Evaluation of Anti-Obesity and Antidiabetic Activities of Orostachys japonicus in Cell and Animal Models.

Orostachys japonicus is a popular traditional medicinal herb used in Asian countries. This study is focused on evaluating its role in lipid and glucose metabolism in cell and animal models to establish the plant as an anti-obesity and antidiabetic herb. A butanol fraction of O. japonicus was used in the study. The lipid production was evaluated by the Oil Red O technique while the expression of adipogenic markers by Western blotting and RT-PCR using 3T3-L1 preadipocyte. The effect on glucose uptake activity was evaluated in C2C12 myoblast cells. The animal study was carried out in C57BL mice to evaluate anti-obesity activity using the high-fat diet model. The evaluation of serum lipid, blood glucose, adipogenic and fibrosis markers in the liver, and fat deposition in the liver and adipose tissue (by histology) of mice was conducted. Butanol fraction of O. japonicus significantly inhibited the lipid production in the 3T3-L1 cells and reduced the expression of PPARγ, C/EBPα, SREBP-1c and aP2. It enhanced glucose uptake in insulin-resistant C2C12 myoblast cells. It reduced body weight, triglycerides, and blood glucose in the obese mice. It significantly inhibited lipid accumulation in the liver and adipose tissue of obese mice along with suppression of expression of adipogenic and fibrosis markers in the liver. In summary, supporting the previous results, this study helped to establish the potent anti-obesity, antidiabetic, and liver-protecting effect of the butanol fraction of O. japonicus.

Evaluation of Antioxidant and Anti-Inflammatory Activities, and Metabolite Profiling of Selected Medicinal Plants of Nepal.

This study aimed to evaluate the antioxidant, antiarthritic, and anti-inflammatory properties of extracts from the leaves of twelve different medicinal plants in Nepal. We then evaluated the total phenolic, flavonoid, and tannin contents of the extract using in-vitro assays and characterized it using GC-MS analysis. Results revealed that most of the leaf extracts contained phenolic compounds, flavonoids, tannins, alkaloids, and saponins. Few plants also showed the presence of glycosides, phytate, and vitamin C. Among the studied plants, Neolamarckia cadamba exhibited the highest total phenolic and tannin contents, as 241.53 ± 0.20 µg of gallic acid equivalent/mg and 74.48 ± 1.081 µg of tannic acid equivalent/mg, respectively. Ipomoea batatas exhibited the highest total flavonoid content, as 53.051 ± 1.11 µg of quercetin equivalent/mg. Moreover, Raphanus sativus demonstrated significant ferrous ion chelating, 2,2-diphenyl-1-picrylhydrazyl, hydrogen peroxide scavenging, and total antioxidant activities with IC50 value of 4.76 ± 0.68 µg/mL, 5.84 ± 0.14 µg/mL, 6.89 ± 0.16 µg/mL, and 8.99 ± 0.20 µg/mL, respectively. Similarly, Colocasia esculenta and Cicer arietinum exhibited the highest hydroxyl radical and nitric oxide scavenging activities, measuring IC50 value of 7.22 ± 0.56 µg/mL and 9.06 ± 0.10 µg/mL, respectively. Among all the extracts, Amorphophallus paeoniifolius displayed significant human red blood cell (HRBC) membrane stabilization activity (IC50 = 6.22 ± 0.78 µg/mL). Furthermore, Raphanus sativus, Chenopodium album, Cicer arietinum, and Murraya koenigii exhibited the highest inhibitory activities against protein denaturation with bovine serum albumin, antiarthritic, lipoxygenase inhibitory, and proteinase inhibitory, measuring IC50 of 7.48 ± 0.48 µg/mL, 9.44 ± 1.62 µg/mL, 14.67 ± 1.94 µg/mL, and 28.57 ± 2.39 µg/mL, respectively. In conclusion, this study demonstrated the twelve leaf extracts' significant antioxidant, antiarthritic, and anti-inflammatory activities.

Yellow Himalayan Raspberry (Rubus ellipticus Sm.): Ethnomedicinal, Nutraceutical, and Pharmacological Aspects.

Yellow Himalayan raspberry (Rubus ellipticus Sm., Rosaceae) is a native species of the Indian subcontinent, Southern China, and the Philippines, which has been historically used as a traditional medicine and food. All of the parts of this plant have been used in traditional medicine to treat respiratory ailments, diabetes, and gastrointestinal disorder, and as an anti-infective agent. The scientific evaluation revealed a richness of macronutrients, micronutrients, and minerals in the fruits, indicating its potential use as a nutraceutical. Furthermore, this plant has been found to be rich in various secondary metabolites, including polyphenols, flavonoids, anthocyanins, tannins, and terpenoids. Ascorbic acid, kaempferol, gallic acid, and catechin are some of the compounds found in this plant, which have been widely discussed for their health benefits. Furthermore, various extracts and compounds obtained from R. ellipticus have shown antioxidant, antidiabetic, anticancer, anti-inflammatory, nephroprotective, antipyretic, anticonvulsant, and anti-infective activities investigated through different study models. These findings in the literature have validated some of the widespread uses of the fruits in folk medicinal systems and the consumption of this nutritious wild fruit by local communities. In conclusion, R. ellipticus holds strong potential for its development as a nutraceutical. It can also improve the nutritional status of villagers and uplift the economy if properly utilized and marketed.

