The chemical profiles of PTP and each herbal extract were determined by LC-ESI-QTOF-MS/MS. Our results show that the total phenolic and flavonoid contents of PTP water extract were 22.35–108.42 mg of gallic acid equivalents and PTP ethanolic extract was 1.19–0.93 mg of quercetin equivalents and the DPPH scavenging capacity assay of PTP ethanolic extract (1 mg/mL) was 92.45 ± 6.58 (Trolox equivalent)/g. The PTP extracts and individual herbs had inhibitory adipogenesis activity, which reduced lipid accumulation by approximately 31% in PTP water extract and 22% in PTP ethanolic extract compared with control cells. These results provided insights into the traditional preparation method of using boiling water as a vehicle for PTP. In conclusion, PTP has antioxidant and anti-adipogenesis potential, indicating it is a promising ingredient in functional food and herbal health products. [ABSTRACT FROM AUTHOR]

Obesity, one of the common worldwide chronic health diseases co‐relates with adipogenesis. Adipogenesis is a complex biological action of the emergence of mature adipocytes from the differentiation of pre‐adipocytes and the disfunction of this process leads to the development of metabolic issues in obesity. Recently, much attention has been paid to utilizing natural compounds to discover their biological activities. This study focused on investigating the probable anti‐adipogenic effects of gallic acid‐g‐chitosan (GAC) and plain chitosan (PC) through regulating the heme oxygenase‐1 (HO‐1)/Nrf2 pathway on mesenchymal stem cells. Gallic acid is grafted onto the PC backbone to improve its specific physical and biological properties. GAC showed promising anti‐adipogenic effects by enhancing HO‐1 expression and lipolysis and as well as suppressing lipid accumulation, reactive oxygen species, and pro‐inflammatory cytokines production, transcription factor expression compared to the PC treatment. On the contrary, zinc protoporphyrin ІX (ZnPP), a HO‐1 inhibitor reversed these effects of GAC on adipogenesis. Taken all together, this study revealed that grafting GA onto the chitosan improved potential anti‐adipogenic activity by induction of the HO‐1/Nrf2 pathway on mesenchymal stem cells (MSCs). Practical applications: GAC is a well‐known copolymer with versatile bioactivities such as antimicrobial, antioxidant, and anti‐diabetic activity. However, the anti‐adipogenic effect of GAC has not been explored in MSCs. This study demonstrated that GAC inhibited adipocyte differentiation in MSCs through HO‐1 activation. These findings suggest that GAC can be applied practically from different perspectives. GAC can be applied in the pharmacological industry to the development of anti‐obesity drugs, medicinal perspectives for the treatment of obesity and obesity‐related diseases, and in the food industry as a functional food to promote health and decrease the risk of diseases. [ABSTRACT FROM AUTHOR]

Red rice bran extract (RRBE) has been reported to have the potential for in vitro metabolic modulation and anti-inflammatory properties. However, little is known about the molecular mechanisms of these potentials in adipose tissue. This study aimed to evaluate the in vivo anti-adipogenic, anti-hypertrophic, and anti-inflammatory activities of RRBE and its major bioactive compounds in mice. After six weeks of consuming either a low-fat diet or a high-fat diet (HFD), 32 mice with initial body weights of 20.76 ± 0.24 g were randomly divided into four groups; the four groups were fed a low-fat diet, a HFD, a HFD plus 0.5 g/kg of RRBE, or a HFD plus 1 g/kg of RRBE, respectively. The 6-week treatment using RRBE reduced HFD-induced adipocyte hypertrophy, lipid accumulation, and inflammation in intra-abdominal epididymal white adipose tissue (p < 0.05) without causing significant changes in body and adipose tissue weight, which reductions were accompanied by the down-regulated expression of adipogenic and lipid metabolism genes, including CCAAT/enhancer-binding protein-alpha, sterol regulatory element-binding protein-1c, and hormone-sensitive lipase (p < 0.05), as well as inflammatory genes, including macrophage marker F4/80, nuclear factor-kappa B p65, monocyte chemoattractant protein-1, tumor necrosis factor-alpha, and inducible nitric oxide synthase (p < 0.05), in adipose tissue. Furthermore, RRBE significantly decreased serum tumor necrosis factor-alpha levels (p < 0.05). Bioactive compound analyses revealed the presence of phenolics, flavonoids, anthocyanins, and proanthocyanidins in these extracts. Collectively, this study demonstrates that RRBE effectively attenuates HFD-induced pathological adipose tissue remodeling by suppressing adipogenesis, lipid dysmetabolism, and inflammation. Therefore, RRBE may emerge as one of the alternative food products to be used against obesity-associated adipose tissue dysfunction. [ABSTRACT FROM AUTHOR]

Sulfuretin is a natural flavonoid found in the plant Rhus verniciflua STOKES. The plant has been traditionally used as medicinal agent for antiviral, cathartic, diaphoretic, anti-rheumatic and sedative activities in East Asia. In this study we isolated and identified sulfuretin from R. verniciflua and investigated its anti-adipogenic activity against 3T3-L1 preadipocytes cells. We evaluated the effects of sulfuretin on the adipogenic transcription factors like peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer-binding protein α (C/EBPα), fatty acid synthase (FAS), Fabp4, adiponectin and zinc fingerprint protein (Zfp) 521 by gene expression (real-time QPCR) and Western blot analysis. Sulfuretin treatment at Day 0 and 2 showed significant reduction of lipid production in 3T3-L1 cells in concentration dependent manner. Gene expression analysis (real-time PCR) revealed that sulfuretin inhibited the both major adipogenic factors (C/EBPα, C/EBPβ and PPARγ) and minor adipogenic factors (sterol regulatory element-binding protein (SREBP1c), adiponectin, FAS, Fabp4, Zfp423, and Ebf1). Western blot analysis showed the increased expression of β-catenin and suppression of PPARγ after sulfuretin treatment. Overall, sulfuretin is a natural flavonoid having potent anti-adipogenic activity through the suppression of major adipogenic factors C/EBPα, C/EBPβ and PPARγ, which initiate adipogenesis.

