Mechanism of Borneolum Syntheticum Effect on Central Nervous and Vascular System Diseases / 中国实验方剂学杂志

In traditional Chinese medicine, Borneolum Syntheticum, a representative drug of aromatic orifice, is often widely used in the clinical treatment of neurotic diseases.In recent years, many scholars at home and abroad have studied and analyzed the effective components and pharmacological effects of Borneolum Syntheticum,and it is considered that Borneolum Syntheticum alone has a significant effect on brain diseases.In this paper, the mechanism of Borneolum Syntheticum on cerebral circulatory system and central nervous system is discussed.In inhibiting brain injury, Borneolum Syntheticum can reduce neuronal vascular endothelial injury, reduce brain edema and decrease the content of Ca2+ in ischemic brain tissue.In the aspect of anti-inflammation, Borneolum Syntheticum can reduce the expression of induced nitric oxide synthase(iNOS) and tumor necrosis factor-α(TNF-α), the number of leukocyte infiltration, the number of intercellular adhesion molecule-1(ICAM-1) positive vessels and the number of TNF-α positive cells.In regulating the blood-brain barrier, Borneolum Syntheticum can increase the expression of zonula occluden-1(ZO-1) and claudin-5 protein in microvascular endothelial cells.The strength of the transdermal absorption of the Borneolum Syntheticum may be related to its configuration, the ability to extract the lipid, and the hydrophilicity.The effect of Borneolum Syntheticum on improving the bioavailability of other drugs is widely used in clinic.Nasal administration of Borneolum Syntheticum can bypass blood-brain barrier (BBB), and reach the central nervous system of the brain. It has a good prospect in the treatment of cerebrovascular disease.In the treatment of brain diseases such as seizures and Alzheimer' s disease, the mechanism of Borneolum Syntheticum is closely related to its effect on various brain neurotransmitters such as γ-aminobutyric acid(GABA),glycine acid(GLY), D-aspartic acid(ASP), glutamic acid(GLU),β-endorphin(β-EP), norepinephrine(NE),epinephrine(E),5-hydroxytryptamine(5-HT),dopamine(DA). However, the experimental results are not the same. It may be related to the different dosage and time of Borneolum Syntheticum administration, which needs to be studied.

Functional Expression of TRPV4 Cation Channels in Human Mast Cell Line (HMC-1)

Mast cells are activated by specific allergens and also by various nonspecific stimuli, which might induce physical urticaria. This study investigated the functional expression of temperature sensitive transient receptor potential vanilloid (TRPV) subfamily in the human mast cell line (HMC-1) using whole-cell patch clamp techniques. The temperature of perfusate was raised from room temperature (RT, 23~25degrees C to a moderately high temperature (MHT, 37~39degrees C to activate TRPV3/4, a high temperature (HT, 44~46degrees C to activate TRPV1, or a very high temperature (VHT, 53~55degrees C to activate TRPV2. The membrane conductance of HMC-1 was increased by MHT and HT in about 50% (21 of 40) of the tested cells, and the I/V curves showed weak outward rectification. VHT-induced current was 10-fold larger than those induced by MHT and HT. The application of the TRPV4 activator 4alpha-phorbol 12,13-didecanoate (4alphaPDD, 1microM) induced weakly outward rectifying currents similar to those induced by MHT. However, the TRPV3 agonist camphor or TRPV1 agonist capsaicin had no effect. RT-PCR analysis of HMC-1 demonstrated the expression of TRPV4 as well as potent expression of TRPV2. The [Ca2+]c of HMC-1 cells was also increased by MHT or by 4alphaPDD. In summary, our present study indicates that HMC-1 cells express Ca2+-permeable TRPV4 channels in addition to the previously reported expression of TRPV2 with a higher threshold of activating temperature.

Entery of calcium into ECV304 endothelial cell via CaCa~(2+) activated non-selective cation channel / 中国药理学通报

AIM To investigate the pathways of Ca 2+ entry into ECV304 endothelial cell and the effect of angiotensin Ⅱ(AⅡ) on calcium activated non setective cation channel(CAN). METHODS The cell attachment and whole cell configurations of patch clamp technique were used to record channel activity. RESULTS (1) The single channel conductance is ? o=(12 90?2 11) pS( n =4) for Ca 2+ passing through CAN of ECV304 cell in condition of pipette solution without K + and Na + but composed 120 mmol?L -1 CaCl 2. The channel current amplitude and open time can be enhanced by 1?10 -7 mol?L -1 AⅡ. The enhanced conductance in CAN is ? 1=(22 18?2 29) pS( n =4). The results of whole cell recording are identified with single channel recording. (2) The whole cell configuration was carried out for recording voltage dependent Ca 2+ channel in ECV304 cell. The peak current amplitude was (29 32?3 56) pA( n =4). This current was inhibited to (6 00?3 94) pA( n =4) by nifedipine and activated by BayK8644. CONCLUSIONS (1)Ca 2+ enters ECV304 cell via Ca 2+ activated non selective cation channel and voltage dependent L type calcium channel. (2) AⅡ can significantly enhance the calcium entry via CAN in ECV304 cell.