• Natural Product Sciences
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• v.28 no.3
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• pp.105-114
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• 2022

Tinospora crispa (L.) is a medicinal plant traditionally used to treat various ailments including diabetes. The stem has been widely studied for its antidiabetic properties, however the antidiabetic potential of its leaves has not been explored. This study investigates the antidiabetic properties of methanolic T. crispa stem and leaves extracts on alloxan-induced diabetic rats. The stems and leaves were extracted using Soxhlet extraction with methanol as solvent. Crude extracts were administered at 500 mg/kg body weight (BW) (high dose) and 250 mg/kg BW (low dose) via oral route to alloxan induced diabetic rats. T. crispa stem and leaves extracts was found to significantly reduce blood glucose following a twelve-week treatment period. The highest mean difference in blood glucose level was exhibited by animals in the high dose treated stem and low dose leaf extracts. Both extracts showed approximately 75% percentage recovery from hyperglycaemia. The highest regenerative capacity was observed in animals treated with the low dose leaf extract.

• Journal of Applied Biological Chemistry
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• v.51 no.3
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• pp.111-116
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• 2008

Aralia elata seeds were successively extracted with water, methanol, ethanol, acetone and chloroform. The crude extracts were investigated for antioxidant and antidiabetic activities. The antioxidant properties of various extracts were evaluated by antioxidant tests, such as DPPH free radical-scavenging activity, hydroxyl radical-scavenging assay, metal-chelating activity, lipid peroxidation inhibition activity and reducing power assay. The 70% methanol extract exhibited the highest activity in the in vitro models of DPPH free radical-scavenging activity, metal-chelating activity, and reducing power assay. Acetone extract showed good effects on lipid peroxidation inhibition and hydroxyl radical-scavenging assay at a low concentration. In addition, the $\alpha$-glucosidase inhibition assay showed that 70% methanol extract had the highest activity. These results indicate the high possibility of using A. elata seeds for medical application due to their efficient antioxidant properties.

• Natural Product Sciences
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• v.29 no.2
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• pp.98-103
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• 2023

Sphaeranthus africanus is commonly used as a traditional remedy for sore throats and pain treatment in Vietnam. The aerial parts have been studied for its anti-inflammatory and anti-proliferative properties. However, the antioxidant and antidiabetic potential of the plant has not been explored. In this work, hydrophilic extracts of the plant's aerial parts were prepared in order to investigate its antioxidant and anti-diabetic properties. Also, the cytotoxicity of the root was evaluated and compared to that of the aerial parts. All of the extracts inhibited lipid peroxidation with IC₅₀ values ranging from 2.05 to 3.56 ㎍/mL, indicating substantial antioxidant activity. At an IC₅₀ value of 4.80 ㎍/mL, the 50% ethanol extract exhibited the most potent inhibition of α-glucosidase. The cytotoxic activity of root extracts is 2 to 5-fold less than that of the aerial parts. Nevertheless, dichloromethane and ethyl acetate extracts of the root demonstrated a selective effect on leukemia cells, with no harm towards the normal HEK-293 cell line. This work provides a scientific support for the antioxidant and antidiabetic activity of the plant. Hence, it may find a promising material for the development of novel antioxidant and antidiabetic agents. More research can be conducted on the phytochemistry and anticancer activities of the plant's root.

• 한국약용작물학회:학술대회논문집
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• 2010.10a
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• pp.416-417
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• 2010

• Biomolecules & Therapeutics
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• v.9 no.1
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• pp.63-68
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• 2001

General pharmacological properties of (R)-JG-381 were examined in laboratory animals to investigate its safety profile. Administration of (R)-JG-381 (50 and 100 mg/kg) in mice and rats had no effects of general behaviors, central nervous system of the animals in test systems of pentobarbital-induced sleeping time, writhing syndromes induced by 0.7% acetic acid, chemo-shock produced by pentylenetetrazole, and, however, had mild effects on motor coordination. Heart rate and blood pressure were not changed by (R)-JG-381 treatment. (R)-JG-381 also showed mild effects on intestinal propulsion and gastric secretion. These results suggest that (R)-JG-381 dose not exert serious pharmacological effects.

• Bulletin of the Korean Chemical Society
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• v.33 no.11
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• pp.3772-3776
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• 2012

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{\mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.224-230
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• 2001

DKY is an oriental drug preparation composed of 17 natural products and is known to have antihyperglycemic action at 100 mg/kg po in animal tests. The general pharmacological properties of DKY preparation were investigate in mice, rats, guinea pigs and rabbits. This preparation did neither show any effects on central nervous system, nor effects on algesia, nor epilepsia at the large doses of 3000 mg/kg po in mice or rats. However, the preparation showed hypothermic action at the doses of 330 and 1000 mg/kg po. In the guinea pig ileum, rat fundus strip and estrogenized rat uterus, DKY did not influence their tension at a concentration of 3$\times$10$^{-3}$ g/ml, and the spasmogenic actions produced by histamine, ACh and 5-HT were not blocked in the presence of DKY at 3$\times$10$^{-3}$ g/ml. The blood pressure and respiration were not considerably influenced at 10 mg/kg iv of DKY in rabbits. It did not influence the intestinal propulsion of mice and the normal gastric secretion of rats. These results may suggest that DKY preparation have little effects on central nervous, autonomic and gastrointestimal systems, except hypothermic action.

