New anti-HBV norbisabolane sesquiterpenes from Phyllantus acidus.

The norbisabolane-type sesquiterpenoids bearing a spiroketal functionality have been found in Phyllanthus spp. and showed anti-HBV activities. As part of an ongoing effort to search for promising anti-HBV sesquiterpenes from Phyllanthus plants, we report four new norbisabolane-type sesquiterpenoids, phyacidusin A (1), phyacidusin B (2), phllanthacidoid A1 (3) and phllanthacidoid N1 (4), from stem of P. acidus collected in Xishuangbanna, Yunnan province, China. The absolute configuration of new compounds was established by coupling constants and ROESY correlations, as well as comparation of NMR data with those of known compounds. The absolute configuration of new compounds 1 and 2 was further confirmed by X-ray diffraction. Compound 2 showed effect to HBsAg with an IC50 value of 11.2 ±â€¯0.01 µM, while compound 3 inhibited HBeAg secretion with an IC50 value of 57.1 ±â€¯0.02 µM. The results enriched the diversity of anti-HBV norbisabolane sesquiterpenes.

Clinical Observation of Chronic Pharyngitis Treated with Acupuncture / 广州中医药大学学报

Objective To compare the clinical efficacy of acupuncture and medicine for the treatment of chronic pharyngitis. Methods Sixty chronic pharyngitis patients were randomized into treatment group and control group, 30 cases in each group. The treatment group was treated with acupuncture mainly on acupoints of Zhaohai(KI6), Lieque(L7), Tiantu(CV22) , Lianquan(CV23), Tianrong(SI17) , Hegu(LI), Yuji (LU10) for nourishing yin to reduce fire and clearing throat. The supplementary acupoints were selected according to the symptoms and physical signs. Acupuncture was performed once a day and 6 times a week. The control group received western medical therapy including pharyngeal application with 1% iodine glycerin preparation and oral use of Cydiodine tablets, 3 times per day. Four weeks constituted one treatment course and the treatment for the two groups covered 2 courses. After treatment, the therapeutic effect was evaluated. The scores of the signs and s ymptoms as well as scores of chronic pharyngitis syndrome discomfort rating questionnaire(CPSDQ) evaluated by visual anal og scale(VAS) were observed. Results (1) The overall effective rate of the treatment group was 93.3%, higher than that of the control group(73.3%), and the inter-group difference was statistically significant (P<0.05). (2) After treatment, scores of the signs and symptoms and VAS for CPSDQ scores in the two groups were reduced as compared with those before treatment(all P<0.05 or P<0.01 ) .The improvement of the scores in the treatment group was superior to that in the control group(all P<0.05 or P<0.01).(3) During the treatment , needling-induced mild pain and bleeding occurred in the treatment group. No acupuncture syncope, stuck needles or allergic and toxic-side effect was shown in the two groups. Conclusion Acupuncture therapy can obviously relieve the symptoms, signs and discomfort in the patients with chronic pharyngitis, and the curative effect is superior to the drugs.

Hinokitiol reduces matrix metalloproteinase expression by inhibiting Wnt/ß-Catenin signaling in vitro and in vivo.

OBJECTIVE: In this study, we investigated the effects of hinokitiol on matrix metalloproteinase (MMP)-1, -3, -13, collagen type II (Col2a1) and ß-catenin expressions in rat chondrocytes induced by interleukin-1ß and in an experimental rat model induced by intra-articular injection of mono-iodoacetate (MIA) into the knee. METHODS: Chondrocytes were cultured from the articular cartilage of 2-week-old rats. Passaged chondrocytes were pretreated with hinokitiol for 2h followed by co-incubation with IL-1ß for 24h. Quantitative real-time polymerase chain reaction and Western blotting were used to assess the expression of MMP-1, -3, -13, Col2a1 and ß-catenin. Chondrocytes were also treated with Licl, Dickkopf-1, and/or hinokitiol for 24h, the MMP-1, -3, -13 and ß-catenin protein levels determined by Western blotting. The in vivo effects of hinokitiol were assessed by morphological and histological analyses following MIA injection. RESULTS: Hinokitiol inhibited IL-1ß-stimulated MMP-1,-3 and -13 expressions and IL-1ß-induced activation of intracellular ß-catenin proteins in cultured chondrocytes. In vivo, morphological and histological examinations demonstrated that hinokitiol significantly ameliorated cartilage degeneration. CONCLUSIONS: Hinokitiol is an effective anti-inflammatory reagent that acts by inhibiting the Wnt/ß-catenin signaling pathway and could be a promising therapeutic agent for the prevention and treatment of osteoarthritis.

