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Two previously undescribed chimonanthine-type [sinodamines A and B] and five related known dimeric tryptamine-derived alkaloids were isolated and characterized from the leaves of the endangered ornamental plant Sinocalycanthus chinensis under the guidance of LC-MS detection and dereplication analyses, along with conventional isolation procedures. Their structures were established on the basis of spectroscopic methods and chemical transformations. Sinodamine A can be regarded as the naturally occurring N-oxide derivative of its pseudo-mesomer sinodamine B. An acid-catalyzed Meisenheimer rearrangement from sinodamine A to its oxazine-form with a final equilibrium of 1:2 was observed by monitoring their NMR spectra. (−)-Folicanthine showed significant cytotoxicity against human lung carcinoma A549 and colorectal carcinoma HT29 cells, with IC50 values of 7.76 and 6.16 μM, respectively.

Chemical investigation on Pilea aquarum subsp. brevicornuta led to the identification of three previously unknown dimeric p-menthene-type monoterpene peroxides, pileadimenthenols A-C (1–3). Their chemical structures and absolute configurations were determined by extensive spectroscopic analyses, X-ray crystal diffraction and ECD calculations. Plausible biogenesis of 1–3 was also proposed. Among the isolates, 2 showed weak cytotoxic activity against HCT-116.

Pinus kwangtungensis is an endangered pine species native to China. In the present study, 15 diterpenoids including three new labdane-type analogs were isolated and characterized during a pioneer phytochemical investigation on a mass-limited sample of the needles and twigs of this plant, which is growing in a Cantonese garden. The new structures, (4S,5R,9S,10R)-6-oxo-labd-7,13-dien-16,15- olid-19-oic acid (1), 15(S)-n-butoxypinusolidic acid (2), and β- d -glucopyranosyl- (4S,5R,9S,10R)-labda-8(17),13-dien-15,16-olid-19-oate (3), were established by extensive spectroscopic methods and some chemical transformations. Among the isolates, lambertianic acid (10) and cassipourol (15) showed inhibitory activities against human protein tyrosine phosphatase 1 B (PTP1B), a target for the treatment of type-II diabetes and obesity, with IC50 values of 25.5 and 11.2 μM, respectively.

Two rare rearranged cuparane-type sesquiterpenoid C-10 epimers [beshanzuenones A (1) and B (2)] and two bisabolane-type sesquiterpenoid spirolactones [beshanzuenones C (3) and D (4)] featuring an unusual [6/6/5]-fused tricyclic ring system were isolated from the shed trunk barks of Abies beshanzuensis, one of the critically endangered plant species in the world. The structures of these four new enone-containing sesquiterpenoids were determined by spectroscopic analyses and single-crystal X-ray diffraction or electronic circular dichroism (ECD) calculations. Compounds 1 and 2 showed considerable activity against the H3N2 virus, whereas 3 and 4 exhibited significant inhibition on PTP1B.

Two new Lycopodium alkaloids, strictumines A (1) and B (2), along with 18 related known compounds were isolated from the whole plant of Lycopodium obscurum L. f. strictum. The structures of the new compounds were established by spectroscopic methods and chemical transformation. This is the first report on chemical constituents of the title plant. All the isolates were evaluated for their inhibitory activity against acetylcholinesterase (AChE), and only a few were found to show slight bioactivity.

Nineteen compounds mainly including pyrrole-containing alkaloids and phytosterols were isolated from the EtOH extract of the fermented mycelia of Xylaria nigripes, a precious medicinal fungus known as Wuling Shen in Chinese. On the basis of spectroscopic methods, the structures of the new naturally occurring compounds were determined to be (4S)-3,4-dihydro-4-(4-hydroxybenzyl)-3-oxo-1H-pyrrolo[2,1-c][1,4]oxazine-6-carbaldehyde (1), methyl (2S)-2-[2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl]-3-(4-hydroxyphenyl)propanoate (2), and 3-{4-[(2R)-(2,3-dihydroxy-3-methylbutoxy]phenyl}-7-hydroxy-4H-chromen-4-one (3), respectively. The absolute configurations of 1 and 2 were deduced by the observed Cotton effects in their circular dichroism (CD) spectra, whereas that of the 1,2-diol moiety in 3 was determined using the Snatzke's method. Their biological activities such as neuroprotective, anti-neuroinflammatory, and cytotoxic properties were also reported.

