Monoterpenoid Indole Alkaloids from Kopsia officinalis and the Immunosuppressive Activity of Rhazinilam.

Six new monoterpenoid indole alkaloids, kopsinidines C-E (1-3), 11,12-methylenedioxychanofruticosinic acid (4), 12-methoxychanofruticosinic acid (5), and N(4)-methylkopsininate (7), as well as chanofruticosinic acid (6, as a natural product) and 23 known alkaloids, were obtained from the twigs and leaves of Kopsia officinalis. Their structures were characterized by physical data analysis. All isolated compounds were evaluated for their immunosuppressive activity on human T cell proliferation. Rhazinilam (29) significantly inhibited human T cell proliferation activated by anti-CD3/anti-CD28 antibodies (IC50 = 1.0 µM) and alloantigen stimulation (IC50 = 1.1 µM) without obvious cytotoxicity for naïve human T cells and peripheral blood mononuclear cells (0-320 µM). Although it did not affect T cell activation, it induced T cell cycle arrest in the G2/M phase and inhibited proinflammatory cytokine production in activated T cells.

[Effects of electroacupuncture at different acupoints on apoptosis and the expression of miRNAs in myocardial cells in rats model of myocardial ischemia].

OBJECTIVE: To observe the effects of electroacupuncture (EA) at different acupoints on apoptosis-related serum and expression of microRNA (miRNA) in rats with myocardial ischemia, so as to explore its mechanism of action. METHODS: A total of 48 male Wistar rats were randomly divided into a normal group, a model group, a Neiguan group and a acupoint compatibility group, 12 rats in each group. Isoprenaline hydrochloride (ISO) with a daily dose of 2 mg/kg was subcutaneously injected for 14 days to establish the myocardial ischemia model in the model group, Neiguan group and acupoint compatibility group. Rats in the normal group were subcutaneously injected with an equal volume of normal saline. After modeling, rats in the Neiguan group were treated with EA at "Neiguan" (PC 6), while rats in the acupoint compatibility group were treated with EA at "Guanyuan" (CV 4), "Zusanli" (ST 36) and "Neiguan" (PC 6). Rats in the normal group and model group were treated with immobilization, once day for 21 days. The contents of creatine kinase-MB (CK-MB), vascular cell adhesion molecule-1 (VCAM-1) and endothelin-1 (ET-1) in serum were detected by enzyme-linked immunosorbent assay (ELISA); apoptosis index (AI) of myocardial cells was detected by TUNEL method; the expressions of miRNA-1, miRNA-133, miRNA-208 and miRNA-499 were detected by real-time PCR method. RESULTS: Compared with the normal group, the serum CK-MB, VCAM-1 and ET-1 were significantly increased in the model group, Neiguan group and acupoint compatibility group (all P < 0.01), and the apoptosis index was significantly increased (all P < 0.01). The CK-MB, VCAM-1 and ET-1 in the Neiguan group and acupoint compatibility group were significantly lower than those in the model group (all P < 0.01); the AI was reduced, which was more significant in the acupoint compatibility group (P < 0.05). Compared with the normal group, the expression of miRNA-133 was reduced (P < 0.01) and those of miRNA-208, miRNA-1 and miRNA-499 were significantly increased in the model group (all P < 0.01). Compared with the model group, the expression of miRNA-133 was increased (both P < 0.01) and that of miRNA-208, miRNA-1 and miRNA-499 were significantly reduced (all P < 0.01) in the Neiguan group and acupoint compatibility group. Compared with the Neiguan group, the expression of miRNA-133 was increased (P < 0.01) and those of miRNA-208, miRNA-1 and miRNA-499 were significantly reduced in the acupoint compatibility group (P < 0.01, P < 0.05). CONCLUSION: EA at acupoints, especially acupoint compatibility group, could effectively prevent and treat myocardial ischemia, and the protective effect is possibly correlated to the double regulation on increasing the expression of miRNA-133 and inhibiting the expression of miRNA-1, miRNA-208, miRNA-499.

[Ginger-partition moxibustion combined with glucocorticoid for thyreoitis at subacute stage: a randomizd controlled trial].

