[Chemical constituents of Helleborus thibetanus].

The chemical constituents of Helleborus thibetanus were isolated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, and semi-preparative RP-HPLC, and the structures of all compounds were identified by modern spectrographic technology(MS, NMR). The MTT method was used to measure the cytotoxicity of compounds 1-8. Twelve compounds were isolated from the roots and rhizomes of H. thibetanus and were identified as(25R)-22ß,25-expoxy-26-[(O-ß-D-glucopyranosyl)oxy]-1ß,3ß-dihydroxyfurosta-5-en(1), ß-sitosterol myristate(2), ß-sitosterol lactate(3), ß-sitosterol 3-O-ß-D-glucopyrannoside(4), 4,6,8-trihydroxy-3,4-dihydronaphthalen-1(2H)-one(5), 1,3,5-trimethoxybenzene(6), 7,8-dimethylbenzo pteridine-2,4(1H,3H)-dione(7), 1H-indole-3-carboxylic acid(8), p-hydroxy cinnamic acid(9), lauric acid(10), n-butyl α-L-arabinofuranoside(11) and methyl-α-D-fructofuranoside(12), respectively. Among them, compound 1 is a new compound and named thibetanoside L; compounds 2, 5-8, 11 are first isolated from the family Ranunculaceae; compound 12 is isolated from the genus Helleborus for the first time. The results of MTT assay showed that the IC_(50) values of compounds 1-8 against HepG2 and HCT116 cells were greater than 100 µmol·L~(-1).

Steroidal constituents from Helleborus thibetanus and their cytotoxicities.

Thibetanosides E-H (1-4), four new steroidal constituents including three rare sulfonates (2-4), were isolated from the roots and rhizomes of Helleborus thibetanus, together with nine known steroidal compounds (5-13). Their structures were elucidated by detailed spectroscopic analysis, including 1D and 2D NMR techniques and chemical evidence. In this study, compounds 2-13 were evaluated for their cytotoxic activities against HCT116, A549 and HepG2 tumor cell lines in vitro. Among them, compound 8 (thibetanoside C) showed cytotoxicities against A549 cells(IC50 39.6 ± 1.9 µmol·L-1) and HepG2 cells(IC50 41.5 ± 1.1 µmol·L-1), respectively. Compound 9 (23S, 24S)-24-[(O-ß-D-fucopyranosyl)oxy]-3ß, 23-dihydroxy-spirosta-5, 25(27)-diene-1ß-ylO-(4-O-acetyl- α-L-rhamnopyranosyl)-(1→2)-O-[ß-D-xylopyranosyl-(1→3)]-α-L-arabinopyranoside) showed cytotoxicity against HCT116 cells(IC50 33.6 ± 2.1 µmol·L-1).

Five new polyhydroxylated furostanol saponins from the rhizomes of Tupistra chinensis.

Five new polyhydroxylated furostanol saponins were isolated from the roots and rhizomes of Tupistra chinensis, and their structures were determined as tupistrosides J-N (1-5), together with four known furostanol saponins (6-9), on the basis of physico-chemical properties and spectral analysis. Among them, compounds 3 and 5 showed cytotoxicity against human cancer cell lines SW620 with IC50 values of 72.5 ± 2.4 and 77.3 ± 2.5 µmol·L-1, respectively. Compound 4 showed cytotoxicity against human cancer cell line HepG2 with IC50 value of 88.6 ± 2.1 µmol·L-1.

Two macamide extracts relieve physical fatigue by attenuating muscle damage in mice.

