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Boesenbergia rotunda has been used as an antiobesity agent by suppressing adipogenesis. This study aimed to investigate the biological activity of B. rotunda on preadipocyte cells and to evaluate the effectiveness and safety of using B. rotunda extract in a capsaicin-loaded body-firming formulation. The antiadipogenesis of B. rotunda ethanolic extract was evaluated in 3T3-L1 preadipocyte cells. After the application of the B. rotunda extract-loaded body-firming formulation on the skin of volunteers for 28 d, thigh circumference, melanin index, and skin erythema were investigated. The results showed that the ethanolic extract of B. rotunda was not toxic toward 3T3-L1 cells at concentrations lower than 20 µg/mL, with antiadipogenesis of the B. rotunda extract occurring at a concentration of 1 µg/mL. The B. rotunda extract containing panduratin A was mixed with capsaicin body-firming products and successfully permeated into and through the skin. Applying this formulation to the thighs of the volunteers two times a day for 21 days led to a significant reduction in thigh circumference and melanin index. A slight elevation in skin erythema was observed, but there was no significant increase in redness or pain. In conclusion, the B. rotunda extract contained bioactive compounds that inhibited antiadipogenesis. The formulations containing B. rotunda extract and capsaicin showed potential as effective body-firming products. [ABSTRACT FROM AUTHOR]

In search of potential natural products for the amelioration of obesity, phytochemical investigation of leaves of Senna siamea Lam. was carried out. It led to the isolation of demethycassiarin B (1), 6,8-dihydroxy-3-methyl-1H isochromenone (2), and 6-hydroxymellein (3). The structures were elucidated by a detailed analysis of spectral data. Compound 1 was found to possess a similar structural skeleton as that of cassiarin B except for a methoxyl substitution. Detailed HPLC and HPTLC analysis of methanolic extract for the presence of compound 1 and cassiarin B were performed. Cassiarin B was not detected in extract. Compounds 2 and 3 have been reported for the first time from the genus Senna. The isolated compounds were evaluated for their antiadipogenic activity in murine 3T3L1 cells. [ABSTRACT FROM AUTHOR]

Cissus quadrangularis L. (CQ) has potential as a therapeutic for managing obesity and balancing metabolic activity, but the main bioactive compound and regulatory mechanism remain unknown. Herein, the CQ hexane extract was fractionated into 30 fractions (CQ-H) using flash column chromatography and analyzed using thin-layer chromatography. The direct antiadipogenesis effect of CQ-H fractions was tested on 3T3-L1 preadipocytes. Lupenone-rich fractions 2H and 3H were identified as containing potent antiadipogenesis agents that reduced differentiated cell numbers and intracellular lipid droplet size. Although the overall mitochondrial density remained unchanged, differentiated cells exhibited a higher mitochondrial density than that in non-differentiated cells. Additionally, 2H increased mitochondrial activity in both cell types as shown by their differentiation and lipid formation stages. Lupenone was isolated from 2H (Lu-CQ) and shown to dose-dependently inhibit adipogenesis, with 2H being more potent than Lu-CQ. Lu-CQ and 2H downregulated the expression of Pparg2 mRNA and upregulated that of glucose transporter genes, Slc2a1 and Slc2a4. Lu-CQ and 2H induced increased glucose uptake by 3T3-L1 cells. These findings suggest that lupenone-rich fractions in CQ contribute to balancing metabolic activity and reducing adipose tissue formation. Further exploration of CQ and its components may prompt innovative strategies for managing obesity and metabolic disorders. [ABSTRACT FROM AUTHOR]

