Pegaharolines A - I, structurally novel indole alkaloids with anti-HSV-2 virus activities from Peganum harmala L. seeds.

Leading by the antiviral activities against HSV-2 virus, bioactivity-guided the fraction of crude alkaloids from seeds of Peganum harmala led to the isolation of nine structurally novel indole alkaloids, pegaharolines A - I (1-9), and 11 known ones (10-20). Compound 3 was an unusual 6/5/5/5 spirotetracyclic indole-derived alkaloids featuring a classic bicyclic indole unit fused with an additional pyrrolizine ring via a spiral atom (C-3). Compound 4 was determined as a novel indole alkaloid, characterized with a rare hexacyclic 6/5/6/5-6/6 ring system, by a single-crystal X-ray diffraction.

Lindenane sesquiterpenoid dimers from Chloranthus holostegius with anti-neuroinflammatory activities in BV-2 microglia.

Fifteen undescribed lindenane-type sesquiterpenoid dimers, designated chloranholides F-T (1-15), together with twenty-five known analogs (16-40), were isolated from the whole plants of Chloranthus holostegius. The isolate structures were elucidated by analysis of spectroscopic data and chemical methods, and their absolute configurations were determined by X-ray crystallography and electronic circular dichroism spectra. In anti-neuroinflammatory assays, all isolates were evaluated by examination of their inhibitory effect on nitric oxide (NO) in LPS-stimulated BV-2 cells, and the results showed that 21-24, 26, 30, 32 and 36 significantly inhibited the production of the inflammatory mediator NO, with IC values ranging from 3.

Two new clerodane diterpenoids and a new pyran-2-one derivative with anti-neuroinflammatory activities from Croton crassifolius.

Two new clerodane diterpenoids (1 and 2), a new pyran-2-one derivative (3), along with five known compounds (4‒8), were isolated from Croton crassifolius. Notably, crassifolin X (1) is a novel clerodane diterpenoid, characterized with a peculiar δ-lactone core being formed between C-1 and C-4. Their structures, including absolute configurations, were established on the basis of spectroscopic methods (UV, IR, HRESIMS and NMR), and circular dichroism experiments.

Three new compounds isolated from the whole plants of pall.

One new alkaloid, 6, 7-dimethoxyisoquinoline--oxide (), one new benzofuran derivative, 3,7-dimethyl-6-acetyl-8-benzofuranol () and one new lignan, salsolains A (), along with seven known compounds (-), were isolated from the whole plant of Pall. Their structures were elucidated by extensive analysis of spectroscopic data (IR, UV, HR-ESI-MS, 1 D and 2 D NMR), and their absolute configurations were determined by the X-ray crystallography and ECD calculation. The activities of compounds - against inflammatory cytokines IL-6 and TNF- levels on LPS-induced RAW 264.

Water-soluble matrine-type alkaloids with potential anti-neuroinflammatory activities from the seeds of Sophora alopecuroides.

A phytochemical investigation on the alkaloids from water-soluble part of Sophora alopecuroides led to obtain forty matrine-type alkaloids (1-40) including eighteen new ones (1-18), which covers almost all positions of the oxygen substitution in matrine-type structure. Notably, eight compounds (1-8) belong to rare bis-amide matrine-type alkaloid. The new structures were determined based on extensive spectroscopic data, electronic circular dichroism (ECD) calculations, and six instances, verified by X-ray crystallography.

Stilbene dimer xylosides and flavanols from the roots of Lysidice rhodostegia and their antioxidant activities.

Eight new stilbene dimer xylosides (1-8) and one new flavanol (9), along with seven known ones (10-16) were isolated from the roots of Lysidice rhodostegia. Their structures were elucidated by extensive analysis of spectroscopic data (IR, UV, HR-ESI-MS, 1D and 2D NMR), ECD calculations and acid hydrolysis. Compounds 1-16 were evaluated for their antioxidant activities using DPPH radical-scavenging assay.

Three new sesquiterpene lactones from the whole plants of .

Three new sesquiterpene lactones, named scabertopinolides H - J (-), along with four known ones, desacylisodeoxyelephantopin 2-methylbutyrate (), iso-17,19-dihydrodeoxyelephantopin (), scabertopinolide D () and 6,7,8)-8-tigloyloxy-1(10),4(5),11(13)-germacratrien-2,15,6,12-diolide () were isolated from the whole plants of . Their structures were elucidated by extensive analysis of spectroscopic data (including IR, UV, HRESIMS, 1 D and 2 D NMR) and single-crystal X-ray. These isolated compounds showed effective anti-inflammatory effects on LPS-stimulated RAW 264.