Four new sesquiterpenoids named pileaterpenes A-D (1–4), together with three known sesquiterpenoids (5–7), were isolated from Pilea aquarum subsp. brevicornuta. The chemical structures of the new compounds were tentatively established by extensive spectroscopic methods and quantum chemical calculations. The absolute configurations of 1–3 were further determined by X-ray crystal diffraction, the modified Mosher’s method or ECD calculation method. All isolates but 7 were evaluated their activities against interleukin-8 (IL-8) production in HT-29 cells induced by IL-1β.

In this review, we intensively focus on the advances in research of natural products (NPs) discovery carried out by domestic scholars in China from 2015 through 2017. In general, a total of 1811 publications (1479 in English and 332 in Chinese) were accumulated regarding newly isolated NPs from plants, microorganisms, and marine sources. As a result, 277 selected papers concerning naturally occurring compounds with extraordinary frameworks, origins, and promising activities were discussed in this review article, mainly organized according to their structural classes and novelties.

Two new [named xylapyrrosides A (1) and B (2)] along with two known [pollenopyrrosides A (3) and B (=acortatarin A, 4)] naturally occurring spirocyclic pyrrole alkaloids were isolated and identified as minor components from the EtOH extract of the dried mycelia of the edible medicinal fungus Xylaria nigripes. Their structures were established by a combination of interpretation of spectroscopic data and single-crystal X-ray diffraction analyses. The isolates possess a unique tricyclic skeleton comprising a common bicyclic 2-formyl-pyrrole-fused morpholine, with a variable ketohexoside ring. This class of alkaloids is quite rare from natural sources. In this study, the total syntheses of compounds 1, 2 and 4 were successfully achieved by two alternative strategies, and three new analogs [named xylapyrrosides A1 (1a), A2 (1b) and B1 (2a)] were also produced. Notably, the total synthesis of such spiroketal alkaloids with a pyranose ring (e.g.,1) was accomplished for the first time. The absolute configurations of the new isolates can be thereafter unequivocally secured by the total syntheses. The above isolated and synthesized spiro-alkaloids were found to show moderate antioxidant effects by preventing the oxidative stress-induced cytotoxicity of A7r5 rat vascular smooth muscle cells (VSMCs).

Two new [named salicifoxazines A (1) and B (2)] and six known dimeric tryptamine-derived alkaloids (3–8) were isolated from the leaves of Chimonanthus salicifolius. The new structures were established on the basis of extensive spectroscopic methods and chemical transformations. The absolute configuration of 1 was determined by the observed Cotton effects in its circular dichroism (CD) spectrum, whereas 2 is a pseudo-mesomer of 1. In fact, the first two naturally occurring asymmetric tetrahydro-1,2-oxazine-containing tryptamine-derived alkaloids 1 and 2 are diastereoisomers at C-3a/C-8a or at C-3a′/C-8a′. Compounds 1, 2, (−)-chimonanthine (3), and meso-chimonanthine (4) were found to show moderate cytotoxic effects against human colorectal carcinoma cells (SW-1116 and HCT-116) and/or gastric carcinoma cells (SGC-7901).

Fourteen new ent-abietane-type diterpenoids, sessilifols A-N (1-14), and three related new norditerpenoids (15-17) were isolated from Chloranthus sessilifolius. The absolute configurations were determined by single-crystal X-ray diffraction analysis, the modified Mosher's method, and/or the observed Cotton effects in their electronic circular dichroism spectra. Sessilifols A (1) and B (2) possess an uncommon five-membered C-ring rearranged by oxidative cleavage of the C-13/C-14 bond in abieta-7,13-diene followed by the formation of a new C-C bond between C-12 and C-14. Sessilifol C (3) is a rare 7,8-seco-9-spiro-fused ent-abietane, whereas sessilifol O (15) represents the first example of a naturally occurring 14-norabietane-type diterpenoid. Compounds 6 and 9 were found to have moderate antineuroinflammatory activities by inhibiting the nitric oxide production in lipopolysaccharide-stimulated murine BV-2 microglial cells, with IC50 values of 8.3 and 7.4 μM, respectively.

Four novel naturally occurring diastereoisomers of dinor-eudesmenes, named chloranthones A-D (1-4, resp.), were isolated as minor components from the EtOH extract of the aerial parts of Chloranthus elatior. The unprecedented framework was established using extensive 2D-NMR techniques. Their absolute configurations were deduced from the observed Cotton effects in their circular dichroism (CD) spectra. A plausible biosynthetic pathway to the dinor-eudesmenes is proposed.

