Bioactivity-guided isolation of anti-inflammatory limonins from Chukrasia tabularis.

Chukrasia tabularis is an economically important tree and widely cultured in the southeast of China. Its barks, leaves, and fruits are consumed as a traditional medicine and perceived as a valuable source for bioactive limonin compounds. The extracts from root barks of C. tabularis showed significant anti-inflammatory effect. The aim of this research was to explore the material basis of C. tabularis anti-inflammatory activity, and to purify and identify anti-inflammatory active ingredients. By a bioassay-guided isolation of dichloromethane fraction obtained two novel phragmalin limonins, Chukrasitin D and E (1 and 2), together with 12 known limonins (3-14). The chemical structure of these compounds is determined on the basis of extensive spectral analysis and chemical reactivity. In addition, the activities of these isolated limonins on the production of nitric oxide (NO), tumor necrosis factor alpha (TNF-α), and nuclear factor kappa B (NF-κB) in RAW264.7 cells induced by lipopolysaccharide (LPS) were evaluated. Limonins 1 and 2 indicated significant anti-inflammatory activity with IC50 values of 6.24 and 6.13 µM. Compound 1 notably inhibited the production of NF-κB, TNF-α and interleukin 6 (IL-6) in macrophages. The present results suggest that the root barks of C. tabularis exhibited anti-inflammatory effect and the limonins may be responsible for this activity.

The in vitro and in vivo anti-inflammatory activities of triterpene saponins from Clematis florida.

Clematis florida is widely used in She Ethnopharmacy in China owing to its significant anti-inflammatory activities. This study aimed to investigate the anti-inflammatory effect of the active fraction of C. florida (CFAF) in an arthritis animal model and its possible mechanism. Pre-inflammatory cytokine levels were examined by ELISA. CFAF can significantly improve the symptoms of arthritis such as paw swelling, arthritic index, and histological condition in AA rat. CFAF can also reduce levels of IL-1ß, TNF-α and IL-6. Further studies showed that triterpene saponins from CFAF induced anti-inflammatory activity inhibited inflammatory mediators by blocking JAK/STAT signalling pathways in the LPS-treated macrophages.

A new indole-type alkaloid from the roots of Clematis florida var. plena.

One new indole-type alkaloid, α-L-rhamnopyranosyl-(1→6)-ß-D- glucopyranosyl 6-methoxy-3-indolecarbonate (1), together with three known alkaloids (2-4), one aromatic acid (5) and five known saponins (6-10), was isolated from the roots of Clematis florida var. plena. Their structures were established by NMR spectroscopic analysis and acid hydrolysis. In in vivo anti-inflammatory activity, n-butanol extract was found to be potent against ear edema in mice, with inhibition rate of 48.7% at a dose of 800 mg/kg. Furthermore, compounds 8 and 9 obtained from the n-butanol extract exhibited significant anti-inflammatory activities with inhibition rates of 50.9% and 54.7% at a dose of 200 mg/kg.

Concurrence of Multiple Cutaneous Malignancies on Sun-exposed Vitiligo Skin of a Patient: A Case Report and Review of the Literature.

There are very few published studies in the literature examining the association between vitiligo and skin cancers and only some anecdotal reports about phototherapy-associated nonmelanoma skin carcinoma (NMSC) in patients with vitiligo. Herein, we report a case of an 84-year-old male with widespread vitiligo with concurrent onset of two primary cutaneous malignancies in sun-exposed vitiligo skin. The association between vitiligo and NMSC deserves further assessment. Chronic sun damage might be a possible causative factor for the development of NMSC in the vitiligo patient.

Essential oil from Siegesbeckia pubescens induces apoptosis through the mitochondrial pathway in human HepG2 cells.

Siegesbeckia pubescens (SP) has been used as a traditional medicine for the treatment of and inflammatory diseases. However, the activities of SP against hepatocellular carcinoma and the related mechanisms remain unclear. The present study aimed to examine the effects of the essential oil of SP (SPEO) on the proliferation of hepatocellular carcinoma cells and the possible mechanisms. The growth inhibition of HepG2 cells was analyzed by MTT assay. Hoechst 33258 and fluorescence microscopy were utilized to observe the nuclear morphological changes of apoptotic cells. Flow cytometry was used to detect cell apoptosis and cell cycle. The expressions of the target proteins were detected by Western blotting. The results showed that SPEO obviously inhibited the proliferation of HepG2 cells in a dose-dependent manner. SPEO activated a series of apoptotic proteins in HepG2 cells, increasing expression levels of Bax, caspase-3 and caspase-9, and decreasing the bcl-2 expression level. SPEO displayed promising anti-hepatocellular carcinoma activities in vitro, partly by inducing apoptosis in HepG2 cells through activating the mitochondrial pathway.

