Chinese Institute of Materia Medica

Beijing, China

Chinese Institute of Materia Medica

Beijing, China
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Bao X.-Q.,Chinese Institute of Materia Medica | Kong X.-C.,Chinese Institute of Materia Medica | Qian C.,Chinese Institute of Materia Medica | Zhang D.,Chinese Institute of Materia Medica
Neuroscience | Year: 2012

The pathogenesis of Parkinson's disease is characterized by progressive degeneration of dopaminergic neurons in substantia nigra (SNpc). FLZ, a novel synthetic squamosamide derivative from a Chinese herb, has been shown to have neuroprotective effects in experimental Parkinson's disease (PD) models. However, it is still unclear whether FLZ protects against PD through regulating the function of dopaminergic system. In this study, we carried out a set of in vitro and in vivo experiments to address these questions. Oral administration of FLZ significantly improved motor dysfunction of mice challenged by MPTP. The beneficial effects of FLZ on motor behavior attributed to the elevation of dopamine level in striatum, tyrosine hydroxylase (TH)-positive cells, and TH activity in the middle brain of mouse. Mechanism study showed that treatment of FLZ increased the phosphorylation of activating protein kinase B (Akt) and mammalian target of rapamycin (mTOR). Using LY294002 to block phosphoinositide 3-kinases (PI3K)/Akt signaling pathway prevented the phosphorylation of mTOR and attenuated the neuroprotection of FLZ in MN9D cells challenged by MPP +. In addition, FLZ reduced the expression of RTP801, an important protein in PD, in mice and cells intoxicated by MPTP/MPP +. Taken together, these results revealed a novel role that FLZ elevated TH expression and activity in dopaminergic neuron through activation of Akt/mTOR survival pathway and inhibition of RTP801 in MPTP/MPP +-induced PD models. The data also provided evidence that FLZ had potent neuroprotecive effects and might become a new promising anti-PD drug. © 2011 IBRO.


Shen Z.,Chinese Institute of Materia Medica
Mini reviews in medicinal chemistry | Year: 2016

BRD4, an epigenetic regulator that recognizes and binds the acetylated lysine residues in histone, has been reported as a potential therapeutic target for cancers. Since the first BRD4 inhibitor JQ1 developed in 2010, numerous BRD4 inhibitors have been discovered in past five years. In this review, we have systematically summarized a series of BRD4 binding compounds, which are divided into five categories based on the similarity of their chemical structures and respectively referred as JQ1 derivatives, tetrahydroquinoline derivatives, 3,5- dimethylisoxazole derivatives, 2-thiazolidinone derivatives and others. The binding affinities for each class of compounds are also discussed.


Zhou X.,Chinese Institute of Materia Medica | Tang L.,Chinese Institute of Materia Medica | Xu Y.,Chinese Institute of Materia Medica | Zhou G.,Chinese Institute of Materia Medica | Wang Z.,Chinese Institute of Materia Medica
Journal of Ethnopharmacology | Year: 2014

Ethnopharmacological relevance Carthamus tinctorius L. (Compositae), a widely used traditional Chinese medicine, was known as Hong hua (Chinese:), safflower. Safflower with a wide spectrum of pharmacological effects has been used to treat dysmenorrhea, amenorrhea, postpartum abdominal pain and mass, trauma and pain of joints, etc. The present paper reviews the advancements in investigation of botany and ethnopharmacology, phytochemistry, pharmacology and toxicology of safflower. Finally, the possible tendency and perspective for future investigation of this plant are discussed, too. Materials and methods The information on safflower was collected via piles of resources including classic books about Chinese herbal medicine, and scientific databases including Pubmed, Google Scholar, ACS, Web of science, CNKI and others. Results Over 104 compounds from this plant have been isolated and identified, and quinochalcones and flavonoids are considered as the characteristic and active constituents of safflower. Safflower with its active compounds possesses wide-reaching biological activities, including dilating coronary artery, improving myocardial ischemia, modulating immune system, anticoagulation and antithrombosis, antioxidation, antiaging, antihypoxia, antifatigue, antiinflammation, anti-hepatic fibrosis, antitumor, analgesia, etc. Conclusions As an important traditional Chinese medicine, it is important to investigate the pharmacological effects and molecular mechanisms of this plant based on modern realization of diseases' pathophysiology. More bioactive components should be identified using bioactivity-guided isolation strategies, and the possible mechanism of action as well as potential synergistic or antagonistic effects of multi-component mixtures derived from safflower need to be evaluated integrating pharmacological, pharmacokinetic, bioavailability-centered and physiological approaches. Further studies on safflower can lead to the development of new drugs and therapeutics for various diseases, and how to utilize it better should be paid more attention to. © 2013 Elsevier Ireland Ltd.