Ethnopharmacological relevance The dried stems of Clematis armandii (Caulis clematidis armandii), named “Chuan-Mu-Tong” in Chinese Pharmacopoeia, have been traditionally used as an herbal remedy mainly for inflammation-associated diseases. The Aim of the study is to identify the potential anti-neuroinflammatory components from Clematis armandii. Materials and methods The ethanol extract of “Chuan-Mu-Tong” was suspended in H2O and exhaustively extracted with CH2Cl2. The CH2Cl2 fraction was successively subjected to column chromatography (CC) over silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures of the isolated compounds were identified by spectroscopic methods and by comparison with those reported in the literature. Their anti-neuroinflammatory activities were evaluated by inhibitory effects on pro-inflammatory mediators [e.g. nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α)] in lipopolysaccharide (LPS)-activated BV-2 cells. Results One new and sixteen known lignans were isolated and characterized. The absolute configuration of the new lignan, (7R,8S)-9-acetyl-dehydrodiconiferyl alcohol (1), was elucidated by a combination of 1D/2D NMR techniques and the Electronic Circular Dichroism (ECD) spectroscopy based on the empirical helicity rules. The anti-neuroinflammatory bioassay showed that compounds 1, (7R,8S)-dehydrodiconiferyl alcohol (2), erythro-guaiacylglycerol-β-coniferyl ether (5), and threo-guaiacylglycerol-β-coniferyl ether (6) displayed significant inhibitory effects on NO production. Among them, neolignans 1 and 2 exhibited more potent activities than the positive control (NG-monomethyl- l -arginine , l -NMMA), with an IC50 value of 9.3 and 3.9 μM, respectively. Moreover, both 1 and 2 were also found to concentration-dependently suppress the TNF-α release in LPS-stimulated BV-2 cells. Conclusion The results revealed that lignans are the major components of “Chuan-Mu-Tong”, and their anti-neuroinflammatory activities strongly support the traditional application of this herb medicine on inflammation. Moreover, the dihydrobenzo[b]furan neolignans 1 and 2 as well as Caulis clematidis armandii could be further exploited as new therapeutic agents to treat inflammation-mediated neurodegenerative and aging-associated diseases.

In search of anti-inflammatory lead compounds from traditional Chinese medicines, a bioassay-guided phytochemical study on Melastoma dodecandrum was carried out. As a result, 18 compounds have been isolated. Their chemical structures were determined on the basis of their physicochemical properties and spectral data. Among the isolates, three pentacyclic triterpenoids, ursolic acid (1), asiatic acid (3) and terminolic acid (6), together with one tannin casuarinin (17), were found to significantly decrease interleukin-8 (IL-8) production in human colon cancer cells. The results imply, at least in part, that the anti-inflammatory effect of M. dodecandrum could be due to inhibition of IL-8 production, demonstrated by these naturally occurring compounds described above.

One (formosumone A, 1) new and fifteen (2-16) known phenolic compounds were isolated from the leaves of Cratoxylum formosum ssp. pruniflorumm, a substitute for the popular bitter nail tea ("Kuding Tea") generally used in Southeast Asia. Their structures were determined by extensive spectroscopic analysis and by comparison with literature data. Compound 1 possesses a rare scaffold of a flavanone coupled with a phloroglucinol moiety, representing the first example of such a scaffold from the Clusiaceae family. Among the isolates, toxyloxanthone B (11) and vismione D (12) were found to show remarkable anti-neuroinflammatory effects by inhibiting nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine BV-2 microglial cells. Additionally, toxyloxanthone B (11) exhibited significant neuroprotective effect against β-amyloid(25-35) (Aβ(25-35))-induced cell viability decrease in SH-SY5Y neuroblastoma cells.

This is an updated fingerprint profile for the simultaneous identification of 29 compounds, mainly including characteristic -terpene trilactones and flavonoid glycosides from Ginkgo biloba leaves (EGb) by employing a high-performance liquid chromatography-photodiode array-evaporative light scattering detector method. Compounds 1 and 6 had not been previously either detected or described in any EGb samples. In general, these 29 compounds were distributed into 5 regions in the fingerprint according to their different structural properties. This efficient analytical method could be generally applied to the quality control of EGb761 and other commercially available EGb products in the Chinese active pharmaceutical ingredients market.

