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Ochrocephalamines B-D (1-3), composed of fused quinolizidine and octahydroquinoline rings, were isolated from Oxytropis ochrocephala Bunge. Ochrocephalamine B (1) has a unique bridged tetracyclic ring skeleton fused with a lactam ring. The structures of 1-3 were elucidated using spectroscopic and computational approaches. Ochrocephalamine C (2) and D (3) demonstrated potent anti-HBV activities and are more potent against the secretion of HBeAg than that of HBsAg.

To investigate anti-arthritic effects of matrine isolated from the roots of S. flavescens on type II collagen-induced arthritis (CIA) in rats and to explore its related potential mechanisms, CIA rats were established and administered with matrine (20, 40 or 80 mg/kg/days, for 30 days). Subsequently, blood was collected to determine serum levels of TNF-α, IL-1β, IL-6, IL-8, IL-17A, IL-10, MMP-2, MMP-3 and MMP-9, and hind paws and knee joints were collected for histopathological examination. Furthermore, indices of the thymus and spleen were determined, and synovial tissues were collected to determine the protein expressions of p-IκB, IκB, Cox-2 and iNOS. Our results indicated that matrine significantly suppressed inflammatory reactions and synovial tissue destruction. Matrine inhibited paw swelling, arthritis indices and weight loss in CIA rats. Additionally, matrine decreased the levels of TNF-α, IL-1β, IL-6, IL-8, IL-17A, MMP-2, MMP-3 and MMP-9. Matrine also down-regulated expressions of p-IκB, Cox-2, and iNOS but up-regulated IκB in synovial tissues in CIA rats. The results suggested matrine possesses an anti-arthritic effect in CIA rats via inhibiting the release of pro-inflammatory cytokines and proteins that promote the NF-κB pathway., Competing Interests: The authors declare no conflict of interest.

Ten alkaloids (1-10), with sophoridine (1) as the most abundant component, were obtained from the whole plants of Oxytropis ochrocephala Bunge. Furthermore, eight new sophoridine derivatives (11-16, 20, 21), with modification on the C-14 position of 1 were synthesized. All compounds (1-16, 20, 21) were evaluated for antiproliferative activity against five human tumor cell lines. Among them, the newly synthesized derivative 20 exhibited the best inhibitory activity against the tested cell lines. Its activity was increased by more than fourfold as compared with parent compound 1., (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Context: Endophytic fungi are microorganisms living within the tissues of host plants, and have proven to be rich sources of biologically active secondary metabolites and therefore have attracted increasing attention in recent years., Objective: To isolate and characterize bioactive constituents from the endophytic fungus cultures of Crocus sativus Linn. (Iridaceae)., Materials and Methods: Endophytes were isolated from the corm of C. sativus. Endophytic fungus cultures were subjected to repeated column chromatography. Chemical structure was elucidated based on extensive spectroscopic methods and X-ray diffraction analysis. Several pathogenic fungi isolates and tumor cell lines were employed to evaluate the antifungal and cytotoxic activities of the isolated compound., Results: An isolate of Penicillium vinaceum (strain no. X17) was obtained from the corm of C. sativus. Chemical investigations of the endophyte culture broth afforded an unique quinazoline alkaloid (1), identified as (-)-(1R,4R)-1,4-(2,3)-indolmethane-1-methyl-2,4-dihydro-1H-pyrazino-[2,1-b]-quinazoline-3,6-dione, which showed cytotoxic (IC(50) range 40.55-76.83 μg/mL) and antifungal (MIC(80) range 16-64 μg/mL) activities., Discussion and Conclusions: Endophytes in C. sativus can be a rich source of novel bioactive compounds, which prompts us to expand the medicinal resource of this valuable plant in another way. Compound 1 exhibited potential cytotoxic and antifungal activities and may be considered a lead compound for promising antifungal and anticariogenic agent.

Daphhimalenine A (1), a novel alkaloid with a rearrangement C-21 skeleton, containing a unique 1-azabicyclo[5.2.1]decane ring system, was isolated from the leaves of Daphniphyllum himalense, along with biogenetically related alkaloids daphhimalenine B (2) and daphnezomine T. Their structures were established on the basis of spectroscopic data, and the absolute configuration of 1 was assigned by computational methods. A plausible biosynthetic pathway of 1 was also proposed.