OBJECTIVE: To compare the clinical effects between ginger-partition moxibustion combined with glucocorticoid and simple oral glucocorticoid for thyreoitis at subacute stage. METHODS: Eighty-one patients were randomly divided into an observation group (41 cases) and a control group (40 cases). In the observation group, ginger-partition moxibustion and hormone were applied. Moxa cones were used at local ashi points, Zusanli (ST 36), Guanyuan (CV 4) and Qihai (CV 6), six cones every point, once every other day and three times a week. Besides, 24 mg methylprednisolone tablets were adopted orally every day, and in two weeks the dose was 16 mg/d, in four weeks 8 mg/d, in six weeks 4 mg/d; all the patients were observed for 8 week. In the control group, simple methylprednisolone was prescribed orally, and the dose, the usage and treatment time were the same as those in the observation group. Erythrocyte sedimentation rate (ESR), triiodothyronine (T3), thyroxin (T4) and ultra-sensitive thyroid stimulating hormone (TSH) before and after treatment were observed in the two groups, as well as fever, the pain of thyroid gland, the regression time of swelling and adverse reaction. RESULTS: The time of thyroid gland pain relieved of the observation group was earlier than that of the control group [(3.07 ± 0.78) days vs (3.62 ± 0.92) days, P < 0.05]. After treatment, T3, T4 and ESR were declined apparently (all P < 0.01), and TSH was obviously increased in the two groups (both P < 0.01). After 2-week treatment, ESR in the observation group was lower than that in the control group (P < 0.05). After 4-week treatment, T3, T4, TSH and ESR in the observation group were better than those in the control group (all P < 0.05). After 8 weeks, all indices in the observation group were superior to those in the control group, without statistical significance between the two groups (all P > 0.05). The effects of the observation group in 2 weeks, 4 weeks and 8 weeks were better than those in the control group (all P < 0.05). The cured course was shorter in the observation group than that in the control group (P < 0.05). The adverse reaction rate in the observation group was lower than that in the control group [4.9% (2/41) vs 22.5% (9/40), P < 0.05]. Three months later after treatment, the cured patients were followed. There was no recrudescence in the observation group and three patients caught the disease again in the control group, but there was no statistical significance between the two groups (P > 0.05). CONCLUSION: Ginger-partition moxibustion combined with glucocorticoid achieves better effect than simple oral glucocorticoid for thyreoitis at subacute stage, and the adverse reaction is less, which presents the clinical advantages of the integration of Chinese and western medicine.

Calophyline A, a new rearranged monoterpenoid indole alkaloid from Winchia calophylla.

Calophyline A (1), a novel unprecedented rearranged monoterpenoid indole alkaloid, along with a new natural product N-methyl aspidodasycarpine (2) and six known analogues, was isolated from the trunk barks of Winchia calophylla. The structure of compound 1 was elucidated on the basis of spectroscopic data and then confirmed by a single-crystal X-ray crystallographic analysis. A hypothetical biogenetic pathway for compound 1 was proposed. All isolated compounds were evaluated for their in vitro cytotoxicity against a small panel of human cancer cell lines.

A refined surgical treatment modality for bromhidrosis: double w incision approach with tumescent technique.

BACKGROUND: Axillary bromhidrosis has a strong negative effect on one's social life. A high success rate and few complications are criteria for an ideal treatment method. OBJECTIVE: To evaluate a new surgical treatment modality for bromhidrosis: Double W incision with full-exposure excision under tumescent anesthesia. MATERIALS & METHODS: Twenty patients with bromhidrosis were treated. Patients were placed in a supine position with their treated arms abducted to 110 degrees . After injection of 60 mL of tumescent solution into each axilla, two small W incisions were made at the superior and inferior axillary poles of the hair-bearing area. The whole hair-bearing skin was undermined at the level of the superficial fat to obtain adequate skin eversion. The flaps were everted to offer full exposure of the apocrine glands, and meticulous excision of each gland was performed. Finally, the incisions were re-approximated, and bulky compressive dressings were applied to the area for 72 hours. RESULTS: Of the 40 axillae (20 patients), 32 (80.0%) showed excellent results, and eight (20.0%) had good results. Malodor was significantly decreased. There were no serious complications. CONCLUSION: This technique can produce excellent results with a lower complication rate than most other surgical modalities and can be performed without costly equipment.

Depigmentation of melanocytes by the treatment of extracts from traditional Chinese herbs: a cell culture assay.

OBJECTIVE: To obtain potential skin whitening agents from traditional Chinese herbs, we tested changes of melanin content in melanocyte cell lines after treatment with extracts of 90 traditional Chinese herbs. METHODS: Mouse melanocyte cell lines were used. Depigmentation activity of the herb extracts were first screened in Mel-Ab cells, and then re-evaluated in melan-a cells and co-culture of melan-a and SP-1 cells. Melanin content and cell viability were the two indications for evaluation. Tyrosinase activity and the expression of melanin synthesis related enzymes in cells treated with the herb extracts were also tested. RESULTS: Nine herb extracts were proved to have depigmentation activity similar to or better than that of arbutin and low cytotoxicity to melanocytes. Two of them were more effective in co-cultured melan-a cells. Most of the effective herb extracts inhibited tyrosinase activity and the expression of tyrosinase. Some of them also inhibited tyrosinase related protein-1 and/or tyrosinase related protein-2 in cultured cells. CONCLUSIONS: We have found 9 herb extracts to be promising skin whitening agents. Among them, water extract of Galla Chinensis and ethanol extract of Radix Clematidis exhibited higher depigmentation activity and caused lower tyrosinase activity in cell culture assays and are worthy to be further studied.