Boesenbergia rotunda has been used as an antiobesity agent by suppressing adipogenesis. This study aimed to investigate the biological activity of B. rotunda on preadipocyte cells and to evaluate the effectiveness and safety of using B. rotunda extract in a capsaicin-loaded body-firming formulation. The antiadipogenesis of B. rotunda ethanolic extract was evaluated in 3T3-L1 preadipocyte cells. After the application of the B. rotunda extract-loaded body-firming formulation on the skin of volunteers for 28 d, thigh circumference, melanin index, and skin erythema were investigated. The results showed that the ethanolic extract of B. rotunda was not toxic toward 3T3-L1 cells at concentrations lower than 20 µg/mL, with antiadipogenesis of the B. rotunda extract occurring at a concentration of 1 µg/mL. The B. rotunda extract containing panduratin A was mixed with capsaicin body-firming products and successfully permeated into and through the skin. Applying this formulation to the thighs of the volunteers two times a day for 21 days led to a significant reduction in thigh circumference and melanin index. A slight elevation in skin erythema was observed, but there was no significant increase in redness or pain. In conclusion, the B. rotunda extract contained bioactive compounds that inhibited antiadipogenesis. The formulations containing B. rotunda extract and capsaicin showed potential as effective body-firming products.

Background: Obesity is among the most serious public health problems worldwide, with few safe pharmaceutical interventions. Natural products have become an important source of potential anti-obesity therapeutics. Dihydromyricetin (DHM) exerts antidiabetic effects. The biochemical target of DHM, however, has been unknown. It is crucial to identify the biochemical target of DHM for elucidating its physiological function and therapeutic value.Objectives: The objective of this study was to identify the biochemical target of DHM.Methods: An abundant antiadipogenic flavanonol was extracted from the herbal plant Ampelopsis grossedentata through bioassay-guided fractionation and characterized with high-resolution LC-MS and 1H and 13C nuclear magnetic resonance. Antiadipogenic experiments were done with mouse 3T3-L1 preadipocytes. A biochemical target of the chemical of interest was identified with drug affinity responsive target stability assay. Direct interactions between the chemical of interest and the protein target in vitro were predicted with molecular docking and subsequently confirmed with surface plasmon resonance. Expression levels of peroxisome proliferator-activated receptor γ (PPARγ), which is associated with 78-kDa glucose-regulated protein (GRP78), were measured with real-time qPCR.Results: DHM was isolated, purified, and structurally characterized. Cellular studies showed that DHM notably reduced intracellular oil droplet formation in 3T3-L1 cells with a median effective concentration of 294 μM (i.e., 94 μg/mL). DHM targeted the ATP binding site of GRP78, which is associated with adipogenesis. An equilibrium dissociation constant between DHM and GRP78 was 21.8 μM. In 3T3-L1 cells upon treatment with DHM at 50 μM (i.e., 16 μg/mL), the expression level of PPARγ was downregulated to 53.9% of the solvent vehicle control's level.Conclusions: DHM targets GRP78 in vitro. DHM is able to reduce lipid droplet formation in 3T3-L1 cells through a mode of action that is plausibly associated with direct interactions between GRP78 and DHM, which is a step forward in determining potential applications of DHM as an anti-obesity agent. [ABSTRACT FROM AUTHOR]

Some lactic acid bacteria (LAB) and their cellular components have antiobesity effects. In this study, we evaluated the antiadipogenic effects of a mixture of two LAB—Lactobacillus curvatus HY7601 and Lactobacillus plantarum KY1032—using 3T3-L1 preadipocytes and HepG2 hepatocarcinoma cells. 3T3-L1 cells treated with a 1:1 ratio of HY7601 and KY1032 during differentiation showed reduced lipid accumulation by Oil Red O staining, as well as decreased leptin secretion and mRNA expression of peroxisome proliferator-activated receptor-γ and CCAAT/enhancer binding protein-α. HY7601 and KY1032 treatment also suppressed mitochondrial biogenesis and inhibited the expression of genes encoding mitochondrial transcription factors, as well as those related to fatty acid synthesis in HepG2 cells. The antiadipogenic effects of LAB were associated with the cell membrane fraction. These results demonstrate that a mixture of two LAB (HY7601 and KY1032) inhibits adipogenesis in preadipocytes and liver cells and is a potential therapeutic strategy for the treatment of obesity. [ABSTRACT FROM AUTHOR]