Obesity is a major risk factor in many health problems. This study explored the anti-obesity and antihyperlipidemic effects of Musa cavendishii Lamb. leaves. Doses of 1200 mg/kg of M. cavendishii methanol extract, or 300 mg/kg of fractions, were given to C57BL/6J mice fed with a high-fat diet (HFD) for 7 weeks. The reduction in fat volume was determined using CT scan and histopathological examination of mice livers. The results showed that the n-hexane and the EtOAc fractions reduced the body fat volume to 2.0% and 2.2% respectively, compared to 20.1% in the HFD group. Also, treated groups showed almost normal liver architecture with no fat vacuoles compared to the HFD group. Moreover, the treated groups showed a reduction in the levels of some obesity-related biochemical parameters, including plasma glucose, cholesterol, and triglycerides levels. Chromatographic fractionation of the bioactive n-hexane extract afforded four known compounds viz., palmitic acid (1), 5-methyl-5-(4,8,12-trimethyl-tridecyl)-dihydro-furan-2-one (2), cycloeucalenol (3), and stigmasterol (4). These compounds were in vitro and in silico studied for their pancreatic lipase (PL) inhibition. Compound 2 showed remarkable PL inhibition (89.8%) compared to orlistat (85.0%) at 200 µM, which was in full agreement with the docking scores (-7.19 and -4.05, respectively). [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of Oroxylum indicum fruit extract on high-fat diet-induced hyperlipidemic mice. Methods: The phytochemical composition of Oroxylum indicum fruit extract was determined by liquid chromatographymass spectrometry/mass spectrometry (LC-MS/MS) and gas chromatography-mass spectrometry. Forty-two male mice were used. The mice were divided into six groups: normal control, high-fat diet control, simvastatin treatment (20 mg/kg BW/day), and Oroxylum indicum fruit extract (100, 200, 300 mg/kg BW/day) treatment groups. Food intake, body weight, serum parameters, lipid profile, and histopathological lesions of the kidney, liver, and epididymal fat were observed. Results: LC-MS/MS results revealed four major components of Oroxylum indicum fruit extract: luteolin, apigenin, baicalein, and oroxylin A. Twenty-seven volatile oils were identified from Oroxylum indicum fruit extract. Daily oral administration of Oroxylum indicum fruit extract at 100 to 300 mg/kg BW/day significantly reduced the body weight, total cholesterol, triglyceride, and low-density lipoprotein cholesterol level (P<0.05), whereas high-density lipoprotein cholesterol was higher than the high-fat diet control group. Treatment with 300 mg/kg BW/day Oroxylum indicum fruit extract reduced the pathological lesion and prevented fat accumulation in the kidney and liver. Conclusions: Oroxylum indicum fruit extract has hypolipidemic effect in hyperlipidemic mice, and the active ingredients of Oroxylum indicum fruit extract, both flavonoids and volatile oils, should be further explored as an antihyperlipidemic agent. [ABSTRACT FROM AUTHOR]

An ethanolic glutinous black rice bran extract (RBE) was prepared and used in the experiments to determine the phenolic and flavonoid contents, antioxidation using DPPH and TBARS assay, anti-adipogenesis, and lipolysis induction in a 3T3-L1 pre-adipocyte model to discover its anti-obesity potential. The results showed that RBE was composed of phenolics, flavonoids, and anthocyanins and showed antioxidative activities (8.58±0.14 mg Vit C eq/g extract and 6.06±0.49 mg BHT eq/g extract). Interestingly, its anti-obesity potential was demonstrated in the interruption of the adipocyte life cycle, i.e. a significant anti-adipogenesis effect in the reduction of lipid accumulation (50.86±3.26 to 97.06±8.09% of the negative control, and triglyceride content in 3T3-L1 pre-adipocytes (36.89±2.08 to 90.56±0.67% of the negative control), and lipolysis induction (relative glycerol content 117.62±1.44 and 163.72±10.18% of control). Therefore, implementation into obesity therapy requires further research.

Objective: To establish an efficacious and efficient fermentation method of enhancing the anti-adipogenesis effect of mulberry (Morus alba) leaves using Cordyceps militais. Methods: Dried mulberry leaves, dried mulberry leaves with 50% raw silkworm pupa and raw silkworm pupa were fermented with Cordyceps militais for 4 weeks at 25 °C, after which the dried mulberry leaves and fermented product were extracted with 70% ethanol and subjected to high performance liquid chromatography (HPLC). The contents of cordycepin, pelargonidin, chlorogenic acid, iso-quercetin and caffeic acid were determined. We then used the 3T3-L1 cells to investigate whether extracts of fermentation enhanced anti-adipogenesis activity in vitro. Results: HPLC showed that fermentation changed the contents of cordycepin, pelargonidin, chlorogenic acid, iso-quercetin and caffeic acid. Furthermore, fermented dried mulberry leaves with 50% raw silkworm pupa had a better efficacy of anti-adipogenesis than dried mulberry leaves, fermented dried mulberry leaves and fermented silkworm pupa and inhibited triglycerides accumulation and glucose consumption. Additionally, fermented dried mulberry leaves with 50% raw silkworm pupa inhibited PPAR-γ signaling. Conclusions: Fermentation with Cordyceps militaris enhanced anti-adipogenesis efficacy of mulberry leaves.

This study aimed to investigate the therapeutic potential of Citrullus mucosospermus extract (CME) in counteracting adipogenesis and its associated metabolic disturbances in murine models. In vitro experiments utilizing 3T3-L1 preadipocytes revealed that CME potently inhibited adipocyte differentiation, as evidenced by a dose-dependent reduction in lipid droplet formation. Remarkably, CME also attenuated glucose uptake and intracellular triglyceride accumulation in fully differentiated adipocytes, suggesting its ability to modulate metabolic pathways in mature adipose cells. Translating these findings to an in vivo setting, we evaluated the effects of CME in C57BL/6N mice fed a high-fat diet (HFD) for 10 weeks. CME administration, concomitantly with the HFD, resulted in a significant attenuation of body weight gain compared to the HFD control group. Furthermore, CME treatment led to substantial reductions in liver weight, total fat mass, and deposits of visceral and retroperitoneal adipose tissue, underscoring its targeted impact on adipose expansion. Histological analyses revealed the remarkable effects of CME on hepatic steatosis. While the HFD group exhibited severe lipid accumulation within liver lobules, CME dose-dependently mitigated this pathology, with the highest dose virtually abolishing hepatic fat deposition. An examination of adipose tissue revealed a progressive reduction in adipocyte hypertrophy upon CME treatment, culminating in a near-normalization of adipocyte morphology at the highest dose. Notably, CME exhibited potent anti-inflammatory properties, significantly attenuating the upregulation of pro-inflammatory cytokines' mRNA levels (TNF-α, IL-1β and IL-6) in the livers of HFD-fed mice. This suggests a potential mechanism through which CME may exert protective effects against inflammation associated with obesity and fatty liver disease.

Background: Phytoconstituents are known to have an arena of health benefits. The choice of extraction solvents for a desired pharmacological activity is poorly characterized. Objectives: The present study compared the use of different solvents to extract phytoconstituents, evaluate cytotoxicity and anti-obesity activities. Materials and Methods: Leaves, bark, flowers or tubers of fourteen commonly utilized plants in the Sri Lankan Ayurvedic system were used to prepare extracts of distilled water (DW), ethanol or n-hexane. Phytochemical screening, total phenolic and flavonoid contents (TPC and TFC), cytotoxicity and triglyceride assays were performed. Results: DW served as the best solvent to extract the highest yield of phytochemicals followed by ethanol marking hexane as the least efficient solvent. The water extract (WE) of Averrhoa bilimbi leaves and ethanol extract (EE) of Cassia auriculata showed the highest TPC. The TFC was lowest in the hexane extract (HE) of all plants. The WE of plants showed =75% cell viability below 500 µg/mL with no potential anti-adipogenic activity. The EE of Justicia adhathoda showed maximum lipid inhibition (88.31%), followed by Aerva lanata (74.65%), and Cyperus rotundus (74.04%) at 100 µg/mL. The EE of Ipomoea aquatica (45.11%), Murrya koenigii (41.04%), and Hemidesmus indicus (32.97%) showed the highest viable anti-adiposity activity at 50 µg/mL. Conclusion: The WE of most plants provided a greater yield of phytoconstituents enabling their safe usage in higher doses during Ayurvedic medication. Ethanol served as a better solvent to extract constituents responsible for anti-adipogenesis and no possible correlation was found between the phenolic content and anti-adiposity. [ABSTRACT FROM AUTHOR]

