ABSTRACT
Two new lignan glucosides, tinsinlignans A and B (1 and 2), two new oxyneolignans, tinsinlignans C and D (3 and 4), along with one known analogue (5), were isolated from the stems of Tinospora sinensis. The structures of the new compounds were elucidated based on analysis of spectroscopic data, and the absolute configuration of 1 was determined through electronic circular dichroism (ECD) calculation based on the time-dependent density functional theory (TD-DFT). Compounds 1-4 were evaluated for their inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells and compounds 1 and 2 exhibited moderate inhibitory activities with IC
Subject(s)
Animals , Mice , Glucosides/pharmacology , Lignans/pharmacology , Lipopolysaccharides , Molecular Structure , Nitric Oxide , Phytochemicals/pharmacology , Tinospora/chemistryABSTRACT
OBJECTIVE: To investigate the effect of the 80% ethanol elution part of Tinospora sinensis macroporous resin extract on the expression of hippocampus proteome in Alzheimer′s disease (AD) model rats induced by D-galactose combined with Aβ2535. METHODS: The AD rats model replicated by D-galactose combined with Aβ2535, The AD rat model was replicated by D-galactose combined with Aβ2535, and randomly divided into sham operation group, model group, Donepezil group (donepezil, 6.0 mg•kg-1), and 80% extraction of Tinospora sinensi group (crude drug 6 g•kg-1). Donepezil group: donepezil 0.1 mL•10 g-1 ig. 80% extraction of Tinospora sinensi group: Tinospora sinensis effective part extraction 0.1 mL•10 g-1 ig. Model group and sham-operation group: physiological saline 0.1 mL•10 g-1 ig. Once a day, continuous administration for 15 d. Separating the hippocampus and extracting the protein, take the system test with nanol-ESI liquid-mass spectrometry, protein discovery software was used for identification, and qualitative analysis different groups of hippocampal proteins by SIEVE software. Take the GO analysis on differential protein with the ANTHER classification system and use IPAD to enrich the pathway. RESULTS: Compared with the model group, the drug-administered group had 66 differential proteins, including tubulin, heat shock proteins, energy metabolism-related proteins, vesicle production/transport related proteins, and brain protection-related proteins, which are closely related to AD. The above differential proteins involve a total of 21 signaling pathways. CONCLUSION: Tinospora sinensis may promote the synthesis and release of neurotransmitters by up-regulating clathrin and vesicle-forming transport and neurotransmitter release, and improve the function of cholinergic function in the brain to achieve the pathological process of AD.
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Objective:To isolate the chemical constituents from lipid-soluble parts of Tibetan Tinospora sinensis and identify the structure of the monomer compounds. Method:Eighty kg of dried rhizomes of T. sinensis were soaked by 80% ethanol (5 times of the dose of crude drug) for 1 hour, boiled under reflux for 1 hour,then and filtered. The above steps were repeated. The two extracts were combined,and the solvent was recovered to obtain a total extract. The obtained extract was extracted with a conventional solvent,and the solution was recovered to obtain petroleum ether extract,methylene chloride extract,ethyl acetate extract,n-butanol extract and water extract. Methylene chloride extract was isolated and purified by silicagel column chromatography,semi-preparative liquid chromatography and SephadexLH-20 chromatography; the chemical structure was identified on the basis of ESI-MS,nuclear magnetic resonance (1H-NMR and 13 C-NMR) spectroscopy data and literatures. Result:Fifteen compounds were isolated and identified respectively as n-dodecanol (1),n-hexacosanol (2),palmitic acid (3),dibutyl phthalate (4),vanillic acid (5),vanillin (6),apocynin (7),tinocordifolioside (8),medioresinol (9),isolariciresinol (10),aurantiamide (11),aurantiamide acetate (12),berberine (13),daucosterol (14),β-sitosterol (15). Conclusion:Except for 3,4,6,14,15,the other 10 compounds were isolated from the plant for the first time.
