OBJECTIVETo study active constituents of Macropanax rosthornii in treating rheumatoid arthritis.

METHODSilica gel column chromatography, preparative HPLC and modern spectrum techniques were applied for a systematic study on chemical constituents contained in M. rosthornii.

RESULTTwelve compounds were separated from M. rosthornii and identified as serratagenic acid (1), serjanic acid (2), betulinic acid (3), 6beta-hydroxy-3-oxo-olean-12-en-28-oic acid (4), 3-O-alpha-L-arabinopyranosyl serratagenic acid (5), 3-O-alpha-L-arabinopyranosyl serratagenic acid-29-methyl ester (6) , 3-O-alpha-L-arabinopyranosyl serratagenic acid-28-O-beta-D-glucopyranosyl ester (7), scopoletin (8), beta-sitosterol (9), daucosterol (10), 3,4-dihydroxybenzoic acid (11), and stearic acid (12).

CONCLUSIONAbove compounds are separated from M. rosthornii for the first time.

Araliaceae ; chemistry ; Chromatography ; methods ; Drugs, Chinese Herbal ; chemistry ; Medicine, Chinese Traditional

OBJECTIVE To optimize the processing technology of honey bran-fried Atractylodis Rhizoma， and to compare the anti-gastric ulcer effect before and after processing. METHODS Combing with entropy-weight and technique for order preference by similarity to ideal solution model， L（9 34） orthogonal experiment design was adopted to optimize the processing technology of honey bran-fried Atractylodis Rhizoma using the comprehensive score of the contents of atractylone， β-cineole， atractylenolide Ⅲ and atractylodine as evaluation index， using the ratio of excipients to medicine， frying temperature and frying time as factors. The validation tests were conducted. The gastric ulcer model of mice was induced by intragastrical administration of anhydrous ethanol； using Compound aluminum hydroxide tablet as positive control， anti-gastric ulcer effect of Atractylodis Rhizoma was compared with that of honey bran-fried Atractylodis Rhizoma using the contents of serum inflammatory factors [interleukin-2 （IL-2）， IL-6， tumor necrosis factor-α （TNF-α）]， ulcer index and inhibitory rate of gastric ulcer as evaluation indexes. RESULTS The optimal processing technology of honey bran-fried Atractylodis Rhizoma was as follows：ratio of adjuvant and medicinal materials of 3∶10 （g/g）， frying temperature at 140 ℃ and frying time of 4 min. Results of 3 validation tests showed that the contents of 4 components （including atractylone）， in honey bran-fried Atractylodis Rhizoma processed by the optimal technology kept stable （RSDs were 3.47%-5.80%， n＝3）； the comprehensive scores were 95.53%-95.89% （RSD＝0.21%， n＝3）. Atractylodis Rhizoma and honey bran-fried Atractylodis Rhizoma could increase the serum content of IL-2 in mice， but reduce serum contents of IL-6 and TNF-α to varying degrees； honey bran-fried Atractylodis Rhizoma could significantly decrease its ulcer indexes （P＜0.05 or P＜ 0.01）； the improvement effect of honey bran-fried Atractylodis Rhizoma on the above indicators was generally better than that of the same dosage of Atractylodis Rhizoma （P＜0.05 or P＜ 0.01）. The inhibitory rates of low-dose， medium-dose and high-dose Atractylodis Rhizoma and honey bran-fried Atractylodis Rhizoma to gastric ulcer in mice were 9.18%， 19.30%， 30.70%， and 50.32%， 61.39%， 53.16%， respectively. CONCLUSIONS The optimal processing technology of honey bran-fried Atractylodis Rhizoma is stable and feasible， and the anti-gastric ulcer effect of Atractylodis Rhizoma has been enhanced after being fried with honey bran.

ObjectiveTo optimize the processing technology of honey bran-fried Rosae Laevigatae Fructus（h-RLF）， formulate relevant quality standards， and explore its improving effect and mechanism on mice with ulcerative colitis（UC） induced by dextran sodium sulfate（DSS）. MethodsTaking the content of polysaccharides and water-soluble extract as the indexes， L₉（3⁴） orthogonal test was used to optimize parameters of the amount of honey bran， frying time and frying temperature. The quality of 15 batches of h-RLF decoction pieces was evaluated according to the optimized process， and the inspection limit standard was preliminarily drawn up. Eighty SPF male Kunming mice were randomly divided into 8 groups， including the blank group， model group， mesalazine group（0.13 g·kg^-1）， RLF group（3.77 g·kg^-1）， bran-fried RLF group（3.77 g·kg^-1）， h-RLF low， medium and high dose groups（1.89， 3.77， 7.54 g·kg^-1）， with 10 mice in each group. The mice in the blank group were free to drink pure water， and the other groups were free to drink 3% DSS solution for 7 days to prepare UC mouse model. Each treatment group was given corresponding drugs by intragastric administration， and the blank and model groups were given equal volume of normal saline. The body weight of mice was recorded daily and the disease activity index（DAI） was calculated. After the administration， the colon tissues of mice were collected to observe the pathological changes by hematoxylin-eosin（HE） staining. The levels of tumor necrosis factor（TNF）-α， interleukin（IL）-1β， IL-6 and IL-10 in the colon of mice were detected by enzyme-linked immunosorbent assay（ELISA）. Western blot was used to detect the expression levels of phosphorylation nuclear transcription factor-κB p65（p-NF-κB p65）， Toll-like receptor 4（TLR4）， p-p38 mitogen-activated protein kinase（p-p38 MAPK）， p-extracellular signal-regulated kinase（p-ERK） and p-c-Jun N-terminal kinase（p-JNK） proteins in colon tissues. ResultsThe optimum processing technology of h-RLF was 20 g honey bran per 100 g RLF， and stir-frying at 200 ℃ for 8 min. The limit standard under the examination of h-RLF was preliminarily formulated as follows：the polysaccharide content should not be less than 25% based on anhydrous glucose（C₆H₁₂O₆）， the content of water-soluble extract should not be less than 38%， the moisture content should not be more than 12.0%， the total ash content should not be more than 5.0%， and the acid-insoluble ash content should not be more than 1.0%. The cluster heat map analysis showed that the quality of RLF from Huanggang， Hubei province was better. Animal experiments showed that compared with the blank group， the DAI score of the model group was significantly increased， the levels of TNF-α， IL-1β and IL-6 in the colon tissue were significantly increased， the IL-10 level was significantly decreased， the colonic mucosa was seriously damaged， accompanied by a large number of inflammatory cell infiltration， tissue congestion and a significant reduction in glands， and the expression levels of p-NF-κB p65， TLR4， p-p38 MAPK， p-ERK and p-JNK proteins were significantly increased（P<0.01）. Compared with the model group， each administration group could alleviate the symptoms of colonic ulcer， the structure of colonic crypt was basically intact， and the glands were arranged in an orderly manner. Among them， the high-dose group of h-RLF had a better effect， which could significantly reduce the DAI score and the levels of TNF-α， IL-1β and IL-6 in colon tissue（P<0.01）， and significantly increase the level of IL-10（P<0.01）， alleviate the colonic mucosal injury， and effectively inhibit the expression levels of p-NF-κB p65， TLR4， p-p38 MAPK， p-ERK and p-JNK proteins（P<0.01）. ConclusionThe key parameters of the processing technology of h-RLF are determined， and the optimized technology is stable and feasible. The established quality standard is simple and reliable， and can be used for the quality control. h-RLF can effectively alleviate DSS-induced UC， and its mechanism may be related to inhibiting the activation of NF-κB/TLR4/MAPK pathway.