Obesity is caused by excessive fat cells and the overgrowth of adipocytes and is a major risk factor for several chronic illnesses. Aronia melanocarpa fruit is rich in anthocyanins and polyphenols and has protective effects against various diseases. In this study, we examined the effect of Aronia extract (Aronia bioactive fraction, ABF®) on the biomarkers of the adipogenic pathway during adipocyte differentiation of 3T3-L1 cells. Lipid accumulation was verified by Oil Red O staining. mRNA and protein expression of lipoprotein lipase (LPL), CCAAT/enhancer-binding protein α (C/EBPα), peroxisome proliferator-activated receptor γ (PPARγ), fatty acid-binding protein 2 (FABP2), and fatty acid synthase (FAS) were assayed by RT-qPCR and Western blot analyses. Adiponectin and leptin secretion were measured using enzyme-linked immunosorbent assays. ABF® treatment downregulated lipid accumulation based on Oil Red O staining. ABF®-treated cells exhibited decreased mRNA and protein expression of LPL, C/EBPα, PPARγ, FABP2, and FAS. Moreover, ABF® treatment significantly increased adiponectin secretion and decreased leptin secretion. In conclusion, ABF® has anti-adipogenic effects on the differentiation of 3T3-L1 cells and may be used as an anti-obesity nutraceutical. [ABSTRACT FROM AUTHOR]

Non-alcoholic fatty liver disease (NALFD) is a disease characterized by liver steatosis. The liver is a key organ involved in the metabolism of fat, protein, and carbohydrate, enzyme activation, and storage of glycogen, which is closely related to the intestine by the bidirectional relation of the gut-liver axis. Abnormal intestinal microbiota composition can affect energy metabolism and lipogenesis. In this experiment, we investigated the beneficial effect of Lactobacillus reuteri MJM60668 on lipid metabolism and lipogenesis. C57BL/6 mice were fed a high-fat diet (HFD) and orally administrated with MJM60668. Our results showed that mice treated with MJM60668 significantly decreased liver weight and liver/body weight ratio, without affecting food intake. Serum levels of ALT, AST, TG, TCHO, and IL-1β in mice fed with MJM60668 were decreased compared to the HFD group. Investigation of gene and protein expression on the lipogenesis and lipid metabolism showed that the expression of ACC, FAS, and SREBP was decreased, and PPARα and CPT was increased. Furthermore, an increase of adiponectin in serum was shown in our experiment. Moreover, serum IL-1β level was also significantly decreased in the treated mice. These results suggested that MJM60668 can strongly inhibit lipogenesis, enhance fatty acid oxidation, and suppress inflammation. Additionally, supplementation of MJM60668 increased the proportion of Akkermansiaceae and Lachnospiracea, confirming a potential improvement of gut microbiota, which is related to mucus barrier and decrease of triglycerides levels.

Obesity and overweight have serious health outcomes. “Phikud Tri-Phon” (PTP) is a traditional Thai medicine comprising three dried fruits from Aegle marmelos L., Morinda citrifolia L., and Coriandrum sativum L. Whether this medicine impacts on metabolic disease is unclear. This study aimed to investigate the phenolic and flavonoid contents of PTP and each of its herbal components, and further assess their antioxidant and anti-adipogenetic activities. Oil-red O staining was measured for lipid accumulation in 3T3-L1 adipocytes. The chemical profiles of PTP and each herbal extract were determined by LC-ESI-QTOF-MS/MS. Our results show that the total phenolic and flavonoid contents of PTP water extract were 22.35–108.42 mg of gallic acid equivalents and PTP ethanolic extract was 1.19–0.93 mg of quercetin equivalents and the DPPH scavenging capacity assay of PTP ethanolic extract (1 mg/mL) was 92.45 ± 6.58 (Trolox equivalent)/g. The PTP extracts and individual herbs had inhibitory adipogenesis activity, which reduced lipid accumulation by approximately 31% in PTP water extract and 22% in PTP ethanolic extract compared with control cells. These results provided insights into the traditional preparation method of using boiling water as a vehicle for PTP. In conclusion, PTP has antioxidant and anti-adipogenesis potential, indicating it is a promising ingredient in functional food and herbal health products.

Agastache rugosa, or Korean mint, is an herb used as a spice, food additive and traditional medicinal ingredient. It has desirable effects, such as its antibacterial, antifungal and antioxidant properties. A. rugosa contains many phenolic compounds studied for their various health benefits, with the primary components being tilianin. A. rugosa extract (ARE), which was extracted with ethanol and freeze-dried, contained 21.14 ± 0.15 mg/g of tilianin with a total polyphenol content of 38.11 ± 0.88 mg/g. Next, the antiadipogenic effect of A. rugosa and tilianin was clarified using 3T3-L1 cells, which differentiate into adipocytes and develop lipid droplets. 3T3-L1 cells were treated with ARE or tilianin and lipid accumulation (%) was calculated through oil red O staining. Tilianin elicited dose-dependent decrease in lipid accumulation (% of positive control) (30 μM 92.10 ± 1.19%; 50 μM 69.25 ± 1.78%; 70 μM 54.86 ± 1.76%; non-differentiation 18.10 ± 0.32%), assessed by oil-red-O staining, whereas ARE treatments caused consistent diminution in lipid accumulation regardless of dose (100 μM 86.90 ± 4.97%; 200 μM 87.25 ± 4.34%; 400 μM 88.54 ± 2.27%; non-differentiation 17.96 ± 1.30%), indicating that both compounds have anti-obesity effects on adipocytes. Treatment with ARE lowered the mRNA (PPARγ; C/EBPα; FABP4; SREBP1; ACC; FAS) and protein (PPARγ; C/EBPα; SREBP1) levels of adipogenesis and lipogenesis-related factors. Tilianin showed a greater effect on the mRNA levels compared with ARE. Thus, tilianin and ARE may have anti-adipogenic and anti-lipogenic effects on 3T3-L1 cells and be possible candidates of obesity-related supplements. [ABSTRACT FROM AUTHOR]

Postmenopausal obesity is becoming a serious global health concern. Soyasaponin Ab (SA) inhibits adipocyte differentiation; however, the preventive and therapeutic potential of SA in postmenopausal obesity has not been clearly established. Here, we investigated the anti-obesity effects of SA in postmenopausal obesity in vitro and in vivo. SA inhibited adipocytic differentiation of 3T3-L1 cells and reduced lipid accumulation and lipid droplet formation. Moreover, SA significantly decreased weight gain, adipocyte area, serum metabolic profiles in OVX mice. SA also inhibited the lipid metabolism-related factors but increased the thermoregulatory factors in both in vitro and in vivo. SA treatment further increased energy expenditure through beige fat activation. Overall, we found that SA effectively accelerated energy consumption by stimulating beige fat activation, even under estrogen-deficient conditions. Thus, SA treatment may be a promising strategy for the prevention of postmenopausal obesity by promoting weight loss, reducing fat accumulation, and improving obesity-related metabolic disorders.

