Study on extraction process and antioxidant activity of iridoid glycosides in Damnacanthus officinarum Huang / 药学实践杂志

Objective To optimize the extraction process of main iridoid glycosides in Damnacanthus officinarum Huang and evaluate the antioxidant activity of Damnacanthus officinarum Huang in vitro. Methods The classical heating-reflux extraction method was selected. The volume fraction of ethanol, the volume of solvent and extraction time were taken as the evaluation factors. The comprehensive score of extraction yield and the monotropein content were used as the evaluation indexes. An orthogonal test was designed to select the best extraction conditions. The total reducing capacity, DPPH clearance rate and hydroxyl radical scavenging rate were measured to determine its antioxidant activity in vitro. Results The optimal extraction process was the reflux with 6 times volume of 60% ethanol for 2 hours. Damnacanthus officinarum Huang has certain antioxidant capacity, and the activity of ethyl acetate part had the best effect. Conclusion The optimized extraction process is stable and feasible, which can be used for extraction of the iridoid glycosides from Damnacanthus officinarum Huang. This study has proved that Damnacanthus officinarum Huang has certain antioxidant activity.

Screening for the Bioactive Fraction of Smilax china L. on Inhibition of Experimentally Induced Benign Prostatic Hyperplasia / 医药导报

Objective To study the effect of extracts of Smilax china L. on inhibition the experimentally induced benign prostatic hyperplasia ( BPH) , and screen the effective fraction. Methods The BPH model was built on the castrated rats by subcutaneous injection of testosterone propionate. Male rats were randomly divided into eight groups ( n=6 ):sham operation, model control, petroleum ether fraction, acetic ether fraction, n-butyl alcohol fraction, water fraction, macroporous resin fraction ( FMR) , and total extracts group. The rats were treated with testosterone propionate by subcutaneous injection for consecutive 3 weeks. Meanwhile, rats were orally administrated with the six extract fractions of S. china L. After the last administration, serum was separated for the determination of prostatic acid phosphatase ( PACP ) , prostate was weighed and histopathological examination was carried out to evaluate the inhibitory effect of S. china L. against BPH. Results All of the six fractions from S. china L. could inhibit BPH, and the n-butanol fraction, water fraction and FMR showed better inhibitory effect, which significantly decreased the prostatic index by 52. 80%, 50. 93% and 67. 70%, respectively, remarkably reduced serum PACP, and notably improved the prostate gland morphology compared with the model group. Among the three fractions, FMR showed the strongest effect against BPH. Conclusion S. china L. ameliorates the experimentally prostatic hyperplasia, and FMR showes the best effect, which might be the bioactive components against BPH.

Study on Active Fractions of Macrothelypteris Oligophlebia for Chronic Non-bacterial Prostatitis in Rats / 中国药师

Objective:To explore the effect of the methanol extract of Macrothelypteris oligophlebia on chronic non-bacterial prosta-titis ( CNP) in rats to confirm the active fractions. Methods:The powdered rhizomes of M. oligophlebia were soaked in methanol. The methanol extract was suspended in water and then extracted successively with chloroform and ethyl acetate to obtain chloroform fraction, ethyl acetate fraction and water fraction. Carrageenan-induced CNP in rats was established. The rats were randomly divided into the sham-operated control group, model group, positive control group, methanol extract group, ethyl acetate fraction group, chloroform fraction group and water fraction group. The anti-prostatitis effect was evaluated by the prostate index, and the pathological examination of prostate was performed using HE staining. The levels of interleukin-10 (IL-10), tumor necrosis factor alpha (TNF-α), cyclooxyge-nase-2 (COX-2) and prostaglandin E2(PGE2) were analyzed using ELISA kits. Results:The ethyl acetate fraction group and metha-nol extract group with high flavonoid content could significantly decrease prostate index (P<0. 01) and the levels of IL-10, TNF-α, COX-2 and PGE2(P<0. 05 or P<0. 01), and improve the prostate morphology when compared with the model group, especially with the ethyl acetate fraction group. Conclusion:The rhizomes of M. oligophlebia show promising therapeutic effect on CNP, and the ethyl acetate fraction is the active fraction.

Flavonoids with special B-ring from Macrothelypteris viridifrons and their anti-proliferative effects on tumor cell / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Macrothelypteris viridifrons and their anti-proliferative effects on tumor cell.</p><p><b>METHOD</b>The compounds were isolated by column chromatography with silica gel, C18 reverse-phase silica gel, sephadex LH-20, and their structures were elucidated on the basis of physiochemical propertities and spectral analysis. The antitumor activities of all compounds were tested with MOLT4, Hep G2, A-549, MCF-7, HT-29, PC-3 tumor cell lines.</p><p><b>RESULT</b>Five compounds were isolated and identified as protoapigenone (1), protoapigenin (2), protoapigenin-4'-O-beta-D-glucopyanoside (3), 5,7-dihydroxy-2-(1,2-isopropyldioxy-4-oxo-cyclohex-5-enyl) -chromen-4-one (4), 5,7-dihydroxy-2-(1-hydroxy-2,6-dimethoxy-cyclohex-4-oxo) -chromen-4-one (5), respectively.</p><p><b>CONCLUSION</b>All compounds were obtained from this plant for the first time. Compounds 1, 4 and 5 showed strong anti-proliferative effects on six tumor cells, which were in concentration-dependent manner.</p>