Six new (leonurusoleanolides E-J, 1-6) and five known (7-11) nortriterpenoids were isolated and characterized from the dried fruits of Leonurus japonicus. They all contain a distinctive 19(18→17)-abeo-28-noroleanane-type spirocylclic skeleton with a trans or a cis acyl substituent at C-3 or C-23. Similar to the previously known leonurusoleanolides A/B (7/8) and C/D (9/10), compounds 1/2 and 3/4 were also found to exist as equilibrium mixtures of trans and cis isomers. The isolated pure compounds and mixtures were evaluated for their cytotoxicity against a small panel of human cancer cell lines (BGC-823 and KE-97 gastric carcinoma, Huh-7 hepatocarcinoma, Jurkat T cell lymphoblasts, and MCF-7 breast adenocarcinoma) using the CellTiter-Glo luminescent cell viability assay method. Among them, (2α,3β,17R*,18β)-3-O-(trans-caffeoyl)-19(18→17)-abeo-28-norolean-12-ene-2,18,23-triol (leonurusoleanolide J, 6) showed the most potent cytotoxic activity, with IC50 values less than 10 μM.

Thirteen sesquiterpenoids were isolated from the EtOH extract of the aerial parts of Chloranthus elatior . On the basis of spectroscopic methods, the structures of the new naturally occurring compounds were elucidated to be (1 R ,4 R ,5 R ,8 S ,10 R )-1-hydroxy-4-methoxy-eudesm-7(11)-en-12,8-olide (1) , 1 α H,5 β H,6 α H,7 α H-4 β ,10 β ,15-trihydroxyaromadendrane (2) , and (1 S ,4 S ,5 S ,6 R ,7 R ,10 S )-1,4-dihydroxymaaliane (3) , respectively.

A novel dimeric diterpene (named trichotomone, 1 ) was isolated from the roots of the medicinal ornamental plant Clerodendrum trichotomum . Compound 1 is a rare phenolic ketal of a regular abietane derivative cyrtophyllone B and a rearranged abietane derivative containing a 17(15→16),18(4→3)- diabeo -abietane framework related to uncinatone. The structure was elucidated by extensive spectroscopic methods. The absolute configuration was defined by comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Trichotomone ( 1 ) exhibited in vitro cytotoxicities against several human cancer cell lines (A549, Jurkat, BGC-823 and 293T WT) with IC 50 values ranged from 7.51 to 19.38 μM.

Two new phloroglucinols, named eucalyptals D (1) and E (2), along with a related known compound (euglobal-In-3, 3) were isolated from the fruits of Eucalyptus globulus. Their structures were established on the basis of extensive spectroscopic studies, revealing that they share a common 3,5-diformyl-isopentyl phloroglucinol unit, but each is instead coupled to a different sesquiterpenoid skeleton (aromadendrene in 1, cadinene in 2, and a spirosesquiterpene in 3). Compound 1 possessed an unusual seven-membered D ring with an ether bridge between C-2 of the aromadendrene moiety and C-2′ of the aromatic unit. The absolute configuration of the isolates was defined by the comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1–3 exhibited significant in vitro cytotoxicities against a few human cancer cell lines (Huh-7, Jurkat, BGC-823, and KE-97) using the CellTiter-Glo™ luminescent cell viability assay method.

Twelve new ent-abietane diterpenoids, chlorabietins A–L (1–12), were isolated from the roots of Chloranthus oldhamii. Their structures and absolute configurations were determined by extensive spectroscopic analyses, X-ray diffraction, and experimental/calculated electronic circular dichroism (ECD) spectroscopy. Among the new isolates, chlorabietins D (4) and E (5) are the first two naturally occurring 8-spiro-fused 9,10-seco-ent-abietanes containing an unexpected cis-fused A/B ring system. Chlorabietin F (6) is a rare chinane-type diterpenoid featuring a hitherto unknown C-ring cleavage between C-13 and C-14, which might be derived from a common precursor of the above spiro-diterpenoid epimers 4 and 5, and their biosynthetic relationships are briefly discussed. Meanwhile, chlorabietin I (9) is the first representative of the abietane-type diterpenoids possessing a tetrahydrofurano function bridging C-6 and C-19. Chlorabietins B (2), C (3), F (6), and G (7) showed anti-neuroinflammatory effects by inhibiting the nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine BV-2 microglial cells, with IC50 values ranging from 16.4 to 33.8 μM.