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Objective To study the chemical constituents and anti-neuroinflammatory activity of the caulis of Tinospora sinensis as a "Yao" medicine. Methods The chemical constituents were isolated and purified by silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. The structures of these compounds were elucidated by extensive spectroscopic analyses and chemical methods. All compounds were evaluated for their anti-neuroinflammatory effect by inhibiting the nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine BV-2 microglial cells except for compounds 7 and 8. Results Thirteen compounds were isolated from the caulis of T. sinensis. They were identified as tinosposide C (1), tinosposide D (2), seco-isolariciresinol 9-O-β-glucopyranoside (3), (+)-pinoresinol 4-O-β-D-glucopyranoside (4), (+)-syringaresinol (5), tanegoside A (6), (E)-3-[(2,3-trans)-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-2,3-dihydrobenzo [b] [1,4]dioxin-6-yl]-N-(4-hydroxyphenethyl) acrylamide (7), thoreliamide B (8), trans-N-p-coumaroyltyramine (9), N-trans-feruloyltyramine (10), N-trans-caffeoyltyramine (11), grossamide K (12), and cis-grossamide K (13), seven of which exhibited significant anti-neuroinflammatory activity with IC50 values ranging from 1.46 to 51.25 μmol/L. Conclusion Compounds 1 and 2 are new compounds and their absolute configurations are confirmed by ECD experiments, compounds 3, 5, 7, 8, and 10-13 are isolated from the plants for the first time. The activity of compounds 9 and 10 is better than positive control minocycline.
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AIM To study the chemical constituents from Tibetan medicine Tinospora sinensis (Lour.)Merr..METHODS The ethyl acetate fraction of ethanol extract from T.sinensis was isolated and purified by silica,Sephadex LH-20,preparative HPLC column and recrystallization,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Nine compounds were isolated and identified as rutin (1),quercetin (2),kaempferol (3),luteolin (4),myricetin (5),paeonol (6),N-cisferuloyltyramine (7),myricetin-3-O-β-D-glucopyranoside (8),quercetin-3-O-α-L-rhamnoside (9).CONCLUSION All the compounds are isolated from this plant for the first time.
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AIM To study the chemical constituents from Tibetan medicine Tinospora sinensis (Lour.)Merr..METHODS The ethyl acetate fraction of ethanol extract from T.sinensis was isolated and purified by silica,Sephadex LH-20,preparative HPLC column and recrystallization,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Nine compounds were isolated and identified as rutin (1),quercetin (2),kaempferol (3),luteolin (4),myricetin (5),paeonol (6),N-cisferuloyltyramine (7),myricetin-3-O-β-D-glucopyranoside (8),quercetin-3-O-α-L-rhamnoside (9).CONCLUSION All the compounds are isolated from this plant for the first time.
ABSTRACT
Guduchi has been widely used in the traditional medicine as an immunomodulator. Description of guduchi in Ayurvedic literature resemble with T. sinensis rather than with commonly available T. cordifolia and hence this may be used as substitutes for T. sinensis. T. cordifolia growing on Azadirachta indica commonly called Neem-guduchi has more immunomodulatory potential. Thus, immunomodulatory activity of three Tinospora spp. was assessed by checking humoral and cell mediated immune responses to the antigenic challenges with sheep RBCs and by neutrophil adhesion tests on albino Wistar rats using Guduchi-Satwa, a well known dosage form. Results revealed that Neem-guduchi possesses higher immunomodulatory potential at the dose of 300 mg/kg, po and validated the traditional claim. Hence, Neem-Guduchi can be employed in immunomodulatory formulation prepared using guduchi.
Subject(s)
Animals , Azadirachta/chemistry , Azadirachta/growth & development , Immunomodulation , Neutrophils/drug effects , Neutrophils/immunology , Phagocytosis/drug effects , Phagocytosis/immunology , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Plant Extracts/immunology , Rats , Tinospora/chemistry , Tinospora/immunologyABSTRACT
Aims: Aim of this study was to evaluate the comparative efficacy of Tinospora cordifolia (Willd.) Miers ex Hook. F., Tinospora sinensis (Lour.) Merrill and T. cordifolia growing on Neem (Azadirachta indica A. Juss.) called Neem-guduchi. Study Design: Selected species have been widely used in the traditional medicine systems in various dosage forms to treat liver disorders. They are of common occurrence and are being used as substitutes to each other. There is no comparative hepatoprotection study yet published, therefore, present study has carried out. Place and Duration of Study: Interactive Research School for Health Affairs, Pune and Amrutvahini College of Pharmacy, Sangamner, between November 2011 and August 2012. Methodology: Guduchi-Satwa, a well-known dosage form was prepared according to the traditional procedure. Hepatoprotective potential was assessed using paracetamolinduced hepatotoxicity model in rats and evaluated by using biochemical parameters viz. alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) and total bilirubin (BIL). Results: Both T. cordifolia and T. sinensis Satwa significantly reduced the paracetamol induced elevated levels of serum ALT, AST, ALP and BIL at dose of 200 mg/kg, i.p. as compared to Neem-guduchi. Conclusions: Satwa preparation form of T. sinensis offers exploitable level of hepatoprotection potential.