Adipogenesis and angiogenesis are fundamental processes involved in growth and development. Adipocytes are highly vascularized tissues requiring continuous supply of nutrients, chemokines, cytokines and precursor cells during their expansion. Proangiogenic and antiangiogenic factors are expressed at different stages of adipocyte differentiation. Expression of angiogenic factors like VEGF in adipocyte suggests the possible role of angiogenesis in adipogenesis. Therefore, inhibitors that target angiogenesis has gained therapeutic relevance to control obesity. Apart from endogenous inhibitors, there are some natural foods that have adipostatic and angiostatic potential that will have limited side effects if consumed in proper dose. These foods have factors that elicit mechanisms like suppression of cell cycle progression, and inflammatory cytokines; deactivation of ERK, AKT, involvement of COX2 and NO pathway. In this review, we elaborate the role of some of the fruits (grapes, berries, citrus), vegetables and spices (spinach, crucifers, capsicum, onion, garic, turmeric, ginger) in adipogenesis and angiogenesis.

Red rice bran extract (RRBE) has been reported to have the potential for in vitro metabolic modulation and anti-inflammatory properties. However, little is known about the molecular mechanisms of these potentials in adipose tissue. This study aimed to evaluate the in vivo anti-adipogenic, anti-hypertrophic, and anti-inflammatory activities of RRBE and its major bioactive compounds in mice. After six weeks of consuming either a low-fat diet or a high-fat diet (HFD), 32 mice with initial body weights of 20.76 ± 0.24 g were randomly divided into four groups; the four groups were fed a low-fat diet, a HFD, a HFD plus 0.5 g/kg of RRBE, or a HFD plus 1 g/kg of RRBE, respectively. The 6-week treatment using RRBE reduced HFD-induced adipocyte hypertrophy, lipid accumulation, and inflammation in intra-abdominal epididymal white adipose tissue (p < 0.05) without causing significant changes in body and adipose tissue weight, which reductions were accompanied by the down-regulated expression of adipogenic and lipid metabolism genes, including CCAAT/enhancer-binding protein-alpha, sterol regulatory element-binding protein-1c, and hormone-sensitive lipase (p < 0.05), as well as inflammatory genes, including macrophage marker F4/80, nuclear factor-kappa B p65, monocyte chemoattractant protein-1, tumor necrosis factor-alpha, and inducible nitric oxide synthase (p < 0.05), in adipose tissue. Furthermore, RRBE significantly decreased serum tumor necrosis factor-alpha levels (p < 0.05). Bioactive compound analyses revealed the presence of phenolics, flavonoids, anthocyanins, and proanthocyanidins in these extracts. Collectively, this study demonstrates that RRBE effectively attenuates HFD-induced pathological adipose tissue remodeling by suppressing adipogenesis, lipid dysmetabolism, and inflammation. Therefore, RRBE may emerge as one of the alternative food products to be used against obesity-associated adipose tissue dysfunction.

The present study aims at demonstrating the anti-adipogenesis and anti-inflammatory of combination of extracts of commiphora wightti, curcuma longa, and tinospora cordifolia using mouse 3T3-L1 cells. Herbal formula (CCT) significantly suppressed the mRNA of PPARγ, leptin, and SREBP1c expression, which is reveals its significant anti-adipogenesis activity. In addition, CCT down-regulated TNFα and iNOS expression, this is an added advantage and helps to alleviate the inflammatory reactions during adipogenesis. These findings encourage for further studies using in vivo models of obesity and associated complications. [ABSTRACT FROM AUTHOR]

Obesity is spawned by an inequality between the portion of energy consumed and the quantity of energy expended. Disease entities such as cardiovascular disease, arteriosclerosis, hypertension, and cancer, which are correlated with obesity, influence society and the economy. Suppression of adipogenesis, the process of white adipocyte generation, remains a promising approach for treating obesity. Oil Red O staining was used to differentiate 3T3-L1 cells for screening 20 distinct Lactobacillus species. Among these, Lactobacillus acidophilus DS0079, referred to as YBS1, was selected for further study. YBS1 therapy decreased 3T3-L1 cell development. Triglyceride accumulation and mRNA expression of the primary adipogenic marker, peroxisome proliferator-activated receptor gamma (PPARγ), including its downstream target genes, adipocyte fatty acid binding protein 4 and adiponectin, were almost eliminated. YBS1 inhibited adipocyte differentiation at the early stage (days 0-2), but no significant difference was noted between the mid-stage (days 2-4) and late-stage (days 4-6) development. YBS1 stimulated the activation of p38 mitogen-activated protein kinase (p38 MAPK) during the early stages of adipogenesis; however, this effect was eliminated by the SB203580 inhibitor. The data showed that YBS1 administration inhibited the initial development of adipocytes via stimulation of the p38 MAPK signaling pathway, which in turn controlled PPARγ expression. In summary, YBS1 has potential efficacy as an anti-obesity supplement and requires further exploration.

Obesity is caused by excessive fat cells and the overgrowth of adipocytes and is a major risk factor for several chronic illnesses. Aronia melanocarpa fruit is rich in anthocyanins and polyphenols and has protective effects against various diseases. In this study, we examined the effect of Aronia extract (Aronia bioactive fraction, ABF®) on the biomarkers of the adipogenic pathway during adipocyte differentiation of 3T3-L1 cells. Lipid accumulation was verified by Oil Red O staining. mRNA and protein expression of lipoprotein lipase (LPL), CCAAT/enhancer-binding protein α (C/EBPα), peroxisome proliferator-activated receptor γ (PPARγ), fatty acid-binding protein 2 (FABP2), and fatty acid synthase (FAS) were assayed by RT-qPCR and Western blot analyses. Adiponectin and leptin secretion were measured using enzyme-linked immunosorbent assays. ABF® treatment downregulated lipid accumulation based on Oil Red O staining. ABF®-treated cells exhibited decreased mRNA and protein expression of LPL, C/EBPα, PPARγ, FABP2, and FAS. Moreover, ABF® treatment significantly increased adiponectin secretion and decreased leptin secretion. In conclusion, ABF® has anti-adipogenic effects on the differentiation of 3T3-L1 cells and may be used as an anti-obesity nutraceutical.

Agastache rugosa, or Korean mint, is an herb used as a spice, food additive and traditional medicinal ingredient. It has desirable effects, such as its antibacterial, antifungal and antioxidant properties. A. rugosa contains many phenolic compounds studied for their various health benefits, with the primary components being tilianin. A. rugosa extract (ARE), which was extracted with ethanol and freeze-dried, contained 21.14 ± 0.15 mg/g of tilianin with a total polyphenol content of 38.11 ± 0.88 mg/g. Next, the antiadipogenic effect of A. rugosa and tilianin was clarified using 3T3-L1 cells, which differentiate into adipocytes and develop lipid droplets. 3T3-L1 cells were treated with ARE or tilianin and lipid accumulation (%) was calculated through oil red O staining. Tilianin elicited dose-dependent decrease in lipid accumulation (% of positive control) (30 μM 92.10 ± 1.19%; 50 μM 69.25 ± 1.78%; 70 μM 54.86 ± 1.76%; non-differentiation 18.10 ± 0.32%), assessed by oil-red-O staining, whereas ARE treatments caused consistent diminution in lipid accumulation regardless of dose (100 μM 86.90 ± 4.97%; 200 μM 87.25 ± 4.34%; 400 μM 88.54 ± 2.27%; non-differentiation 17.96 ± 1.30%), indicating that both compounds have anti-obesity effects on adipocytes. Treatment with ARE lowered the mRNA (PPARγ; C/EBPα; FABP4; SREBP1; ACC; FAS) and protein (PPARγ; C/EBPα; SREBP1) levels of adipogenesis and lipogenesis-related factors. Tilianin showed a greater effect on the mRNA levels compared with ARE. Thus, tilianin and ARE may have anti-adipogenic and anti-lipogenic effects on 3T3-L1 cells and be possible candidates of obesity-related supplements.