Both beshanzuenones A (Ia) and B (Ib) show considerable activity against the H3N2 virus, whereas beshanzuenones C (IIa) and D (IIb) exhibit significant inhibition on the human PTP1B enzyme.

Nine unexpected new flavonol glycoside cyclodimers in the truxinate (1–7, biginkgosides A–G, respectively) or truxillate [biginkgosides H (8) and I (9)] forms were isolated as minor components from the extract of Ginkgo biloba leaves. The new dimers possess an unusual cyclobutane ring formed by a [2+2]-cycloaddition between two symmetric (for compounds 1–5 and 7–9) or nonsymmetric (for 6) flavonol coumaroyl glucorhamnosides. A plausible biosynthetic pathway for these new compounds based on the frontier molecular orbital theory of cycloaddition reactions is briefly discussed. An antineuroinflammatory screening revealed that biginkgosides E (5) and H (8) inhibited nitric oxide production in lipopolysaccharide-activated BV-2 microglial cells, with IC50 values of 2.91 and 17.23 μM, respectively. Additionally, biginkgoside F (6) showed a significant neuroprotective effect (34.3% increase in cell viability at 1 μM) against Aβ25–35-induced cell viability decrease in SH-SY5Y neuroblastoma cells.

Compounds (I), (II), and (III) are isolated from the ethanol extract of the fermented mycelia of Xylaria nigripes.

Twelve new ent-abietane diterpenoids, chlorabietins A–L (1–12), were isolated from the roots of Chloranthus oldhamii. Their structures and absolute configurations were determined by extensive spectroscopic analyses, X-ray diffraction, and experimental/calculated electronic circular dichroism (ECD) spectroscopy. Among the new isolates, chlorabietins D (4) and E (5) are the first two naturally occurring 8-spiro-fused 9,10-seco-ent-abietanes containing an unexpected cis-fused A/B ring system. Chlorabietin F (6) is a rare chinane-type diterpenoid featuring a hitherto unknown C-ring cleavage between C-13 and C-14, which might be derived from a common precursor of the above spiro-diterpenoid epimers 4 and 5, and their biosynthetic relationships are briefly discussed. Meanwhile, chlorabietin I (9) is the first representative of the abietane-type diterpenoids possessing a tetrahydrofurano function bridging C-6 and C-19. Chlorabietins B (2), C (3), F (6), and G (7) showed anti-neuroinflammatory effects by inhibiting the nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine BV-2 microglial cells, with IC50 values ranging from 16.4 to 33.8 μM.

During a further and comprehensive phytochemical investigation on the shed trunk barks of the critically endangered plant Abies beshanzuensis, one new (1) and ten known (2–11) lignans with diverse structures were isolated. On the basis of spectroscopic methods, the new structure was established to be (7S,8R,8′R)-4′-methoxyl-α-conidendrin (1). Among the isolated lignans, (−)-matairesinol (5) and (−)-arctigenin (6) showed significant anti-neuroinflammatory activities by inhibiting the overproduction of nitric oxide in lipopolysaccharide-stimulated murine BV-2 microglial cells, with IC50 values of 11.5 and 19.0 μM, respectively.

The EtOH extract of the aerial parts of Xanthium sibiricum afforded six sesquiterpene lactones (STLs), including two new eremophilanolides. The structures of the new compounds were established on the basis of spectroscopic methods and the modified Mosher's method to be the C-11 epimers of 2 S ,4 S ,5 R ,7 R ,8 R -2-hydroxy-eremophil-1(10)-en-12,8-olide [11 R : 1 (sibiriolide C); 11 S : 2 (sibiriolide D)]. The isolated compounds were evaluated for their in vitro cytotoxicities against five human cancer cell lines (Huh-7 hepatocarcinoma, KB nasopharynx carcinoma, Jurkat T cell lymphoblast, BGC-823 and KE-97 gastric carcinoma) using the CellTiter-Glo™ luminescent cell viability assay method. Compounds 4 – 6 , each possessing an α -methylene- γ -lactone moiety, were found to have noteworthy cytotoxic effects with IC 50 values ranging from 1.1 to 18.0 μM.