β-Carboline Alkaloids from the Seeds of and Their Anti-HSV-2 Virus Activities.

Pegaharines A-G (-), six novel β-carboline alkaloids representing three types of skeleton, were isolated from the seeds of . Compound is a peculiar β-carboline alkaloid characterized by the unprecedented carbon skeleton of an azepine-indole system. Compounds - represent the first examples of heterodimers constructed from rare tetracyclic β-carboline and classic tricyclic β-carboline alkaloids.

One new sesquiterpene pyridine alkaloid from the stems and leaves of .

A new sesquiterpene pyridine alkaloid (), along with four known compounds (-), were isolated from the stems and leaves of . The new structure was determined by extensive spectroscopic analyses (IR, UV, NMR, HRESIMS and ECD). In addition, compound showed a stronger anti-respiratory syncytial virus (RSV) activity with an IC value of 1.

Two new isoquinoline alkaloids from the seeds of .

Two new isoquinoline alkaloids, 6 ,6a--nantenine -oxide (), 6,6a--nantenine -oxide (), along with nine known alkaloids, nantenine (), oxonantenine (), protopine (), nornantenine (), -methyl-laurotetanine (), isocorydine (), -methyflavinantine (), -methyl-2,3,6-trimethoxymorphinan-dien-7-one -oxide () and (+)-10--methylhernovine -oxide () were isolated from the seeds of Their structures were elucidated by extensive analyses of spectroscopic data (IR, UV, HRESIMS, 1 D and 2 D NMR), ECD calculation and comparison with the related literatures. In addition, the cytotoxicity against A549 cells of these alkaloids was determined by the MTT assay.

Hyperpatulones A-F, polycyclic polyprenylated acylphloroglucinols from and their cytotoxic activities.

Six new compounds, hyperpatulones A-F (1-6), along with ten additional known related derivatives (7-16), were isolated from (Guttiferae). Their structures were elucidated by extensive analysis of spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR), X-ray crystallography, electronic circular dichroism (ECD) spectroscopy and Rh(OCOCF)-induced ECD. All compounds were tested for their cytotoxic activities on human HepG-2, HeLa, MCF-7, and A549 cell lines 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.

Isolation and identification of new prenylated acetophenone derivatives from .

Three new prenylated acetophenone derivatives, acronyculatin P (), acronyculatin Q (), and acronyculatin R () were isolated from the leaves of . Their structures were identified by extensive analyses of spectroscopic data (IR, UV, ESI-HRMS, 1D and 2D NMR) and comparison with the literatures. In addition, the cytotoxic activity against MCF-7 cells of the compounds were evaluated by the MTT assay and the IC values were 56.

Sophalines E-I, Five Quinolizidine-Based Alkaloids with Antiviral Activities against the Hepatitis B Virus from the Seeds of Sophora alopecuroides.

Five novel quinolizidine-based alkaloids (1-5) were obtained from the seeds of Sophora alopecuroides L. Compounds 1 and 2 are the first examples of sparteine-indolizine and matrine-indolizine alkaloids, respectively, whereas 3 and 4 are epimeric normatrine-julolidine alkaloids with unusual skeletons. The structures of these compounds were determined by spectroscopic methods, single-crystal X-ray diffraction, and electronic circular dichroism analyses.

Cytotoxic and anti-inflammatory active phloroglucinol derivatives from Rhodomyrtus tomentosa.

Seven undescribed phloroglucinol derivatives, tomentodiones N-T, and eleven known ones were isolated from Rhodomyrtus tomentosa. Tomentodione N is the first example of a β-triketone unit coupled with an isoamyl alcohol through a furan fused-ring, and tomentodiones N, S, T were three racemates. The undescribed structures were elucidated by means of spectroscopic, X-ray diffraction, electronic circular dichroism calculation, and chemical methods.

Sesquiterpene lactones from Elephantopus mollis and their anti-inflammatory activities.

Seven sesquiterpene lactones, 8-O-methacryloylelephanpane, 2,4-bis-O-methyl-8-O-methacryloylelephanpane, 4-O-ethyl-8-O-methacryloylelephanpane, 8-O-methacryloylisoelephanpane, 2-O-demethyltomenphantopin C, molephantin A, molephantin B, along with ten known ones, were isolated from Elephantopus mollis (Asteraceae). Their structures were elucidated by extensive analysis of spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The isolates were evaluated for their anti-inflammatory activities on LPS-stimulated RAW 264.