Curcumin is a known anti-adipogenic agent for alleviating obesity and related disorders. Comprehensive comparisons of the anti-adipogenic activity of curcumin with other curcuminoids is minimal. This study compared adipogenesis inhibition with curcumin, demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC), and their underlying mechanisms. We differentiated 3T3-L1 cells in the presence of curcuminoids, to determine lipid accumulation and triglyceride (TG) production. The expression of adipogenic transcription factors and lipogenic proteins was analyzed by Western blot. A significant reduction in Oil red O (ORO) staining was observed in the cells treated with curcuminoids at 20 μM. Inhibition was increased in the order of curcumin < DMC < BDMC. A similar trend was observed in the detection of intracellular TG. Curcuminoids suppressed differentiation by downregulating the expression of peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα), leading to the downregulation of the lipogenic enzymes acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS). AMP-activated protein kinase α (AMPKα) phosphorylation was also activated by BDMC. Curcuminoids reduced the release of proinflammatory cytokines and leptin in 3T3-L1 cells in a dose-dependent manner, with BDMC showing the greatest potency. BDMC at 20 μM significantly decreased leptin by 72% compared with differentiated controls. Molecular docking computation indicated that curcuminoids, despite having structural similarity, had different interaction positions to PPARγ, C/EBPα, and ACC. The docking profiles suggested a possible interaction of curcuminoids with C/EBPα and ACC, to directly inhibit their expression.

Abstract Background Blood stasis syndrome (BSS) is a general pattern identification and refers to pathological stagnation of blood circulation, dysfunction of endothelial cells or metabolic disorder in traditional Korean medicine (TKM). Dohongsamul-Tang (DHSMT) is a well-known traditional herbal formula which used for treatment and prevention of BSS by promoting blood circulation in TKM. Methods Cytotoxicity of DHSMT was examined by cell counting kit-8 (CCK-8). We also investigated the anti-adipogenesis effect of DHSMT by using Oil Red O staining, intracellular triglyceride assay leptin ELISA and western blot analysis in 3T3-L1 adipocytes. In addition, the accumulation of adiponectin, resistin and plasminogen activator inhibitor-1 (PAI-1) were measured by magnetic bead panel kit. Results Oil Red O staining showed that DHSMT markedly reduced fat accumulation without affecting cell cytotoxicity. DHSMT also significantly decreased accumulation of triglyceride and adipokines such as leptin, adiponectin, resistin and PAI-1 compared with fully differentiated adipocytes. Furthermore, our results found that DHSMT significantly suppressed the adipocyte differentiation by downregulating adipogenic-specific transcriptional factors such as peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer binding proteins alpha (C/EBPα) and fatty acid binding protein 4 (FABP4) in adipocytes. Conclusions Taken together, our findings provide that DHSMT has potential for treatment and prevention of obesity or MS related to BSS.

This study examined the anti-obesity and anti-adipogenic effects of Antrodia cinnamomea. Oral administration of aqueous extract of A. cinnamomea (ACW) significantly reduced high-fat diet-induced body weight gain and relative perirenal and mesenteric fat weight in C57BL/6J mice. Administration of ACW significantly reduced serum insulin, leptin, aspartate aminotransferase levels, HOMA-IR index, and hepatic cholesterol and triacylglycerol levels. Next, investigation of whether ACW and its polysaccharides (PS) and non-polysaccharides (NPS) subfractions possess anti-adipogenic action was conducted. Evidence showed that ACW, PS and NPS significantly inhibited lipid deposits in 3T3-L1 adipocytes. Both ACW and NPS significantly inhibited mitotic clonal expansion process of adipocyte differentiation. ACW and NPS also significantly decreased the expressions of PPARγ, C/EBPα, aP2 and FAS genes, while PS markedly inhibited PPARγ and aP2 gene expression. Our data indicated that ACW inhibits preadipocyte differentiation and adipogenesis. These results suggested that ACW may have therapeutic potential for obesity and related metabolic disorders.

• Soyasaponin Ab is a soy bioactive compound that helps in the treatment of postmenopausal obesity. • Soyasaponin Ab inhibits adipogenesis and lipogenesis at both in vitro and in vivo levels. • Energy expenditure were increased by soyasaponin Ab trough beige fat activation as well as white fat browning. • Obesity-related metabolic disorders could be alleviated by Soyasaponin Ab treatment. Postmenopausal obesity is becoming a serious global health concern. Soyasaponin Ab (SA) inhibits adipocyte differentiation; however, the preventive and therapeutic potential of SA in postmenopausal obesity has not been clearly established. Here, we investigated the anti-obesity effects of SA in postmenopausal obesity in vitro and in vivo. SA inhibited adipocytic differentiation of 3T3-L1 cells and reduced lipid accumulation and lipid droplet formation. Moreover, SA significantly decreased weight gain, adipocyte area, serum metabolic profiles in OVX mice. SA also inhibited the lipid metabolism-related factors but increased the thermoregulatory factors in both in vitro and in vivo. SA treatment further increased energy expenditure through beige fat activation. Overall, we found that SA effectively accelerated energy consumption by stimulating beige fat activation, even under estrogen-deficient conditions. Thus, SA treatment may be a promising strategy for the prevention of postmenopausal obesity by promoting weight loss, reducing fat accumulation, and improving obesity-related metabolic disorders. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Adipostatic potential of fruits, vegetables and spices. • Angiostatic potential of fruits, vegetables and spices. • Involvement of COX2 and NO pathway. • These natural foods can be used as potent nutraceutical agents to modulate adipogenesis and angiogenesis. Abstract Adipogenesis and angiogenesis are fundamental processes involved in growth and development. Adipocytes are highly vascularized tissues requiring continuous supply of nutrients, chemokines, cytokines and precursor cells during their expansion. Proangiogenic and antiangiogenic factors are expressed at different stages of adipocyte differentiation. Expression of angiogenic factors like VEGF in adipocyte suggests the possible role of angiogenesis in adipogenesis. Therefore, inhibitors that target angiogenesis has gained therapeutic relevance to control obesity. Apart from endogenous inhibitors, there are some natural foods that have adipostatic and angiostatic potential that will have limited side effects if consumed in proper dose. These foods have factors that elicit mechanisms like suppression of cell cycle progression, and inflammatory cytokines; deactivation of ERK, AKT, involvement of COX2 and NO pathway. In this review, we elaborate the role of some of the fruits (grapes, berries, citrus), vegetables and spices (spinach, crucifers, capsicum, onion, garic, turmeric, ginger) in adipogenesis and angiogenesis. [ABSTRACT FROM AUTHOR]

Cirsium brevicaule A. GRAY is a wild perennial herb, and its roots (CbR) have traditionally been used as both food and medicine on the Japanese islands of Okinawa and Amami. The present study evaluated the antiadipogenic effect of CbR using mouse embryonic fibroblast cell line 3T3-L1 from JCRB cell bank. Dried CbR powder was serially extracted with solvents of various polarities, and these crude extracts were tested for antiadipogenic activity. Treatment with the methanol extract of CbR showed a significant suppression of lipid accumulation in 3T3-L1 cells. Methanol extract of CbR was then fractionated and subjected to further activity analyses. The phenylpropanoid glycosidic molecule syringin was identified as an active compound. Syringin dose dependently suppressed lipid accumulation of 3T3-L1 cells without cytotoxicity, and significantly reduced the expressions of peroxisome proliferator-activated receptor gamma, the master regulator of adipogenesis, and other differentiation markers. It was demonstrated that syringin effectively enhanced the phosphorylation of the AMP-activated protein kinase and acetyl-CoA carboxylase. These results indicate that syringin attenuates adipocyte differentiation, adipogenesis, and promotes lipid metabolism; thus, syringin may potentially serve as a therapeutic candidate for treatment of obesity.