Two new phloroglucinols, named eucalyptals D (1) and E (2), along with a related known compound (euglobal-In-3, 3) were isolated from the fruits of Eucalyptus globulus. Their structures were established on the basis of extensive spectroscopic studies, revealing that they share a common 3,5-diformyl-isopentyl phloroglucinol unit, but each is instead coupled to a different sesquiterpenoid skeleton (aromadendrene in 1, cadinene in 2, and a spirosesquiterpene in 3). Compound 1 possessed an unusual seven-membered D ring with an ether bridge between C-2 of the aromadendrene moiety and C-2′ of the aromatic unit. The absolute configuration of the isolates was defined by the comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1–3 exhibited significant in vitro cytotoxicities against a few human cancer cell lines (Huh-7, Jurkat, BGC-823, and KE-97) using the CellTiter-GloTM luminescent cell viability assay method.

A new tetrastilbene named carasinol D (1) was isolated from the roots of Caragana sinica. Its structure was elucidated by spectroscopic analysis. Compound 1 was obtained from carasinol B (2) by an acid-catalyzed conversion.

In a continual effort to search for any anti-HIV agent from traditional Chinese medicine, one new resveratrol tetramer, cararosinols B, was isolated from the ethanol extract of aerial parts of Caragana rosea . Its structure was elucidated by spectroscopic analysis and comparison with known compounds.

Three unprecedented phloroglucinol-diterpene adducts, chlorabietols A–C (1–3), were isolated from the roots of the rare Chloranthaceae plant Chloranthus oldhamii. They represent a new class of compounds, featuring an abietane-type diterpenoid coupled with different alkenyl phloroglucinol units by forming a 2,3-dihydrofuran ring. Their structures were elucidated by detailed spectroscopic analysis, molecular modeling studies, and electronic circular dichroism calculations. Compounds 1–3 showed inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 12.6, 5.3, and 4.9 μM, respectively.

Four new diastereomers of dinor-eudesmenes, named chloranthones A-D (Ia)-(Id), are isolated as minor components from the EtOH extract of the aerial parts of Chloranthus elatior.

Ten new lycodine-type alkaloids, named casuarinines A-J (1-10), along with eight known analogues (11-18), were isolated from the whole plant of Lycopodiastrum casuarinoides . The new structures were established by spectroscopic methods and chemical transformations. Casuarinines A-D (1-4) and J (10) are common lycodine alkaloids possessing four connected six-membered rings, while tricyclic casuarinines E-H (5-8) are the piperidine ring cleavage products. In particular, casuarinine I (9) has an unprecedented five-membered tetrahydropyrrole ring instead of the piperidine ring. A plausible biosynthetic pathway to 9 is proposed. Among the compounds reported, casuarinine H (8) exhibited significant neuroprotective effect against hydrogen peroxide (H₂O₂)-induced neuronal cell damage in human neuroblastoma SH-SY5Y cells, while casuarinines C (3) and I (9) showed moderate inhibitory activity against acetylcholinesterase (AChE).

Four ( 1 – 4 ) hitherto unknown and seven ( 5 – 11 ) known ergostane-type sterols were isolated from the EtOH extract of the dried fruiting bodies of the polypore macrofungus Fomes fomentarius . On the basis of spectroscopic analysis, the structures of polyhydroxylated sterols 1 – 4 were elucidated to be (22 E ,24 R )-3 β ,5 α ,6 β ,14 α -tetrahydroxyergosta-7,9(11),22-triene (fomentarol A, 1 ), (22 E ,24 R )-3 β ,5 β ,6 α ,7 α -tetrahydroxy-8 α ,9 α -dihydroergosta-14,22-diene (fomentarol B, 2 ), (22 E ,24 R )-3 β ,5 α -dihydroxy-6 β -ethoxyergosta-7,22-diene (fomentarol C, 3 ), and (22 E ,24 S )-3 β ,25-dihydroxy-15 α - O - β - d -glucopyranosylergosta-7,22-dien-6-one (fomentarol D, 4 ), respectively. Rings A/B and B/C are in turn cis -fused in compound 2 , which is uncommon in natural ergostane-type sterols. The potential biogenetic relationship of 2 and other ergostane-type sterols isolated from F. fomentarius was briefly discussed. Moderate cytotoxic effects of the isolated sterols against a small panel of human cancer cell lines were also established.