Four new Daphniphyllum alkaloids, dapholdhamines A-D (1-4), were isolated from the leaves of Daphniphyllum oldhami. The structures and relative configurations of 1-4 were elucidated on the basis of spectroscopic data.

A new alkaloid, daphenylline (1), with an unprecedented rearranged 22-nor-calyciphylline skeleton, was isolated from the fruits of Daphniphyllum longeracemosum. Its structure and stereochemistry were elucidated on the basis of spectroscopic and computational approaches. A plausible biosynthetic pathway of 1 was also proposed.

To study the correlation of the reversal effect of tetrandrine (Tet) in combination with droloxifene (DRL) on multidrug resistant cell line K562/A02 and induction apoptosis, the apoptosis of K562 cells and K562/A02 cells after the treatment of Tet and DRL alone or their combination was detected by flow cytometry (FCM). The results showed 0.62 microg/ml Tet and 1.94 microg/ml DRL alone could induce apoptosis of K562 cells in time-dependent manner after culture for 48 hours. Neither Tet at 0.62 microg/ml nor DRL at 1.94 microg/ml alone could induce apoptosis of K562/A02 cells, but in the combination of them two induced apoptosis of few K562/A02 cells in culture for 72 hours. In conclusion, the mechanism of Tet and DRL reversing multidrug resistance has no correlation with the apoptosis of K562/A02 cells.

Objective: The progress in the research on matrine was involved to provide references for the exploitation and utilization of the matrine., Method: Pharmacological functions and mechanism were reviewed according to related experimental studies., Result: Matrine has various pharmacological activities., Conclusion: Matrine has extensive applied prospect and will be developed further.

Objective: To study the reversal effect of tetrandrine (Tet) and droloxifene (Drol) on multidrug resistant cell line K562/A02 and apoptosis induction., Methods: The cytotoxicity of daunorubicin (DNR) was assayed by MTT method. The effects of Tet and DRL, alone or combined were detected through the apoptosis of K562/A02 by agarose gel electrophoresis., Results: The cytotoxicity of DNR to K562/A02 was enhanced by 0.62 microg/ml Tet or 1.94 microg/ml Drol with IC(50) 7.28 +/- 2.06 microg/ml, 7.58 +/- 3.44 microg/ml, giving a reversal effect of 2.94 and 2.82. But IC(50) of combined Tet and Drol was 1.66 +/- 0.41 microg/ml with the reversal effect markedly increased to 12.9. Neither 0.62 microg/ml Tet nor 1.94 microg/ml Drol could induce apoptosis of K562/A02 cells., Conclusion: Multidrug resistance (MDR) can be partially reversed by Tet or Drol, of which the combination shows a great synergistic reversal effect. The mechanism of Tet and Drol reversing multidrug resistance is not correlated with the apoptosis of K562/A02 cells.

Four new indole alkaloids, trigonoliimines D-G ( 1- 4, resp.), were isolated from Trigonostemon lii. Their structures were elucidated by spectroscopic methods, including extensive 1D- and 2D-NMR experiments. [ABSTRACT FROM AUTHOR]

Two new bis-alkaloids, flavifloramides A ( 1) and B ( 2), as well as two known alkaloids, N- trans-feruloyltyramine ( 3) and paprazine ( 4), were isolated from the aerial part of Piper flaviflorum. The structures of the new compounds were elucidated by spectroscopic analyses, including 2D-NMR techniques. [ABSTRACT FROM AUTHOR]

Abstract: Daphnioldhamine A, the first Daphniphyllum alkaloid with transannular effect, easily tautomerized under acidic or alkaline conditions, was isolated from the fruits of Daphniphyllum oldhami. The structure was elucidated by spectroscopic and computational approaches and chemical transformation. A plausible biosynthetic pathway of daphnioldhamine A was also proposed. [Copyright &y& Elsevier]

The article presents information on a study conducted on the isolation of alkaloids from the aerial part of the plant Piper flaviflorum, or Piperaceae. The dried and powdered material of the plant was extracted with ethanol under reflux, and after removing the solvent by vaporization, the residue extracts were suspended in water and partitioned by using petroleum ether CH2Cl2 and other compounds.