The 50% ethanolic corn silk extracts (CSEs) derived from sweet (SP and SV) and waxy corn silk (KJ and KT) cultivars were investigated for their phytochemical compositions using HPLC-UV method, antioxidation using FRAP and DPPH assays and anti-obesity potential in 3T3-L1 adipocyte. Different major compositions among CSEs were manifested: flavonoids as quercetin glucoside derivatives and phenolics as ferulic acid in sweet CSEs, and phenolics as p-coumaric acid and derivatives of gallic acid in waxy CSEs. Related to high phytochemical contents, the antioxidant activity, anti-pre-adipocyte proliferation, anti-adipogenesis, and lipolysis induction in sweet CSEs were higher than in waxy CSEs. Moreover, significant correlations between phytochemical contents and anti-proliferation and anti-adipocyte differentiation were indicated in sweet CSEs. Interestingly, lipolysis induction was detected in both sweet and waxy CSEs. Conclusively, the anti-obesity potential of CSEs involving anti-adipogenesis and lipolysis induction is manifested in association with the composition of flavonoids and phenolics as the functional ingredient.

Due to the side effects of obesity medications, many studies have focused on the natural products used in the daily diet to control weight. Moringa seed pods and leaves are widely used as vegetables or diet supplements due to the high nutrition value. However, no bioactivity-guided anti-adipogenic study was previously conducted. Therefore, a preadipocyte cell line was adopted as the bioactivity assay to identify the anti-adipogenic compounds in the peeled Moringa seed. Two known sulphur-containing compounds (1 and 2) were isolated and identified. Compound 2, 4-(α-l-rhamnosyloxy) benzyl isothiocyanate, showed a great anti-adipogneic effect with an IC50 value of 9.2 μg/mL. The isothiocyanate (ITC) group in compound 2 could be responsible for the inhibitory activity. In addition, a series of compounds with the ITC group were used to further investigate the structure-activity relationship, indicating foods containing ITC derivatives have the potential of being used to control weight.

Soy isoflavones are popular ingredients with anti-adipogenic and anti-lipogenic properties. The anti-adipogenic and anti-lipogenic properties of genistein are well-known, but those of genistin and glycitein remain unknown, and those of daidzein are characterized by contrasting data. Therefore, the purpose of our study was to investigate the effects of daidzein, glycitein, genistein, and genistin on adipogenesis and lipogenesis in 3T3-L1 cells. Proliferation of 3T3-L1 preadipocytes was unaffected by genistin and glycitein, but it was affected by 50 and 100 µM genistein and 100 µM daidzein for 48 h. Among the four isoflavones, only 50 and 100 µM genistin and genistein markedly suppressed lipid accumulation during adipogenesis in 3T3-L1 cells through a similar signaling pathway in a dose-dependent manner. Genistin and genistein suppress adipocyte-specific proteins and genes, such as peroxisome proliferator-activated receptor γ (PPARγ), CCAAT-enhancer-binding protein α (C/EBPα), and adipocyte binding protein 2 (aP2)/fatty acid-binding protein 4 (FABP4), and lipogenic enzymes such as ATP citrate lyase (ACL), acetyl-CoA carboxylase 1 (ACC1), and fatty acid synthase (FAS). Both isoflavones also activate AMP-activated protein kinase α (AMPKα), an essential factor in adipocyte differentiation, and inhibited sterol regulatory element-binding transcription factor 1c (SREBP-1c). These results indicate that genistin is a potent anti-adipogenic and anti-lipogenic agent.

Mastoparan B (MP-B), a cationic tetradecapeptide isolated from the venom of the Vespa basalis, exhibits cardiovascular effects, local edema and antibacterial activity. In this study, the anti-adipogenic effect of an MP-B analogue and its mechanism of action in 3T3-L1 preadipocytes were studied. The MP-B analogue (MP-B12) inhibited preadipocyte differentiation and decreased the expression of adipogenic transcription factors, including CCAAT/enhancer binding protein-alpha (C/EBPα), nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) and sterol regulatory element-binding protein-1 (SREBP-1). Moreover, MP-B12 regulated the phosphorylation of Akt and glycogen synthase kinase-3 beta (GSK-3β), both of which play a role in preadipocyte differentiation, in which insulin and certain growth factors stimulated adipogenesis. This study demonstrates that MP-B12 inhibits preadipocyte differentiation and the accumulation of lipid droplets in 3T3-L1 preadipocytes and could potentially be used to treat obesity. Video Clip of Methodology: 4 min 11 sec Full Screen Alternate

Obesity is associated with higher risks of developing diabetes and cardiovascular disease. Green tea, rich in polyphenolic compounds such as epigallocatechin gallate (EGCG) and epigallocatechin (EGC), has been shown to display anti-obesity effects. Houttuynia cordata leaves have also been shown to exhibit anti-obesity effects due to their chlorogenic acid content. Lactic acid bacteria are able to increase the production of polyphenolic compounds. This study aims to develop a novel anti-obesity fermentation product by combining H. cordata leaf tea with green tea, using Lactobacillus paracasei subsp. paracasei NTU 101 (NTU 101) for fermentation due to the advantages of bioconverting the polyphenolic compounds. The regulation of adipogenesis factors and the anti-obesity effect of the NTU 101-fermented tea were evaluated in an in vitro 3T3-L1 pre-adipocyte model and an in vivo obese rat model, respectively. The results show that the NTU 101-fermented tea, which contained higher EGCG, EGC, and chlorogenic acid levels than unfermented tea, was able to inhibit the lipogenesis of mature 3T3-L1 adipocytes by the stimulation of lipolysis. Furthermore, the body weight gain, body fat pad, and feeding efficiency of obese rats, induced with a high fat diet, were decreased by the oral administration of NTU 101-fermented tea. The significant anti-obesity effect was probably due to lipolysis. However, NTU 101 bacteria cells and EGCG may also act as functional ingredients to contribute to the anti-obesity effects of NTU 101-fermented products. [ABSTRACT FROM AUTHOR]

