Background. Currently, obesity and its comorbidities have become a serious threat to human health necessitating urgent development of safe and effective therapy for their management. Materials and Methods. In this research, a novel polyherbal formulation (F2) was prepared by mixing specific proportions of royal jelly and lemon juice with ethanol extracts of Orostachys japonicus, Rhus verniciflua, and Geranium thunbergii. The antioxidant activity was assessed using DPPH and ABTS assay methods. The antiobesity potential of the F2 was assessed in vitro using 3T3-L1 fibroblast and in vivo using a high-fat diet (HFD) fed C57BL/6J mice model. F2 was administered in mice at the dose of 23 mg/kg and 46 mg/kg, twice daily by oral gavage. A well-accepted antiobesity agent, Garcinia cambogia (GC), at 200 mg/kg was used as a positive control. Results. F2 was observed to exhibit synergistic antiadipogenic activity in 3T3-L1 cells. This inhibition was reinforced by the downregulation of specific adipogenic transcription factors. Furthermore, F2 was also found to reduce mice body weight gain, food efficiency ratio, fasting blood glucose level, fat deposition into the liver, and mass of white adipose tissue. F2 also played a role in the excretion of fat consumed by the mice. For most of the assays performed, the F2 (46 mg/kg) was comparable to the positive control GC (200 mg/kg). In addition, potential and synergistic antioxidant activity was observed on F2. Conclusion. The results revealed that the formulation F2 exhibited potential antiobesity activity through the inhibition of adipocyte differentiation, dietary fat absorption, and reduction of free fatty acids deposition in tissues.

BackgroundRoyal jelly (RJ) has been used traditionally for dietary, cosmetic and health purposes for a long time in different parts of the world. Scientific studies have also shown its numerous health-promoting properties including hypoglycemic and anti-hypercholesterolemic action. In this study, we investigated the anti-adipogenic activity of RJ in 3 T3-L1 cells and isolated the major responsible root component for the activity.MethodsAn active anti-adipogenic compound was isolated through bioassay-guided isolation process by successive treatment of RJ and its active fractions on 3 T3-L1 cell line. (E)-10-Hydroxy-2-decenoic Acid (10-HDA) was identified using NMR spectroscopy and ultra-performance liquid chromatography (UPLC). As 10-HDA showed significant anti-adipogenic activity with Oil Red O staining and TG content assay on 3 T3-L1 adipocytes, further study was carried out in molecular level for the expression of adipogenic transcription factors such as PPARγ, FABP4, C/EBPα, SREBP-1c, and Leptin. The effect of 10-HDA on preliminary molecules such as pAkt, pERK, C/EBPβ, and pCREB were studied in the early stage of adipogenesis. The effect of 10-HDA on reactive oxygen species (ROS) production in fully differentiating adipocytes was measured by nitro blue tetrazolium (NBT) assay.ResultResults showed that triacylglycerol accumulation and ROS production was markedly suppressed by 10-HDA. Preliminary molecules such as pAkt, pERK, pCERB, and C/EBPβ were found to be down-regulated by 10-HDA, which led to down-regulation of key adipogenic transcription factors such as PPARγ, FABP4, CEBPα, SREBP-1c, and Leptin on 3 T3-L1 adipocytes.ConclusionOur results suggest that anti-adipogenesis of 10-HDA on 3 T3-L1 adipocyte takes place via two mechanisms: inhibition of cAMP/PKA pathway and inhibition of p-Akt and MAPK dependent insulin signaling pathway. So it is considered that 10-HDA, a major component of RJ, can be a potential therapeutic medicine for obesity.Electronic supplementary materialThe online version of this article (10.1186/s12906-018-2423-2) contains supplementary material, which is available to authorized users.

Sulfuretin is a natural flavonoid found in the plant

Obesity is a life-threatening metabolic disorder necessitating urgent development of safe and effective therapy. Currently, limited such therapeutic measures are available for obesity. The present study was designed to develop a novel, safe and effective herbal therapy for the management of obesity. A polyherbal formulation (18KHT01) was developed by homogeneously mixing a specific proportion of crude Quercus acutissima (acorn jelly powder), Camellia sinensis (dry leaf buds), and Geranium thunbergii (dry aerial part) along with Citrus limon (fruit juice). Synergistic antioxidant, antiadipogenic, and anti-obesity activities were evaluated by in vitro as well as in vivo studies. In vitro experiments revealed strong synergistic antioxidant and anti-adipogenic activities of 18KHT01. Molecular assessment of 18KHT01 showed significant down-regulation of vital adipogenic factors such as PPARγ, C/EBPα, aP2, SREBP-1c, FAS, and LPL. Based on the results of the preliminary toxicity study, 75 and 150 mg/kg, twice daily doses of 18KHT01 were administered to evaluate anti-obesity activity in diet-induced obese (DIO) C57BL/6J mice model. The major obesity-related parameters such as body weight, weight gain, food efficiency ratio, as well as serum lipid profile were significantly reduced by 18KHT01 with potential synergism. Also, the high-fat diet-induced insulin resistance was suggestively alleviated by the formulation, and thus ameliorated fasting blood glucose. Histological evaluation of liver and white adipose tissue revealed that the significant reduction of fat depositions and thus reduction of these tissue weights. Synergy evaluation experiments exhibited that the 18KHT01 offered strong synergism by improving efficacy and reducing the toxicity of its ingredients. Overall results evidenced the 18KHT01 as a safe and potent anti-obesity herbal therapy.