Four Matrine-Based Alkaloids with Antiviral Activities against HBV from the Seeds of Sophora alopecuroides.

Four novel matrine-based alkaloids (1-4) were isolated from the seeds of Sophora alopecuroides. Compounds 1 and 2 possess unprecedented 6/6/6/4 and 6/5/6/6 ring systems, respectively, while 3 and 4 are a pair of stereoisomeric matrine-acetophenone alkaloids with an unusual skeleton. Their structures were elucidated by means of spectroscopic methods and single-crystal X-ray diffraction.

Three new diterpenoids from Croton laui Merr. et Metc.

Three new diterpenoids, including one labdane diterpenoid (1) and two cembrane diterpenoids (2-3), were isolated from the aerial parts of Croton laui, along with four known analogues (4-7). Their structures were elucidated by spectroscopic analysis and comparison with literature data. All compounds were evaluated for their cytotoxicity against two tumour cell lines.

New labdane diterpenoids from Croton laui and their anti-inflammatory activities.

Nine new labdane diterpenoids (1-9) were isolated from the aerial parts of Croton laui, along with eight known analogues (10-17). Their structures were identified on the basis of the spectral data (IR, UV, HRESIMS, 1D and 2D NMR), and the structure of 8 was confirmed by single crystal X-ray diffraction analyses. In addition, compounds 1, 4, 7, 8, and 14 showed weak anti-inflammatory activities in LPS-stimulated RAW 264.

Diterpenoid Alkaloids from Delphinium ajacis and Their Anti-RSV Activities.

Five new diterpenoid alkaloids, ajacisines A-E (-), were isolated from , along with seven known alkaloids (-). On the basis of their spectral data (IR, UV, HR-ESI-MS, 1D and 2D NMR) and chemical properties, the structures of compounds - were identified. All isolated compounds were evaluated for their antiviral activities against respiratory syncytial virus, and compounds - and exhibited moderate to weak effects with IC values of 75.

Molecular and functional characterization of a candidate sex pheromone receptor OR1 in Spodoptera litura.

Olfaction is primarily mediated by highly specified olfactory receptors (ORs). Here, we cloned and identified an olfactory receptor, named SlituOR1 (Genbank no. JN835269), from Spodoptera litura and found evidence that it is a candidate pheromone receptor.

New Phloroglucinol Derivatives from the Fruit Tree Syzygium jambos and Their Cytotoxic and Antioxidant Activities.

Seven new phloroglucinol derivatives (1-7) were isolated from the fruit tree Syzygium jambos together with four known triterpenoids (8-11) and two known flavones (12 and 13). According to the spectroscopic analyses (infrared, electrospray ionization mass spectrometry (ESIMS), high-resolution ESIMS, 1D and 2D nuclear magnetic resonance), the structures of compounds 1-7 were elucidated as jambone A (1), jambone B (2), jambone C (3), jambone D (4), jambone E (5), jambone F (6), and jambone G (7). All the isolates were determined for their cytotoxic activities on melanoma cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and compounds 10 and 11 showed potent activities.

Six new prenylated acetophenone derivatives from the leaves of Acronychia oligophlebia.

Six new prenylated acetophenone derivatives were isolated from the leaves of Acronychia oligophlebia. The chemical structures of them were elucidated by extensive analysis of spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The cytotoxic activity of the isolates was evaluated against MCF-7 cells.

Molecular identification and characterization of the Orco orthologue of Spodoptera litura.

A highly conserved and broadly expressed receptor protein Orco (olfactory coreceptor) is crucial for insect olfaction, and an orthologue of Orco has been identified in several insect species. Here we report the identification and characterization of Orco from Spodoptera litura. The protein displays high primary amino acid sequence conservation with other previously identified Orco orthologues.

Induced epigenetic modifications of the promoter chromatin silence survivin and inhibit tumor growth.

Anti-apoptotic survivin is over-expressed in a variety of human carcinomas and is considered as a therapeutic target in cancers. Suppression of survivin mRNA by RNAi and anti-sense nucleotides has proved to be a powerful anti-tumor therapy in both animal models and human investigations. In this communication, we tested an alternative approach to silence survivin by knocking down its gene transcription through a short methylated oligonucleotide (SurKex) that is complementary to the survivin gene promoter.