Dispersive liquid-liquid microextraction combined with high-performance liquid chromatography for the determination of clozapine and chlorpromazine in urine / 华中科技大学学报（医学）（英德文版）

A simple method has been proposed for the determination of clozapine (CLZ) and chlorpromazine (CPZ) in human urine by dispersive liquid-liquid microextraction (DLLME) in combination with high-performance liquid chromatography-ultraviolet detector (HPLC-UV). All important variables influencing the extraction efficiency, such as pH, types of the extraction solvent and the disperser solvent and their volume, ionic strength and centrifugation time were investigated and optimized. Under the optimal conditions, the limit of detection (LODs) and quantification (LOQs) of the method were 13 and 39 ng/mL for CLZ, and 2 and 6 ng/mL for CPZ, respectively. The relative standard deviations (RSDs) of the targets were less than 5.1% (C=0.100 μg/mL, n=9). Good linear behaviors over the tested concentration ranges were obtained with the values of R (2)>0.999 for the targets. The absolute extraction efficiencies of CLZ and CPZ from the spiked blank urine samples were 98.3% and 97.8%, respectively. The applicability of the technique was validated by analyzing urine samples and the mean recoveries for spiked urine samples ranged from 93.3% to 105.0%. The method was successfully applied for the determination of CLZ and CPZ in real human urine.

A New Phenolic Acid from Rhizomes of Abacopteris penangiana / 中草药·英文版

Objective To study the chemical constituents of Abacopteris penangiana.Methods The compounds were separated and purified by various chromatographic techniques and their structures were elucidated on the basis of physiochemical properties and spectroscopic methods.Results Seven compounds were purified and their structures were identified as:(7'Z)-3-O-(3,4-dihydroxy phenylethenyl)-caffeic acid(1),caffeiein B(2),matteucinol(3),protocatechuic acid(4),p-methoxybenzoic acid(5),β-sitosterol(6),and daucosterol(7).Conclusion Compound 1 is a new phenolic acid compound named abacopteric acid,and the other compounds are isolated from the plant for the first time.

Anti-inflammatory and analgesic activity of topical administration of siegesbeckia pubescens

Several topical formulations containing methanolic extract of Siegesbeckia pubescens was investigated for antiinflammatory and analgesic activities in rat. The effects were studied using carrageenan-induced edema and formalin testing. Piroxicam gel and methyl salicylate ointment were studied as positive control for antiinflammatory and analgesic activity, respectively. The edema inhibition of the preparations containing extract at the doses of 1-5% w/w were significantly different from the control group. The antiinflammatory effect of Siegesbeckia pubescens 4-5% w/w was similar to the effect of piroxicam gel 3 h after carrageenan injection. The analgesic activity of topical preparation with more than 4% w/w was observed in the late phase. The topical analgesic activity of the extract was less than the analgesic activity of methyl salicylate ointment. The results of the present study further confirm the use of Siegesbeckia pubescens traditionally for the treatment of painful inflammatory conditions and can be useful for the treatment of local inflammation

Development and evaluation of the sinomenine transdermal patch

Sinomenine transdermal patch was prepared and its properties were studied. The patches were produced by salivation method. The releasing rate in vitro of the patch was determined by HPLC. Peel test was used to evaluate the adhesion. Acute skin irritation test was performed in comparison with formalin [0.8%] by using mouse model. The Sinomenine TDDS Patch was prepared. The releasing rate in vitro followed the Higuchi equation [r>0.99], the releasing amount was beyond 90% in 24h. The peel adhesion to steel [N/25 mm] is 10 or above. The skin irritation tests showed negligible erythema and edema. The Sinomenine transdermal patch was prepared successfully and it may be beneficial for topical use

Studies on Iridoid Glucosides from Verbena officinalis / 中草药

For the purpose to seek the active components in the aerial parts of Verbena officinalis L.with anti-early pregnancy activity, the methanolic extract of this drug was repeatedly chromatographed onsilica gel column. Three iridoid glucosides were isolated and identified on the basis of physical, chemicalevidences and spectroscopic analysis (UV, IR, 1HNMR, 13CNMR, 1H-1HCOSY, 1H-13CCOSY and DEPT)as verbenalin (Ⅰ), 3, 4-dihydroverbenalin (Ⅲ) and hastatoside (Ⅲ).Ⅱ is a new natural compound.

Study on Antioxidant Stilbenes from the Rhizomes of Smilax china / 中药新药与临床药理

Objective To study the stilbene constituents from the traditional Chinese medicine Smilax china and to determine their antioxidant activity. Methods The compounds were separated and purified by column chromatography with silica gel, RP C18, and Sephadex LH- 20, and were identified by IR, MS, NMR. DPPH method was used to evaluate the free radical scavenging activity of the isolated compounds. Results Three compounds were isolated from the EtOAc fraction of the rhizomes of S. china and were identified as: resveratrol (1), oxyresveratrol (2) and 3, 5, 3′ , 4′ - tetrahydroxylstilbene (3). Compounds 1～ 3 showed strong antioxidant activity, and could scavenge DPPH free radicals, effectively. At the concentration of 50 ? mol/L, their DPPH free radical scavenging rates were 79.47 % , 89.89 % and 93.86 % , respectively. Conclusion Stilbenes might be the material foundation of antioxidant activities of rhizomes of S. china.