• Nutrition Research and Practice
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• v.15 no.5
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• pp.568-578
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• 2021

BACKGROUND/OBJECTIVES: Psidium guajava L. (guava) leaves have been shown to exhibit hypoglycemic and antidiabetic effects in rodents. This study investigated the effects of guava leaf extract on adipogenesis, glucose uptake, and lipolysis of adipocytes to examine whether the antidiabetic properties are mediated through direct effects on adipocytes. MATERIALS/METHODS: 3T3-L1 cells were treated with 25, 50, 100 ㎍/mL of methanol extract from guava leaf extract (GLE) or 0.1% dimethyl sulfoxide as a control. Lipid accumulation was evaluated with Oil Red O Staining and AdipoRed assay. Immunoblotting was performed to measure the expression of adipogenic transcription factors, fatty acid synthase (FAS), and AMP-activated protein kinase (AMPK). Glucose uptake under basal or insulin-stimulated condition was measured using a glucose analog 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-D-glucose. Lipolysis from fully differentiated adipocytes was measured by free fatty acids release into the culture medium in the presence or absence of epinephrine. RESULTS: Oil Red O staining and AdipoRed assay have shown that GLE treatment reduced lipid accumulation during adipocyte differentiation. Mitotic clonal expansion, an early essential event for adipocyte differentiation, was inhibited by GLE treatment. GLE inhibited the expression of transcription factors involved in adipocyte differentiation, such as peroxisome proliferator-activated receptor 𝛄 (PPAR𝛄), CCAAT/enhancer-binding protein α (C/EBPα), and sterol regulatory element-binding protein-1c (SREBP-1c). FAS expression was also decreased while the phosphorylation of AMPK was increased by GLE treatment. In addition, GLE increased insulin-induced glucose uptake into adipocytes. In lipid-filled mature adipocytes, GLE enhanced epinephrine-induced lipolysis but reduced basal lipolysis dose-dependently. CONCLUSIONS: The results show that GLE inhibits adipogenesis and improves adipocyte function by reducing basal lipolysis and increasing insulin-stimulated glucose uptake in adipocytes, which can be partly associated with antidiabetic effects of guava leaves.

• Journal of Pharmacopuncture
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• v.26 no.4
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• pp.319-326
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• 2023

Objectives: The study's goal was to find out whether Chrysanthemum rubellum extract has anti-diabetic properties by concentrating on α-glucosidase and the PTP-1B signaling pathway. C. rubellum flowers were used for extraction using Methanol/water (80/20) as solvent. Methods: LC-MS techniques was used to check the presence of phytoconstituents present in C. rubellum extract. In vitro antidiabetic activity was evaluated using α-glucosidase inhibitory activity and PTP-1B signaling pathway. On Streptozotocin (STZ)-induced rats with diabetes, the in vivo antidiabetic efficacy was assessed using a test for oral glucose tolerance. Results: The phytoconstituents identified in the extract of C. rubellum were apigenin, diosmin, myricetin, luteolin, luteolin-7-glucoside, and Quercitrin as compound 1-6, respectively. Results showed that diosmin exhibited highest α-glucosidase inhibitory activity i.e. 90.39%. The protein level of PTP-1B was lowered and the insulin signalling activity was directly increased by compounds 1-6. The maximum blood glucose levels were seen in all groups' OGTT findings at 30 minutes following glucose delivery, followed by gradual drops. In comparison to the control group, the extract's glucose levels were 141 mg/dL at 30 minutes before falling to 104 mg/dL after 120 minutes. The current study has demonstrated, in summary, that extract with phytoconstituents reduce blood sugar levels in rats. Conclusion: This finding suggests that extract may reduce the chance of insulin resistance and shield against disorders like hyperglycemia.

• Advances in Traditional Medicine
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• v.3 no.2
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• pp.84-89
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• 2003

The antidiabetic efficacy of Enicostemma littorale Blume (chhota chirayata) aqueous extract was examined in newly diagnosed non-insulin-dependent diabetes mellitus (NIDDM) patients taking only the extract and was administered as two divided doses, half an hour before meal as 5g of aqueous extract per single dose. Out of the 20 patients volunteered, 11 successfully completed the 2 month trial and a significant decrease in fasting & postprandial blood glucose and glycosylated haemoglobin levels were observed along with a significant improvement in the antioxidant parameters of the patients. There was also a significant increase in serum insulin levels in 7 patients after extract treatment as compared to levels before treatment. Serum total cholesterol and serum triglyceride levels were decreased significantly with a significant increase in serum HDLCholesterol levels. Other vital parameters remained stable and no side effects were observed. This is the first report showing the hypoglycemic, antioxidant and hypolipidemic properties of the aqueous extract of E. littorale Blume in non-insulin dependent diabetes mellitus patients.