BACKGROUND: Macamides, the main active components contained in maca, have attracted increasing attention due to their various bioactivities. In this study, crude macamide extract (CME) and purified macamide extract (PME) were prepared by enzyme-assisted extraction and macroporous resin separation, and the anti-fatigue effects of CME and PME were evaluated in a forced swimming model. RESULTS: The composition analysis results revealed that both CME and PME mainly contain eight kinds of macamide. Based on the results of a weight-loaded forced swimming test, compared with a control group, CME and and PME groups could prolong exhaustive swimming time, increase levels of liver glycogen (LG) and muscle glycogen (MG), accelerate fatty acid oxidation in serum to provide energy, eliminate the accumulation of blood lactic acid (BLA) and blood urea nitrogen (BUN), and decrease the serum biomarkers for muscle damage, such as lactate dehydrogenase (LDH) and creatine kinase (CK). Histological analysis also indicated that CME and PME attenuated damage to skeletal muscle and the myocardium in mice during exercise. CONCLUSION: Two macamide extracts have a beneficial effect on relieving physical fatigue by attenuating the damage of skeletal muscle and myocardium during exercise, and a better effect was observed in the PME group. © 2018 Society of Chemical Industry.

Bysspectin A, an unusual octaketide dimer and the precursor derivatives from the endophytic fungus Byssochlamys spectabilis IMM0002 and their biological activities.

Bysspectin A (1), a polyketide-derived octaketide dimer with a novel carbon skeleton, and two new precursor derivatives, bysspectins B and C (2 and 3), were obtained from an organic extract of the endophytic fungus Byssochlamys spectabilis that had been isolated from a leaf tissue of the traditional Chinese medicinal plant Edgeworthia chrysantha, together with a known octaketide, paecilocin A (4). Their structures were determined by HRMS, 1D and 2D NMR spectroscopic analysis. A plausible route for their biosynthetic pathway is proposed. Compounds 1-3 were tested for their antimicrobial activities. Only compound 3 was weakly active against Escherichia coli and Staphyloccocus aureus with MIC values of 32 and 64 µg/mL, respectively. Further, the inhibitory effects on human carboxylesterases (hCE1, hCE2) of compounds 1 and 4 were evaluated. The results demonstrated that bysspectin A (1) was a novel and highly selective inhibitor against hCE2 with the IC50 value of 2.01 µM. Docking simulation also demonstrated that active compound 1 created interaction with the Ser-288 (the catalytic amino-acid in the catalytic cavity) of hCE2 via hydrogen bonding, revealing its highly selective inhibition toward hCE2.

[Influence of Electroacupuncture Stimulation with Different Intensities and Therapeutic Intervals on Learning-memory Ability and Expression of Aß 1-40 and Arginine Vasopressin Genes in the Hippocampal CA 1 Region in VD Rats].

OBJECTIVE: To observe the influence of electroacupuncture (EA) stimulation with different electrical current intensities and therapeutic intervals on learning-memory ability and expression of ß-amyloid peptide Aß 1-40 and arginine vasopressin (AVP) genes in the hippocampal CA 1 region in vascular dementia (VD) rats, so as to provide evidence for treatment of VD. METHODS: A total of 48 male SD rats were randomly divided into sham, model, 0.5 mA-5 d-EA, 1.5 mA-5 d-EA, 0.5 mA-1 d-EA and 1.5 mA-1 d-EA groups (n=8 in each group). The VD model was established using modified 4-vessels occlusion method. EA (alternative 2 Hz/15 Hz, 0.5 mA, 1.5 mA) was applied to "Baihui" (GV 20) and "Dazhui" (GV 14) for 30 min, once a day (1 d) or once every 5 d for 10 times. The learning-memory ability was detected using Morris water maze tests (place navigation task and spatial probe trials), and the expression of Aß 1-40 and AVP genes in hippocampal CA 1 region was determined using real time-PCR. RESULTS: In comparison with the sham group, the average escape latency of place navigation task, and the duration for crossing the target-platform for the 1st time (spatial navigation task) were significantly increased (P<0.05), and the times to cross the target-platform within 2 min (spatial probe trials) were significantly decreased in the model group (P<0.05), suggesting a reduction of learning-memory ability. The expression level of Aß 1-40 mRNA was remarkably increased (P<0.05), and that of AVP mRNA notably decreased in the model group (P<0.05). Following EA intervention, the increased escape latency and the duration of crossing the target-platform for the 1st time and the increased Aß 1-40 mRNA expression, and the decreased target-platform crossing times within 2 min as well the down-regulated AVP mRNA expression level were reversed in the 4 EA groups compared with the model group (P<0.05). The therapeutic effects of higher stimulating intensity (1.5 mA-1 d-EA and 1.5 mA-5 d-EA) were markedly superior to those of lower intensity (0.5 mA-1 d-EA and 0.5 mA-5 d-EA), and the effects of higher frequency of EA intervention (0.5 mA-5 d-EA and 1.5 mA-5 d-EA) were obviously superior to those of lower frequency of EA (0.5 mA-1 d-EA and 1.5 mA-1 d-EA) in suppressing the increased 3 indexes and the decreased 2 indexes mentioned above (P<0.05). CONCLUSIONS: EA can improve the learning-memory ability of VD rats, which Feb be related to its effects in inhibiting the expression of Aß 1-40 mRNA and up-regulating the expression of AVP mRNA in hippocampal CA 1 region; and the therapeutic effects of higher stimulating intensity and higher intervention frequency are obviously better than those of lower stimulating intensity and lower therapeutic frequency.