The roots of the medicinal ornamental plant Clerodendrum trichotomum yielded a series of rearranged abietane diterpenoids, including three 17(15 → 16)-abeo-abietane (1–3) and three 17(15 → 16),18(4 → 3)-diabeo-abietane (4–6) derivatives. Their structures were elucidated by means of spectroscopic methods. The absolute configuration of (10R,16R)-12,16-epoxy-11,14,17-trihydroxy-6-methoxy-17(15 → 16)-abieta-5,8,11,13-tetraene-7-one (1) was deduced by a combination of single crystal X-ray diffraction analysis and the observed Cotton effects in its circular dichroism (CD) spectrum. All isolates were tested for their cytotoxicities against five human cancer cell lines (BGC-823, Huh-7, KB, KE-97, and Jurkat). Among them, compounds 4, 6, 9, 10, 12, and 14, each possessing a common 17(15 → 16),18(4 → 3)-diabeo-abietane framework, were found to have remarkable cytotoxic effects with IC50 values ranging from 0.83 to 50.99 μM.

The methanol extract of the whole plant of Hedyotis chrysotricha demonstrated cytotoxicity against SK-HEP-1 human hepatocarcinoma cells in a primary screening for novel antitumour agents. Bioassay-guided fractionation and purification led to an active principle (24S)-ergostane-3β,5α,6β-triol (1) along with four inactive compounds (2-5). The in vitro transwell migration assay showed that compound 1 remarkably reduced the migration of SK-HEP-1 cells by 78.9% at a dose of 30 µM, without any apoptotic effect on this cell line. Moreover, all the isolated compounds were further evaluated for their cytotoxicities against another four human cancer cell lines (MCF-7, NUGC3, SH-SY5Y and PC-3).

To investigate whether mesenchymal stem cells (MSCs) transplantation after acute myocardial infarction (AMI) can improve heart function and decrease infarct size in rabbits and their correlation.Twenty-four rabbits were randomly divided into AMI group and MSCs group, each n=12. Exogenous MSCs labeled with bromodeoxyuridine (BrdU) were injected into the border and central area of the ischemic myocardium. Heart function was assessed with echocardiography before transplantation of MSCs and in 6th week after the transplantation. Surviving MSCs in infarcted myocardium were identified by immunohistochemistry. Infarct size was measured histologically. Correlation of heart function and infarct size were analysed.Immunohistochemical stain revealed that BrdU-positive cells were seen in the infarcted myocardium in MSCs group but not in AMI group. Transplantation of MSCs was associated with a significant diminution of left ventricular end-diastolic dimension (LVEDD), and left ventricular end-systolic dimension (LVESD, both P0.05), and left ventricular ejection fraction (LVEF) and fractional shortening (DeltaFS%)increased (both P0.05) as compared with AMI group. Infarct size as measured histologically was significant smaller in MSCs group than AMI group (P0.05). There were negative correlations between LVEF and infarct size in two groups (both P0.01).Exogenous MSCs transplantation can improve heart function by decreasing infarct size and therefore it might be beneficial in the treatment of AMI.

This study was intended to look for anti-HIV chemical constituents of aerial parts of Caragana rosea Turcz. Column chromatographic technique was used for the isolation and purification of constituents of Caragana rosea under the guide of anti-HIV assay. The structures were established on the basis of physical and chemical properties and spectroscopic data. Five compounds were obtained from the EtOAc fraction of aerial parts of Caragana rosea and identified as myricetin (1), mearnsetin (2), p-hydroxy cinnamic acid (3), cararosinol A (4) and cararosinol B (5). At the same time, one possible transformation route between cararosinol B and kobophenol A, another resveratrol tetramer isolated from this plant previously, was proposed. Compounds 4, 5 are new resveratrol tetramers, compounds 1 -3 were isolated from this plant for the first time. All compounds showed no activities in an in vitro assay against HIV-1.

Nineteen new derivatives of the naturally occurring compound, goniothalamin, were prepared by chemical modification and semi-synthetic methods. The antitumor activities of these derivatives and goniothalamin were evaluated in vitro against human tumor cell lines, and most of them showed an inhibitory effect against HL-60 cancer cells. The derivatives 10-nitro-goniothalamin and 10-amino-goniothalamin gave selective inhibition concentration (IC50) of 1.10 and 1.14 microg/ml, respectively, against human stomach cancer SGC-7901 cells, while that of etoposide (vp-16) as the positive control was 6.07 microg/ml. Finally, the partition coefficients, logP (pi values), of these derivative molecules, were evaluated by calculating the additive approximate organic fragment logP value.