Shi J.,Beijing University of Chemical Technology | Lu C.,Beijing University of Chemical Technology | Yan D.,Chinese Institute of Materia Medica | Ma L.,Chinese Institute of Materia Medica
Biosensors and Bioelectronics | Year: 2013

In this work, based on electronic spinning resonance and chemiluminescence (CL) measurements, it is found that the reaction kinetics of Co(II)-triggered Fenton-like reaction is much faster than those of other transition metal ions, which facilitates the observation of the strong CL signals from Co(II). Utilizing the polymer-surfactant complexes (i.e., necklace model) to act as a novel CL microenvironment, a highly selective CL sensing system for the detection of Co(II) has been successfully fabricated based on the CL resonance energy transfer between the Fenton-like reaction and necklace model microenvironment-modulated carbon dots. Under optimized experimental conditions, this proposed CL system exhibits a stable response to Co(II) over a concentration range from 1.0 to 1000. nM with a detection limit as low as 0.67. nM. Finally, this system has been successfully used for the detection of Co(II) in HepG2 cells, and the results were agreed with those obtained by inductively coupled plasma mass spectrometry (ICP-MS) method. © 2013 Elsevier B.V.


Patent
Chinese Institute of Materia Medica | Date: 2011-03-16

The present invention relates to novel coumarin derivatives, their carboxamides, pharmaceutical compositions containing them, and their uses as drugs for kidney protection, treating drugs of hypertension, cardio-cerebrovascular diseases, non-insulin dependent diabetes, tumor, pre-cancerous lesion, and edemas.Claimed are compounds of general formula (I):^(3) is selected from the group consisting_(9)R_(4) is selected from the group consisting of hydrogen, CONHR_(10),R_(5) is selected from the group consisting of H, and C_(1)-C_(4) alkyl;R_(6) is selected from the group consisting of H, C_(1)-C_(12) alkyl, halogen, NO_(2), and CONHR_(13),R_(8) is selected from the group consisting of H, C_(1)-C_(4) alkyl or alkoxyl, NO_(2).The other variables are as defined in claims.


Patent
Chinese Institute of Materia Medica | Date: 2010-04-13

The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinsons disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.


Patent
Chinese Institute of Materia Medica | Date: 2010-05-19

The invention relates to a compound of the following general formula (I):


Patent
Shijiazhuang Pharma. Group Zhongqi Pharmaceutical Technology Shijiazhuang Co. and Chinese Institute of Materia Medica | Date: 2014-01-29

The present invention discloses the use of L-butylphthalide of formula (I) in the manufacture of medicaments for the prevention and treatment of cerebral infarct, especially induced by focal cerebral ischemia.


Patent
Chinese Institute of Materia Medica | Date: 2010-04-13

The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinsons disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.


Patent
Shijiazhuang Pharma. Group Zhongqi Pharmaceutical Technology Shijiazhuang Co. and Chinese Institute of Materia Medica | Date: 2016-01-20

The present invention discloses the use of L-butylphthalide of formula (I) in the manufacture of medicaments for the prevention and treatment of cerebral infarct, especially induced by focal cerebral ischemia.

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