The aim of the present study was to investigate the effects of AdipoRon, an adiponectin receptor agonist, on adipogenesis in C3H10T1/2 cells and to explore the underlying mechanisms. C3H10T1/2 cells were treated with increasing doses of AdipoRon for 8 days, and Oil Red O staining was used to assess lipid accumulation. The protein and mRNA expression levels of adipogenic transcription factors and adipocyte‑specific genes were examined by western blotting and reverse transcription quantitative polymerase chain reaction, respectively. AdipoRon treatment inhibited lipid accumulation in C3H10T1/2 cells in a dose‑dependent manner and significantly suppressed the expression of adipogenic transcription factors, including peroxisome proliferator‑activated receptor γ, CAAT/enhancer binding protein (C/EBP)‑β and C/EBPα. In addition, cells treated with AdipoRon exhibited a significant decrease in the expression of adipocyte‑specific genes, including fatty acid binding protein 4, fatty acid synthase, leptin, adiponectin, and stearoyl‑CoA desaturase‑1. Notably, AdipoRon significantly increased the phosphorylation of adenosine monophosphate‑activated protein kinase (AMPK) and acetyl‑CoA carboxylase (ACC). The results indicated that AdipoRon exerted an inhibitory effect on adipogenesis in C3H10T1/2 cells by downregulating the expression of adipogenic transcription factors and adipocyte‑specific genes and by promoting the phosphorylation of AMPK and ACC, which suggested that AdipoRon may be a potential drug to prevent and treat diseases caused by abnormal adipogenesis, such as obesity. [ABSTRACT FROM AUTHOR]

Boesenbergia rotunda (L.) Mansf contained a potent anti-obesity agent. The objectives of this study were to investigate the anti-adipogenesis and lipolysis effects of panduratin A from B. rotunda extract and develop extract-loaded lipolytic body microspicule (MS) serum. Panduratin A that was separated from the ethanolic extract of B. rotunda in fraction 3 (BP-3) were studied the bioactivity of 3T3-L1 preadipocyte cells. The extract-loaded MS serum was formulated and evaluated for safety and efficacy. The BP-3 extract containing panduratin A at 0.29 g per g of the extract was not toxic to the cells at concentrations lower than 10 µg/mL, and the antiadipogenesis and lipolysis effects of the BP-3 extract were strong at 10 µg/mL. To deliver bioactive panduratin A into and through the skin, MS serum was successfully formulated. Application of BP-3 extract-loaded MS serum to the human thigh for 14 d reduced the thigh circumference and increased skin hydration and firmness. Although the skin erythema was increased, no severe redness or pain was found. In conclusion, BP-3 extract acts as a potent bioactive compound to inhibit adipocyte cells, and the antiadipogenesis and lipolysis effects of BP-3 extract in MS serum might play an important role as a potential lipolytic body product for reducing human subcutaneous fat mass.

Ethanol extracts of Psoraleae semen (PSE) are used in Korean folk medicine for tuberculostasis, nycturia, sarcoma, inflammation, and cancer. We investigated the utility of P. semen extract for the suppression of angiogenesis and adipogenesis. Eighteen natural products were screened using anti-angiogenesis experiments, and one candidate product was identified. Psoraleae semen provided dosedependent inhibition of angiogenesis, adipogenesis, and cell adhesion in vitro and weight loss in mice in vivo. The anti-angiogenenic efficacy of PSE was superior to that of epigallocatechin gallate (EGCG) obtained from green tea leaves. The expression of angiogenesis and adipogenesisrelated signal molecules was reduced by increasing the doses of PSE. A diet supplemented with PSE provided more effective weight loss in LB mice than did orlistat, a representative synthetic diet drug, which also caused hairloss in LB mice. P. semen may be a useful antiadipogenic compound if these in vitro results are replicated under in vivo conditions. [ABSTRACT FROM AUTHOR]