The new quinolizidine alkaloid (+)-(14β)-14-ethylmatridin-15-one (I) is isolated from the poisonous plant Oxytropis ochrocephala. [ABSTRACT FROM AUTHOR]

Ten known alkaloids are isolated from Oxytropis ochrocephala with sophoridine (I) as the most abundant component. [ABSTRACT FROM AUTHOR]

isolation, structure elucidation, and cytotoxicity of four new indole alkaloids, trigonoliimines A (I), B (IIb), C (IIa), and D (III) [ABSTRACT FROM AUTHOR]

Preliminary tests reveal that (I) exhibits no cytotoxicity. [ABSTRACT FROM AUTHOR]

Two new quinolizidine-based alkaloids, ochrocephalamines E (1) and F (2), were isolated from Oxytropis ochrocephala Bunge. Compound 1 represented the first 14-nor matrine-type alkaloid with 6/6/6/5 ring system. Compound 2 shared the aloperine-type scaffold including the C-10 location of carbonyl group. The inhibitory activities of 2 against the secretion of HBsAg and HBeAg were respectively 22.34 ± 4.38% and 18.00 ± 5.01% at the noncytotoxic concentration of 1×10-5 mol/L, which was more active than the positive control hyperoside (16.09% and 12.23%). [Display omitted] • Two new quinolizidine-based alkaloids were isolated from Oxytropis ochrocephala Bunge. • Compound 1 represented the first 14-nor matrine-type alkaloid with 6/6/6/5 ring system. • Compound 2 exhibited potential activity in inhibiting HBsAg and HBeAg secretion. Two new quinolizidine-based alkaloids, ochrocephalamines E (1) and F (2) were isolated from Oxytropis ochrocephala Bunge (Fabaceae). Their structures were elucidated by extensive spectroscopic analysis and electronic circular dichroism (ECD) calculations. Compound 1 represented the first 14-nor matrine with 6/6/6/5 ring system, while compound 2 shared the aloperine-type scaffold including the carbonyl group at C-10 postition. The inhibitory activities of 2 against the secretion of HBsAg and HBeAg were respectively 22.34 ± 4.38% and 18.00 ± 5.01% at the noncytotoxic concentration of 1 × 10-5 mol/L, which were more active than the positive control hyperoside (16.09% and 12.23%). The binding mode between compound 2 and HBV core protein was illustrated by molecular docking. [ABSTRACT FROM AUTHOR]

Abstract: A phytochemical work on the alkaloid constituents from Trigonostemon lii Y.T. Chang was conducted to give six new β-carboline alkaloids, trigonostemines A–F (1–6) and eight known β-carboline alkaloids (7–14). Their structures were elucidated by extensive spectroscopic techniques including 2D NMR experiments and mass spectrometry. All of the compounds were evaluated for their cytotoxic activities against the HL-60, SMMC-7721, A-549, MCF-7, and SW480 human cancer cell lines. Trigonostemines A and B (1 and 2) exhibited stronger inhibitory activities than the positive control (cisplatin) in some cell lines. [Copyright &y& Elsevier]

Abstract: Two novel alkaloids, trigonoine A containing a 2,8-diazabicyclo[3.3.1]nonane ring system and trigonoine B formed by a combination of a 2,3-dihydroquinolin-4-one and 3H-pyrrolo[2,3-c]quinoline rearranged from β-carboline skeleton were isolated from the leaves of Trigonostemon lii. Their structures were elucidated by 1D and 2D NMR spectroscopic methods. [Copyright &y& Elsevier]

A new alkaloid, daphenylline (1), with an unprecedented rearranged 22-nor-calyciphylline skeleton, was isolated from the fruits of Daphniphyllum longeracemosum. Its structure and stereochemistry were elucidated on the basis of spectroscopic and computational approaches. A plausible biosynthetic pathway of 1was also proposed. [ABSTRACT FROM AUTHOR]

Six new β-carboline alkaloids (I) and (II) are isolated and tested for their anticancer activity against five human cancer cell lines. [ABSTRACT FROM AUTHOR]