Myrrh essential oil (MEO) is widely used as remedies for the different human ailment in different parts of the world. The misuse of this natural product in higher doses may lead to fever, inflammation, and liver and kidney problems. In this study, we performed the acute and subacute toxicity analysis of MEO in mice model after subcutaneous injection and evaluated the safe dose to prevent the possible risk and side effects. Initially (first phase study) higher dose of MEO (20, 40, and 80 μL) was injected, and later in the second phase study lower dose of MEO (1, 5, and 10 μL) was injected for three days in each group of mice. Blood samples were taken for the investigation of hematological parameters and activity of various enzymes. The liver, kidney, spleen, lungs, and heart were excised for histological study. The body weight and skin abnormalities were also evaluated. In the first phase study, the mice showed granuloma formation at the site of injection. The liver showed dilated sinusoids and enlarged central vein. In the spleen the distinction between red and white pulp was lost. The kidney showed the degeneration of glomerulus. The enzyme activity and body weight were also decreased by the higher dose. The WBC count also increased nearly by twofold. Pruritus and self-trauma were also evident. Later in the second phase study, the skin abnormalities (granuloma) and damage in the structure of tissue (in liver, spleen, and kidney) were absent along with no change in enzyme levels, blood parameters, and body weight compared to the control. The MEO was toxic to liver, spleen, and kidney in the higher doses. The safe volume of MEO useful for various studies in mice was evaluated. The safe use of MEO should be assured, it should not be misused, being considered as a natural remedy, and there should be awareness of its toxicity and side effects.

Background: Ponciri Fructus, a crude drug consisting of the dried immature fruits of Poncirus trifoliata (L.) Raf., is a popular folk medicine used for the treatment of allergy and gastrointestinal disorders in Korea and China. In this study, the anti-adipogenic activity of extracts and isolated compounds were evaluated using 3T3-L1 preadipocytes. Methods: Dried immature fruits were extracted and fractionated into n-hexane, ethyl acetate (EtOAc), n-butanol and water-soluble fractions. The ethanol extract and fractions were tested for anti-adipogenic activity in the 3T3-L1 cell line. The active fractions (n-hexane and EtOAc fractions) were further subjected to chromatographic techniques to isolate and identify active compounds. Furthermore, the isolated compounds were evaluated for their anti-adipogenic activity. Results: Altogether, seven compounds, including two flavonoids, one phytosteroid and four coumarin derivatives, were isolated. Ethanol extract, n-hexane fraction, EtOAc fraction and three isolated compounds (phellopterin, oxypeucedanin and poncirin) showed significant anti-adipogenic activity as observed by reduced lipid deposition in differentiated 3T3-L1 cells. Further, oxypeucedanin downregulated the key adipogenic markers, such as peroxisome proliferator-activated receptors proteins γ (PPAR-γ), sterol response element binding proteins-1 (SREBP-1), CCAAT/enhancer binding proteins-α (C/EBP-α), adipocyte-specific lipid binding proteins (FABP-4), adipocyte fatty acid binding proteins (aP2), lipoprotein lipase (LPL) and leptin. Conclusion: This study indicated that the ethanol extract, hexane fraction and ethyl acetate fraction of P. trifoliata fruits possess strong anti-adipogenic activity, containing the active compounds such as phellopterin, oxypeucedanin and poncirin. Further research is recommended to explore their efficacy and safety in animal and clinical models.

Angiopteris helferiana C.Presl is a gigantic fleshy-type fern, belonging to Marattiaceae family. In previous study, we reported the potent anti-adipogenic and anti-inflammatory activities of ethylacetate (EtOAc) and n-butanol (BuOH) fractions of methanol extract of rhizomes of A. helferiana. In continuation, in this study, we report the isolation, characterization, and bioactivity analysis of principle bioactive compounds in these fractions. (−)-epi-Osmundalactone (1) and angiopteroside (2) were isolated from EtOAc and BuOH fractions, respectively. The structures of these compounds were established on the basis of NMR spectroscopic data. The quantification study using UPLC revealed the contents of compounds 1 and 2 in the dried rhizome to be 1.54% and 3.2%, respectively. These compounds were evaluated for their anti-adipogenic and anti-inflammatory activities using 3T3-L1 and RAW 264.7 cells, respectively. Compound 1 (2.5 µg/mL) and 2 (20 µg/mL) inhibited the lipid production by 35% and 25%, respectively. Regarding the anti-inflammatory activity, compound 1 (5 µg/mL) inhibited the nitrite production by nearly 82%. In conclusion, the presence of potent anti-adipogenic and anti-inflammatory compounds in A. helferiana indicate its potential role in the use of herb-based treatment for obesity and other related diseases.

Obesity and overweight have posed a severe threat to humanity, needing urgent efforts for the development of safe and effective therapeutic interventions. In this research work, we have developed two polyherbal formulations A and B basically consisting of Helianthus tuberosus root powder (also called inulin of synanthrin) along with other herbs for the treatment of obesity. Evaluation of the antioxidant activity of both formulations using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2 ′ -azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical scavenging assays showed good antioxidant potentials. Both formulations A and B showed good antiobesity activity on a diet-induced obesity (DIO) model of mice by effectively lowering the body weight of mice compared to the high-fat diet (HFD) control mice, mainly by reducing the food efficiency ratio (FER). Furthermore, both formulations ameliorated lipoprotein misbalances induced by obesity and thus decreased the atherogenic index. Treatment with both formulations significantly decreased the liver and epididymal white adipose tissue (WAT) weight. This was supported by the improvement in steatosis of the liver and reduced hypertrophy in WAT on histological examination. In addition, formulations A and B have been seen as effective in controlling fasting blood glucose levels probably by alleviating HFD-induced insulin resistance. All of these results collectively suggest that formulations A and B serve as potentially safe and effective herbal interventions to control obesity and its comorbidities.