Abstract: Dyslipidemia and insulin resistance are commonly associated with catabolic or lipodystrophic conditions (such as cancer and sepsis) and with pathological states of nutritional overload (such as obesity-related type 2 diabetes). Two common features of these metabolic disorders are adipose tissue dysfunction and elevated levels of tumour necrosis factor-alpha (TNF-α). Herein, we review the multiple actions of this pro-inflammatory adipokine on adipose tissue biology. These include inhibition of carbohydrate metabolism, lipogenesis, adipogenesis and thermogenesis and stimulation of lipolysis. TNF-α can also impact the endocrine functions of adipose tissue. Taken together, TNF-α contributes to metabolic dysregulation by impairing both adipose tissue function and its ability to store excess fuel. The molecular mechanisms that underlie these actions are discussed. [Copyright &y& Elsevier]

Obesity is a worldwide epidemic contributing to a higher risk of developing maladies such as type 2 diabetes, heart disease, and cancer. Shiya tea (leaves of Adinandra nitida), a traditional Chinese tea, is widely consumed due to its palatable flavor and various curative effects, such as reducing blood pressure and blood lipids, as well as anti-inflammation, etc. However, no relevant research on the antiobesity effects of Shiya tea has been reported. In particular, no health-benefiting compounds, other than flavonoids, in Shiya tea have been reported. Thus, 3T3-L1 preadipocytes have been used as a bioactivity-guided identification model to verify the inhibitory effects of Shiya tea on adipogenesis, as well as to identify antiadipogenic compounds. Four triterpenoid saponins (1-4), including one new compound (2α,3α-dihydroxyursolic acid 28- O-β-d-glucopyranosyl ester, compound 1), and a flavonoid (5) have been identified using NMR (1D and 2D NMR) and liquid chromatography (LC)-MS techniques. Compound 1, the major antiadipogenic constituent with an IC 50 value of 27.6 μg/mL, has been identified for the first time in Shiya tea. To understand the structure-activity relationship, three hydrolytic compounds (1s, 2s, and 5s) were obtained to provide an inhibitory effect on lipid accumulation during 3T3-L1 adipocyte differentiation. The inhibitory effect of the triterpenoid (1s) possessing no sugar group decreased significantly, while the flavonoid (5s) also without a sugar group showed increased activity. In addition, the hydroxyl group position may also play a role in inhibitory efficacy.

The pro-inflammatory response and recruitment of macrophages into adipose tissue contribute to metabolic dysfunction. Here, we reported the anti-inflammatory and antiadipogenic effects of the methanol (MeOH) extract and ethyl acetate (EtOAc) fraction of bamboo leaf and its molecular mechanism in RAW264.7 cells and 3T3-L1 adipocytes, respectively. Functional macrophage migration assays also were performed. Surprisingly, the EtOAc fraction of MeOH extracts from native Korean plant species Sasa coreana Nakai (SCN) has shown potent anti-inflammatory properties; SCN pretreatment inhibited nitric oxide (NO) production (p < 0.01) and inducible nitric oxide synthase (iNOS) expression in lipopolysaccharide (LPS)-stimulated macrophages. Inflammatory genes induced by LPS, including TNFα, IL-1β, and IL-6, were significantly attenuated by SCN (p < 0.01). Pretreatment with SCN antagonized NF-κB nuclear translocation and the simultaneous degradation of inhibitory κB protein. Furthermore, SCN selectively inhibited the LPS-induced phosphorylation of JNK (p < 0.01) and p38 (p < 0.05) but not ERK (p > 0.05). Similar to leaf extracts of other bamboo species, we identified that SCN contained several flavonoids including orientin, isoorientin, and vitexin; these compounds inhibited LPS-induced NO production (p < 0.05) and iNOS expression. In addition, SCN inhibited adipocyte differentiation in a dose-dependent manner, as demonstrated by Oil Red O staining and the protein expression of mature adipogenic marker genes. Treatment with the major flavonoids of SCN also inhibited adipogenesis. Furthermore, conditioned medium obtained from adipocytes stimulated macrophage chemotaxis, whereas medium from adipocytes treated with SCN significantly inhibited macrophage migration. Therefore, SCN is a potential therapeutic agent for the prevention of inflammation and obesity.