Ardeemins and cytochalasins from Aspergillus terreus residing in Artemisia annua.

Three new alkaloids, 15b-dehydro-5- N-acetylardeemin ( 3), 10-phenyl-[12]-cytochalasins Z16 ( 6) and Z17 ( 7), were characterized from the liquid culture of the endophytic fungus ASPERGILLUS TERREUS IFB-E030 along with six known derivatives, 5- N-acetylardeemin ( 1), 15b- ß-hydroxyl-5- N-acetylardeemin ( 2), cytochalasin E ( 4), rosellichalasin ( 5), cytochalasins Z11 ( 8), and Z13 ( 9). The structures of the new metabolites were established mainly by a combination of their 1D- and 2D-NMR spectra, single crystal X-ray diffraction, and the modified Mosher reaction. Biological assays indicated that cytochalasin Z17 ( 7) had moderate cytotoxicity against human nasopharyngeal epidermoid tumor KB cell line with an IC (50) value of 26.2 µM.

Cephalosol: an antimicrobial metabolite with an unprecedented skeleton from endophytic Cephalosporium acremonium IFB-E007.

Cephalosol (1), a potent antimicrobial secondary metabolite with a new carbon skeleton, was characterized from the culture of Cephalosporium acremonium IFB-E007 that used to reside as an endophyte in Trachelospermum jasminoides (Apocynaceae). Its structure and absolute configuration were unambiguously determined by spectroscopic and computational approaches.

[Transurethral holmium laser enucleation of the prostate for the treatment of benign prostatic hyperplasia].

OBJECTIVE: To evaluate the efficacy and safety of transurethral holmium laser enucleation of the prostate (HoLEP) for the treatment of benign prostatic hyperplasia (BPH). METHODS: A retrospective review was conducted of transurethral (HoLEP) performed on 68 patients, aged 65.7 (50 - 91) with benign prostatic hyperplasia. The efficacy and complications were all assessed. RESULTS: The mean procedure time was 87 mins (45 - 158 mins). The mean specimen weight was 61 g (31 - 128 g). The procedure allows a precise, bloodless field with no need for transfusion. No TUR syndrome and other major complications were encountered during the operation. The mean catheter time and hospital stay were 2.8 d (1 - 4 d) and 3.6 d (2 - 5 d), respectively. Follow-up of 7.6 months (1 - 13 months) revealed that the urination symptoms were markedly improved in all patients, and that the IPSS decreased from 25.7 +/- 6.9 to 7.7 +/- 4.3 (P < 0.01) and the maximum urine flow rate increased from 8.1 +/- 4.2 ml/s to 18.8 +/- 4.6 ml/s (P < 0.01). Postoperative complications occurred in 3 patients. 2 with transient incontinence were recovered within 3 months postoperatively. The other one with mild posterior urethral stricture was treated effectively with urethral sounding. CONCLUSIONS: Was associated with high effectiveness, safety, short hospital stay and less complications, HoLEP is a new minimally invasive surgical procedure for BPH.