Abstract: Ramulus mori is known as a medical herb for improving health. The antioxidant and anti‐obesity effects of an ethanolic extract of R. mori containing oxyresveratrol (ERM) were investigated. The antioxidant activity of ERM was determined by in vitro chemical‐ and cell‐based methods. ERM showed high antioxidant activities. In particular, ERM showed a high scavenging activity for peroxyl radicals in both chemical‐ and cell‐based assays. To investigate the inhibitory effect of ERM on adipogenic differentiation, 3T3‐L1 cells were treated with ERM (20, 30, and 40 μg/mL) for 8 days during induction of differentiation. ERM significantly suppressed lipid accumulation in 3T3‐L1 adipocytes and decreased expression levels of adipogenic genes peroxisome proliferator‐activated receptor gamma (PPARγ), CCAAT/enhancer‐binding proteins alpha (C/EBPα), and sterol regulatory element‐binding protein 1 (SREBP1). ERM also induced G0/G1 phase arrest in 3T3‐L1 adipocytes during mitotic clonal expansion (MCE). The results suggest that ERM possesses anti‐adipogenic activity and antioxidant property. Practical applications: Ramulus mori, a branch of Morus alba L., has been used as a traditional herb tea in Asia and is approved as a food source in South Korea, indicating it is safe. An ethanolic extract of R. mori containing oxyresveratrol (ERM) significantly suppresses lipid accumulation in 3T3‐L1 adipocytes and inhibits adipogenesis. ERM shows a strong antioxidative activity. Adipogenesis is the process of adipocyte differentiation, which leads to lipid accumulation in obesity. Obesity is one of metabolic disorders and a major risk factor for various chronic diseases. Additionally, antioxidants can protect cells from damage caused by free radicals. Therefore, ERM could be developed as a health functional food to prevent obesity and many diseases caused by oxidative damage. [ABSTRACT FROM AUTHOR]

Among several metabolic disorders, the pathogenesis of insulin resistance is considered to be multifactorial. Raffinose, an oligosaccharide isolated from the rhizome of Costus speciosus showed ≤50% inhibition of lipid accumulation in differentiated HepG2 and 3T3-L1 cells through exhibiting partial agonism to PPARγ, and, an enhanced secretion of adiponectin in 3T3-L1 adipocytes. Raffinose was also observed to attenuate the expression of SREBP1c, ACC and FAS which are involved in the fatty acid synthesis. A corresponding upregulation of PPARα and ACO involved in fatty acid oxidation was observed in steatotic HepG2 hepatocytes and 3T3-L1 adipocytes. In vitro evaluation of its anti-diabetic potential showed a dose dependent enhancement of glucose uptake. Investigation of the insulin sensitizing efficacy of Raffinose revealed an increase in Glut4 translocation via phosphorylation of IRβ/PI3K/Akt in differentiated L6 myocytes and 3T3-L1 preadipocytes. In addition, Raffinose was potentially involved in glycogen synthesis by inhibiting the activation of GSK3β. Hence, Raffinose could be a useful therapeutic agent for metabolic maladies. [ABSTRACT FROM AUTHOR]

The objective of the present study was to evaluate the effects of water-extracted plum (WEP) on adipocyte differentiation, adipogenesis and inflammation in differentiated 3T3-L1 adipocyte cells. WEP was assessed for basic analyses, including high-performance liquid chromatography, total phenolic and flavonoid content and antioxidant activity [1,1-diphenyl-2-picrylhydrazyl (DPPH) assays] in vitro. Moreover, the cell viability was measured using an MTT assay. Adipogenesis and lipid accumulation in 3T3-L1 adipocytes was investigated using Oil Red O staining, and the expression of genes and proteins associated with adipogenesis and lipolysis were examined by reverse transcription polymerase chain reaction and western blotting. In addition, sulforaphane using a positive control was performed simultaneously. The WEP significantly suppressed adipocyte differentiation and lipid accumulation in differentiated adipocytes without cytotoxicity. WEP resulted in direct anti-obesity effects through the modulation of adenosine monophosphate-activated protein kinase, sterol regulatory element-binding protein 1c, cytidine-cytidine-adenosine-adenosine-thymidine/enhancer binding protein α and peroxisome proliferator-activated receptor γ. These regulations of molecular expressions were significantly activated via the phosphoinositide 3-kinase/Akt pathway. Moreover, these results provide potential anti-adipogenic effects of WEP and may have potential as a natural agent for the prevention and improvement of obesity. [ABSTRACT FROM AUTHOR]

This study examined the anti-obesity and anti-adipogenic effects of Antrodia cinnamomea . Oral administration of aqueous extract of A. cinnamomea (ACW) significantly reduced high-fat diet-induced body weight gain and relative perirenal and mesenteric fat weight in C57BL/6J mice. Administration of ACW significantly reduced serum insulin, leptin, aspartate aminotransferase levels, HOMA-IR index, and hepatic cholesterol and triacylglycerol levels. Next, investigation of whether ACW and its polysaccharides (PS) and non-polysaccharides (NPS) subfractions possess anti-adipogenic action was conducted. Evidence showed that ACW, PS and NPS significantly inhibited lipid deposits in 3T3-L1 adipocytes. Both ACW and NPS significantly inhibited mitotic clonal expansion process of adipocyte differentiation. ACW and NPS also significantly decreased the expressions of PPARγ, C/EBPα, aP2 and FAS genes, while PS markedly inhibited PPARγ and aP2 gene expression. Our data indicated that ACW inhibits preadipocyte differentiation and adipogenesis. These results suggested that ACW may have therapeutic potential for obesity and related metabolic disorders. [ABSTRACT FROM AUTHOR]

Blood stasis syndrome (BSS), additionally called Eohyul, is a basic pathological concept in Traditional Korean Medicine. Do In Seung Gi‑Tang (DISGT) is herbal medicine used for the treatment of BSS. It primarily treats metabolic diseases (MDs) including obesity, hypertension, diabetes mellitus and gynecological diseases, by promoting blood circulation. The present study aimed to investigate the anti‑adipogenesis effect of DISGT in 3T3‑L1 adipocytes using Oil Red O staining, and assessing levels of triglycerides (TGs) and leptin in adipocytes by ELISA and western blot analysis. The results demonstrated that DISGT treatment had inhibitory effects on fat droplet formation, TG accumulation, leptin production and cytokine content, during 3T3‑L1 adipocyte differentiation, without affecting cell viability. Additionally, DISGT treatment significantly suppressed the protein expression levels of peroxisome proliferator‑activated receptor γ and CAAT/enhancer binding protein α. These results provide evidence that DISGT has anti‑adipogenesis effects on preadipocytes and adipocytes by significantly blocking adipocyte differentiation and lipid accumulation, and suppressing adipogenic gene expression. Therefore, the present study demonstrated the potential of DISGT as a therapeutic agent for the treatment of MDs. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Corn silk or the stigma of Zea mays L. has traditionally been used in weight loss stimulation and treatment of cystitis, urinary infections and obesity. Purple corn silk, rich of polyphenolic substances, was reported on anti-diabetic and anti-obesity effect in animal studies. However, scientific evidence on mechanisms and targets of action of purple corn silk related to adipocyte life cycle has been limited. Aim of study To determine phytochemical compositions and investigate anti-obesity potential of the purple corn silk focusing on interruption of adipocyte life cycle; effect on pre-adipocyte proliferation, adipogenesis, adipocyte lipolysis, and apoptosis. Materials and methods The ethanolic purple corn silk extract (PCS) was prepared and investigated for phytochemical compositions by LC/MS/MS technique and anti-obesity potential using murine 3T3-L1 cell line. Using methyl thiazole tetrazolium (MTT) assay, the effects on pre-adipocytes and adipocyte viability and on pre-adipocytes proliferation at 24-, 48-, and 72-h incubation period were evaluated. In addition, anti-adipogenesis via inhibition on adipocyte differentiation and reduction of total lipid accumulation was evaluated using Oil Red O staining and spectrophotometric methods, respectively. The lipolysis effect was determined by measurement of glycerol released content using glycerol test kit after 48-h treatment of PCS to adipocytes. Apoptosis inductive effect was done by using 2-(4-Amidinophenyl)-6-indolecarbamidine dihydrochloride (DAPI) staining method. Results The polyphenols including anthocyanins, quercetin and phenolic acids and derivatives were found as the major chemical compositions of the PCS. With multiple-stages interruption on the adipocyte life cycle, anti-obesity effect of PCS was interestingly demonstrated. When compared to the control, the PCS at concentration range between 250–1000 μg/mL showed anti-adipogenesis effect as expressing of significant inhibition on pre-adipocyte proliferation at all incubation period (43.52±5.28 – 75.51±9.09%) and significant decreasing of total lipid accumulation at concentration of 500 μg/mL (80.22±6.58%) and 1000 μg/mL (69.62±5.42%). Moreover, the PCS exhibited lipolysis and apoptosis inductive effect with dose dependent manner and significance at concentration of 1000 μg/mL by increase of released glycerol content (173.88±6.13% of the control) and of nuclei condensing and apoptotic bodies (with relative apoptosis induction as 131.74±1.64% of the control). Conclusion Our data has evidenced the anti-obesity potential of PCS related interruption at multiple stages of adipocyte life cycle. Its potency was attributed to inhibition on adipocyte proliferation and adipogenesis as well as induction on lipolysis and apoptosis at high concentration. However, further in vivo investigation should be considered to insist the possibility in applications of PCS in prevention and treatment of obesity. [ABSTRACT FROM AUTHOR]