Clinical observation of Alzheimer's disease treated with acupuncture / 中国针灸

<p><b>OBJECTIVE</b>To compare the differences in the clinical efficacy on Alzheimer's disease between acupuncture and medicine.</p><p><b>METHODS</b>One hundred and forty-one patients were randomized into an acupuncture group (72 cases) and a medicine group (69 cases). In the acupuncture group, the needling technique for benefiting qi, promoting blood circulation, regulating mind and improving intelligence was used at Shenting (GV 24), Baihui (GV 20), Fengchi (GB 20), Wangu (GB 12), Danzhong (CV 17), Zhangwan (CV 12), Qihai (CV 6), Xuehai (SP 10) and Zusanli (ST 36). The supplementary acupoints were selected according to the symptoms and physical signs. Acupuncture was given once a day and 6 treatments were required for a week. In the medicine group, the choline sterase inhibitor, donepezil (aricept) was prescribed for oral administration, 1 tablet (5 mg) each time, once every night. Four weeks later, the dose was increased to 2 tablets (10 mg) each time. In the two groups, the treatment of 4 weeks made one session and 4 sessions were required. The changes of scores before and after treatment in the minimum mental state examination (MMSE), the activity of daily living scale (ADL), Alzheimer's disease assessment scale-cognition (ADAS-cog) and the digit span (DS) were observed.</p><p><b>RESULTS</b>After treatment, scores of MMSE and DS were increased as compared with those before treatment (both P < 0.05) and scores of ADL and ADAS-cog were reduced as compared with those before treatment. The score differences in MMSE, ADL, ADAS-cog and DS before and after treatment were significant in the two groups (all P < 0.01).</p><p><b>CONCLUSION</b>The needling technique for benefiting qi, promoting blood circulation, regulating mind and improving intelligence significantly improves the overall function, cognition and activity of daily life in the patients of Alzheimer's disease and the efficacy is better than donepezil.</p>

[Electrochemotherapy and its mechanism for sarcoma of KM mice].

In this paper are analyzed the effect of electrochemotherapy and its mechanism. The favorable parameter of electric pulses (EP) was studied in vitro using the S-180 cells exposed to various EP. After the tumor model was copied, the tumor-bearing mice were randomly divided into four groups: control, chemotherapy, electrotherapy, and electrochemotherapy. The tumor inhibitory ratio, the cure ratio and the level of oxygen free radicals (OFR) were determined. The inhibitory ratio and cure ratio of electrochemotherapy group were significantly higher than those in the chemotherapy, electrotherapy and control groups (P < 0.05). The injury of OFR was decreased while the immunological competence was increased. The mechanism of electrochemotherapy may be related with the enhancement of cell membranepermeability, the depression of drug resistance, the improvement of immunological competence, and so on.

[Progress in electrochemotherapy].

Electrochemotherapy (ECT) is a novel cancer treatment in which electric pulses (EPs) inducing cell membrane pored (electroporation) are used as a means of delivering antitumor drugs to the cytoplasm of cancer cells. The minimal thresholds of electric field strength of in vitro tumor cell line and tumor tissue are 450-650 V/cm and 400-600 V/cm, respectively. The typical electrical requirement is 600-1300 V/cm, pulse width of 100 micros, 8 pulses, 1 Hz. More than 10 kinds of antitumor drugs have been applied to ECT, in which the most efficacious drug is Bleomycin, and then Cisplatin. Some exciting inhibitory effects on cells in vitro and on solid tumors in clinical trials have been noticed. The factors influencing ECT effects include the electric parameters, diameter of electrode, distribution of electric field lines, size of tumor, model of drugs injection and kinds of drugs. Some questions of ECT are still open, such as the dosages and kinds of drugs for clinical trials, model of drug injection, influence on normal tissues, therapeutic mechanism.

[Study of high-intensity electric pulse inhibited sarcoma for improving antitumor drug effect].

This article reports the experiment studies on treating the S-180 sarcomas of KM mice with high-intensity electric pulse and antitumor drug (cyclophosphamide). The results showed that the experimental group of electric field combined with drug has the best effect on tumor, compared with the control group. In addition, electric field can inhibit the formation of vas Capillaries and decrease the supply of nutrition for tumor cell. In conclusion, electric field has inhibited the growth of tumor.