Essential Oil from Siegesbeckia pubescens Induces Apoptosis through the Mitochondrial Pathway in Human HepG2 Cells / 华中科技大学学报（医学）（英德文版）

Siegesbeckia pubescens (SP) has been used as a traditional medicine for the treatment of and inflammatory diseases.However,the activities of SP against hepatocellular carcinoma and the related mechanisms remain unclear.The present study aimed to examine the effects of the essential oil of SP (SPEO) on the proliferation of hepatocellular carcinoma cells and the possible mechanisms.The growth inhibition of HepG2 cells was analyzed by MTT assay.Hoechst 33258 and fluorescence microscopy were utilized to observe the nuclear morphological changes of apoptotic cells.Flow cytometry was used to detect cell apoptosis and cell cycle.The expressions of the target proteins were detected by Western blotting.The results showed that SPEO obviously inhibited the proliferation of HepG2 cells in a dose-dependent manner.SPEO activated a series of apoptotic proteins in HepG2 cells,increasing expression levels of Bax,caspase-3 and caspase-9,and decreasing the bcl-2 expression level.SPEO displayed promising anti-hepatocellular carcinoma activities in vitro,partly by inducing apoptosis in HepG2 cells through activating the mitochondrial pathway.

Blocking NAD(+)/CD38/cADPR/Ca(2+) pathway in sepsis prevents organ damage.

BACKGROUND: Although the nicotinamide adenine dinucleotide (NAD(+))/CD38/cyclic ADP ribose (cADPR)/Ca(2+) signaling pathway has been shown to regulate intracellular calcium homeostasis and functions in multiple inflammatory processes, its role in sepsis remains unknown. The aim of this study was to determine whether the NAD(+)/CD38/cADPR/Ca(2+) signaling pathway is activated during sepsis and whether an inhibitor of this pathway, 8-Br-cADPR, protects the organs from sepsis-induced damage. MATERIALS AND METHODS: Male Sprague-Dawley rats were subjected to cecal ligation and puncture (CLP) or sham laparotomies. NAD(+), cADPR, CD38, and intracellular Ca(2+) levels were measured in the hearts, livers, and kidneys of septic rats at 0, 6, 12, 24, and 48 h after CLP surgery. Rats were also divided into sham, CLP, and CLP+8-Br-cADPR groups, and the hearts, livers, and kidneys were hematoxylin-eosin-stained and assayed for malondialdehyde and superoxide dismutase activities. RESULTS: NAD(+), cADPR, CD38, and intracellular Ca(2+) levels increased in the hearts, livers, and kidneys of septic rats as early as 6-24 h after CLP surgery. Treatment with 8-Br-cADPR inhibited sepsis-induced intracellular Ca(2+) mobilization, attenuated tissue injury, reduced malondialdehyde levels, and increased superoxide dismutase activity in septic rats. CONCLUSIONS: The NAD(+)/CD38/cADPR/Ca(2+) signaling pathway was activated during sepsis in the CLP rat model. Blocking this pathway with 8-Br-cADPR protected hearts, livers, and kidneys from sepsis-induced damage.

HPLC-based activity profiling of anti-hepatocellular carcinoma constituents from the Tibetan medicine, Caragana tibetica.

During the screening of a traditional Chinese folk herb library against HepG2 and Hep3B cell lines, the EtOAc extract from the Tibetan medicine, Caragana tibetica (CT-EtOAc) exhibited potential anti-hepatocellular carcinoma (anti-HCC) activity. HPLC-based activity profiling was performed for targeted identification of anti-HCC activity from CT-EtOAc by MS-directed purification method. CT-EtOAc was separated by time-based fractionation for further anti-HCC bioassay by a semipreparative HPLC column (150 mm × 10 mm i.d., 5 µm) with a single injection of 5 mg. Bioassay-guided and ESIMS-directed large scale purification was performed with a single injection of 400 mg of CT-EtOAc by peak-based fractionation. A 1.4-mm heavy wall micro NMR tube with z-gradient was used to measure one and two dimensional NMR spectra for the minor or trace amounts of components of the extract. Two active compounds could be elucidated as naringenin chalcone (CT-1) and 3-hydroxy-8, 9-dimethoxypterocarpan (CT-2) relevant to anti-HCC effects for the EtOAc extract of C. tibetica rapidly and unambiguously by this protocol.

[Clinical observation on treatment of female delayed acne vulgaris with qingre cuochuang tablet].

OBJECTIVE: To observe the clinical therapeutic effect of Qingre Cuochuang tablet (QCT) in treating female delayed acne vulgaris (FDAV, with patients age more than 25 years old), to evaluate objectively the sexual hormone in patients and to assess the effect of QCT on sexual hormone. METHODS: Sixty FDAV patients were randomly divided into the treated group (n = 40) and the control group (n = 20), they were treated with QCT and western medicine (including antisterone, tetracycline and metronidazole) respectively. Besides, 10 healthy female subjects aged > or = 25 years were selected as normal control. Serum levels of testosterone (T) and estradiol (E2) in all patients and healthy subjects as well as the clinical therapeutic effect of the treatments were observed and compared. RESULTS: The total effective rate in the treated group and the control group was 92.5% and 90.0% respectively, comparison between them showed insignificant difference. Serum level of T in the patients before treatment were higher than that in healthy subjects (P < 0.01), and showed no difference between the treated group and the control group. After treatment, it lowered significantly in the treated group (P < 0.01), but unchanged in the control group, E2 level showed no significant change in both groups before and after treatment. CONCLUSION: QCT has definite clinical effect in treating FDAV, it could lower the serum level of T and with few adverse reaction.