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Statistical Design of Sustained-Release Tablet Garcinia cambogia Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity.

ABSTRACT: Obesity is a major health concern worldwide, and it is leading to worsening disease morbidity and mortality. Herbal supplements and diet-based therapies have attracted interest in the treatment of obesity. It is known that Garcinia cambogia (GA) and mulberry leaf, which contain polyphenols, have anti-obesity activity. Herein, we developed a combined tablet consisting of GA extract and bioconverted mulberry leaf extract (BMUL) using a statistical design approach. The ratio and amount of sustained polymers were set as factors. In the cell study, the combination of GA and BMUL showed synergistic anti-obesity activity. In a statistical model, the optimized amounts of hydroxypropyl methylcellulose 2208 (HPMC 2208) and polyethylene oxide 303 (POLYOX 303) were 41.02% and 58.98%, respectively. Additionally, the selected ratio of microcrystalline cellulose (MCC) was 0.33. When the release, hardness, and friability of the GABMUL tablet were evaluated, the error percentages of the response were lower than 10%. This indicates that the GABMUL tablet was successfully prepared.

SUBMITTER: Lee HJ

PROVIDER: S-EPMC7600061 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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Statistical Design of Sustained-Release Tablet <i>Garcinia cambogia</i> Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity.

Lee Hye-Jin HJ Na Young-Guk YG Han Mingu M Pham Thi Mai Anh TMA Lee Hyeonmin H Lee Hong-Ki HK Myung Chang-Seon CS Han Joo-Hui JH Kang Jong-Seong JS Kim Kyung-Tae KT Cho Cheong-Weon CW

Pharmaceutics 20200929 10

Obesity is a major health concern worldwide, and it is leading to worsening disease morbidity and mortality. Herbal supplements and diet-based therapies have attracted interest in the treatment of obesity. It is known that <i>Garcinia cambogia</i> (GA) and mulberry leaf, which contain polyphenols, have anti-obesity activity. Herein, we developed a combined tablet consisting of GA extract and bioconverted mulberry leaf extract (BMUL) using a statistical design approach. The ratio and amount of su ...[more]

PMID: 33003619

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Project description:Obesity is a major global health problem which is associated with various diseases and psychological conditions. Increasing understanding of the relationship between obesity and gut microbiota has led to a worldwide effort to use microbiota as a treatment for obesity. However, several clinical trials have shown that obesity treatment with single strains of probiotics did not achieve as significant results as in animal studies. To overcome this limitation, we attempted to find a new combination that goes beyond the effects of probiotics alone by combining probiotics and a natural substance that has a stronger anti-obesity effect. In this study, we used a diet-induced obesity mouse (DIO) model to investigate the effects of combining Lactobacillus plantarum HAC03 with Garcinia cambogia extract, as compared to the effects of each substance alone. Combining L. plantarum HAC03 and G. cambogia, treatment showed a more than two-fold reduction in weight gain compared to each substance administered alone. Even though the total amount administered was kept the same as for other single experiments, the combination treatment significantly reduced biochemical markers of obesity and adipocyte size, in comparison to the treatment with either substance alone. The treatment with a combination of two substances also significantly decreased the gene expression of fatty acid synthesis (FAS, ACC, PPARγ and SREBP1c) in mesenteric adipose tissue (MAT). Furthermore, 16S rRNA gene sequencing of the fecal microbiota suggested that the combination of L. plantarum HAC03 and G. cambogia extract treatment changed the diversity of gut microbiota and altered specific bacterial taxa at the genus level (the Eubacterium coprostanoligenes group and Lachnospiraceae UCG group) and specific functions (NAD salvage pathway I and starch degradation V). Our results support that the idea that the combination of L. plantarum HAC03 and G. cambogia extract has a synergistic anti-obesity effect by restoring the composition of the gut microbiota. This combination also increases the abundance of bacteria responsible for energy metabolism, as well as the production of SCFAs and BCAAs. Furthermore, no significant adverse effects were observed during the experiment.

Project description:Background1-Deoxynojirimycin (DNJ), a component of mulberry leaf extract (MLE), reduces postprandial hyperglycemia by inhibiting intestinal a-glycosidase. The aim of this exploratory study was to investigate the effects of MLE on the glycemic indexes (GI) of common dietary carbohydrates.MethodsThis single-center, randomized, open-label, 7-cycle self-controlled crossover study enrolled 15 healthy volunteers at the National Drug Clinical Trial Institution, Second Affiliated Hospital of Tianjin University of Traditional Chinese Medicine (June 2014 to December 2014). The participants were randomized to receive glucose (3 occasions), glucose+MLE, sucrose+MLE, maltose+MLE, and maltodextrin+MLE orally during 7 visits (every 3 days). Blood glucose level was tested at 15 minutes before and at 15, 30, 45, 60, 90, and 120 minutes after carbohydrate intake. The GI of each carbohydrate relative to glucose (GI = 100) was calculated using the incremental area under the curve method. Safety was assessed at each visit.ResultsAll participants completed the protocol. After carbohydrate ingestion, blood glucose level peaked at 30 minutes (glucose, glucose+MLE, sucrose+MLE, and maltose+MLE) or 45 minutes (maltodextrin+MLE) before returning to preprandial levels at 120 minutes. At 30 minutes, the change in blood glucose level was lower for sucrose+MLE, maltose+MLE, and maltodextrin+MLE than for glucose or glucose+MLE (P < .05). GI was lowest for sucrose+MLE (43.22 ± 17.47) and maltose+MLE (49.23 ± 22.39), intermediate for maltodextrin+MLE (75.90 ± 26.01), and higher for glucose+MLE (91.88 ± 27.24). MLE reduced the GIs for maltose, sucrose, maltodextrin, and glucose by 53.11%, 33.51%, 31.00%, and 8.12%, respectively. MLE was well tolerated.ConclusionsCoconsumption of MLE with sucrose, maltose, or maltodextrin can reduce the GI values of these carbohydrates.Trial registrationChinese Clinical Trial Registry Platform, no. ChiCTR-IPR-15006484. Registered on May 28, 2015.

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Dataset Information

Statistical Design of Sustained-Release Tablet Garcinia cambogia Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity.

Publications

Statistical Design of Sustained-Release Tablet <i>Garcinia cambogia</i> Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity.

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