Sobokchukeo-Tang (ST) is a well-known formula that is used for treating primary dysmenorrhea caused by blood stasis syndrome (BSS) in Korea and China. The current study investigated the anti-inflammatory and anti-adipogenesis effects of ST on adipocytes and macrophages. The anti-inflammatory efficacy of ST was evaluated in RAW 264.7 cells and differentiated THP-1 cells. To induce inflammation, the cells were treated with lipopolysaccharide (LPS; 1 μg/ml). Following the induction of inflammation, the levels of proinflammatory cytokines, interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in the cell supernatant were detected using enzyme-linked immunosorbent assay. 3T3-L1 preadipocytes differentiated into adipocytes in response to insulin, isobutyl-1-methylxanthine and dexamethasone (MDI). To confirm the anti-adipogenesis efficacy of ST, we investigated Oil Red O staining was performed, triglyceride (TG) and leptin secretion were measured, and the protein expression of lipid metabolism-associated factors was determined. ST significantly inhibited TNF-α and IL-6 production in the LPS-treated RAW 264.7 cells compared with LPS stimulation alone. In addition, the concentrations of IL-6 and TNF-α were significantly inhibited by ST in LPS-treated THP-1 cells. Lipid accumulation was reduced by ST, similarly to the positive control treatment, SB203580. In the ST-treated group, the TG and leptin concentrations were inhibited by up to 50 and 83%, respectively, compared with MDI induction only. The ST-treated group reduced the protein expression of peroxisome proliferator-activated receptor-γ and CCAAT/enhancer-binding protein α compared with MDI induction only. The results of the present study demonstrated that ST exerts anti-inflammatory effects on LPS-treated mouse and human macrophage cell lines. ST inhibited adipogenesis in MDI-induced 3T3-L1 adipocytes, as indicated by the significant reduction in TG and leptin concentrations without cytotoxicity. Thus, ST may be useful as a therapeutic agent for preventing lipid-associated diseases, including obesity and atherosclerosis. [ABSTRACT FROM AUTHOR]

This study aimed to describe the structural features and anti-adipogenesis effect of polysaccharides obtained from Lycium barbarum L. by a bioactivity-oriented purification method. First, crude polysaccharide LICP009 was identified as the main bioactive compound with potential inhibition of intracellular lipid accumulation. Bioactivity guided fractionation was further performed using ion-exchange chromatography and Sephadex G-50 to obtain the purified component LICP009-2-1. This component was mainly composed of arabinose (Ara), galactose (Gal), glucose (Glc), galacturonic acid (GalA), and glucuronic acid (GlcA) in a molar ratio of 40.2:31.5:4.2:5.8:5.7 with a molecular weight of 1.35 × 104 g/mol. Linkage and NMR data indicated that the backbone of LICP009-2-1 was consisted of a repeated unit of →3,6)-β-D-Gal p- (1→ residues, with three branches composed of α-L-Ara f -(1→, α-L-Ara f -(1 → 5)-α-L-Ara f -(1 → 5)-α-L-Ara f -(1 → 3)-β-D-Gal p -(1→, and α-L-Ara f -(1 → 2)-α-L-Ara f -(1→[4)-β-D-Gal p -(1] 3 →. In differentiated 3T3-L1 adipocyte model, LICP009-2-1 exhibited an antiadipogenic effect by decreasing lipid accumulation, as well as downregulating the expression of key transcription factors and proteins in the adipogenesis pathway in a dose-dependent manner. In high-fat-diet-induced obese mice, oral administration of LICP009-2-1 counteracted the progression of obesity and hyperlipidemia. These results indicated that LICP009-2-1 plays anti-adipogenic and anti-obesity roles both in vitro and in vivo , and could be an anti-obesity agent utilized as medicinal, pharmacological and functional food ingredient. • Polysaccharide from Lycium barbarum L. was studied by activity-oriented approach. • LBPs showed anti-adipogenesis activity in differentiated 3T3-L1 adipocytes and high-fat-diet-induced obese mice. • LICP009-2-1 with potential activity was mainly composed of.→3,6)-β-D-Gal p- (1 →. [ABSTRACT FROM AUTHOR]

Carduus crispus, native to Europe and Asia, is a traditional herbal medicine used for treating inflammatory disorders in Korea. Obesity is characterized by a state of chronic inflammation with increased inflammatory markers along with the expression and release of inflammation-related adipokines. Most anti-obesity drugs have been developed based on this concept. Our research for anti-obesity agents derived from C. crispus utilized the 3T3-L1 cell line. The methanol extract was initially screened and exhibited significant inhibition of adipogenesis in 3T3-L1 adipocytes. Among five liquid-liquid partition fractions, the ethyl acetate (EA) fraction showed the most potent suppressive effect compared with hexane, chloroform, n-butanol, and water. The EA fraction was considered for further study because of the presence of abundant polyphenols, including flavonoids. To isolate the active components from the EA fraction, elution-extrusion countercurrent chromatography was used. Among the seven fractions from the EA layer, fraction 6 inhibited lipid accumulation as well as CCAAT/enhancer-binding protein alpha and peroxisome proliferator-activated receptor gamma protein expression levels. The active component apigenin (fraction 6) was confirmed using high-performance liquid chromatography, electrospray ionization mass spectrometry, and one-dimensional nuclear magnetic resonance spectroscopy. The present data suggest that apigenin is one of the main bioactive compounds from C. crispus for inhibiting adipogenesis in 3T3-L1 adipocytes via the activation of AMP-activated protein kinase. [ABSTRACT FROM AUTHOR]

The article discusses the synthesis of combretastatin which isolated from the bark of Combretum caffrum. It examines the mechanism of action of the combretastatin with the aforementioned drugs such as trimethoxybenzene group. It also cites the structure of the combretastatin library which derived from combretastatins.