Screening of Antioxidant, Antibacterial, Anti-Adipogenic, and Anti-Inflammatory Activities of Five Selected Medicinal Plants of Nepal.

Introduction: Herbal products have been widely used for the treatment of diseases throughout the ages. In this research, we investigated antioxidant, antibacterial, anti-adipogenic, and anti-inflammatory activities of methanolic extracts of five ethnomedicinally important plants; namely, Alnus nepalensis, Dryopteris sparsa, Artocarpus lacucha, Litsea monopetala, and Lyonia ovalifolia. Methods: We investigated the DPPH free radical scavenging potential, sensitivity of selected bacterial strains towards the extracts using a disc diffusion assay, anti-inflammatory activity in RAW-264.7 cells, and anti-adipogenic activity by the ORO assay in 3T3-L1 preadipocytes. Results and discussion: The extract of A. nepalensis showed significant antioxidant activity (IC50=4.838 µg/mL), followed by A. lacucha, L. monopetala, and L. ovalifolia, exhibiting comparable IC50 values to that of ascorbic acid (IC50=5.063 µg/mL). Alnus nepalensis also showed good antibacterial activity in disc diffusion methods, with remarkable zones of inhibition in A. baumannii (14.66 mm) and P. mirabilis (15.50 mm) bacterial species. In addition, A. nepalensis was found to increase adipogenesis in 3T3-L1 cells, evidenced by increased lipid deposition in differentiated 3T3-L1 cells. A similar pattern of increased adipogenesis was observed on treatment with L. ovalifolia extracts. On the other hand, A. lacucha effectively reduced lipid deposition in 3T3-L1 cells at 100 µg/mL (75.18±6.42%) by inhibiting adipogenesis, showing its potential use in the management of obesity. Furthermore, A. lacucha 100 µg/mL (15.91±0.277 µM) and L. monopetala 75 µg/mL (12.52±0.05 µM) and 100 µg/mL (11.77±0.33 µM) significantly inhibited LPS-induced nitric oxide production in RAW 264.7 cells. Also, A. nepalensis and L. ovalifolia inhibited NO production significantly, endorsing their anti-inflammatory potential. Conclusion: The findings from these in-vitro studies suggest that the selected five plants possess remarkable antioxidant, antibacterial, anti-adipogenic, and anti-inflammatory activities. This study opens the door to conduct further advanced in-vivo experiments to find possible lead compounds for the development of valuable therapeutic agents for common health problems.

Anti-Obesity Potential of Ponciri Fructus: Effects of Extracts, Fractions and Compounds on Adipogenesis in 3T3-L1 Preadipocytes.

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.

Bioactive Chemical Constituents and Pharmacological Activities of Ponciri Fructus.

Ponciri Fructus is a crude drug obtained from the dried immature fruits of Poncirus trifoliata (L). Raf. (Syn. Citrus trifoliata L.). This study aims to compile and analyze the ethnomedicinal uses, bioactive constituents, and pharmacological activities of Ponciri Fructus. Various online bibliographic databases namely, SciFinder, PubMed, Google Scholar, and Web of Science were used for collecting information on traditional uses, biological activities, and bioactive constituents. Concerning ethnomedicinal uses, Ponciri Fructus is extensively used in traditional Korean, Chinese, and Kampo medicines to mitigate allergic reactions, inflammation, edema, digestive complications, respiratory problems, spleen-related problems, liver complications, neuronal pain, hyperlipidemia, rheumatoid arthritis, cardiovascular problems, hernia, sinusitis, and insomnia. Several studies have shown that Ponciri Fructus is a major source of diverse classes of bioactive compounds namely flavonoids, terpenoids, coumarins, phytosterols, and alkaloids. Several in vivo and in vitro pharmacological activity evaluations such as antidiabetic, anti-obesity, anti-inflammatory, antiallergic, antimelanogenic, gastroprotective, anticancer, and neuroprotective effects have been conducted from Ponciri Fructus. However, scientific investigations focusing on bioassay-guided isolation and identification of specific bioactive constituents are limited. Therefore, an in-depth scientific investigation of Ponciri Fructus focusing on bioassay-guided isolation, mechanism based pharmacological studies, pharmacokinetic studies, and evaluation of possible toxicities is necessary in the future.

Efficacy of a Novel Herbal Formulation (F2) on the Management of Obesity: In Vitro and In Vivo Study.

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.