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One novel spirolactone, aquilarisinolide (1), three new sesquiterpenoids, (2R,4S,5R,7R)-2-hydroxyeremophila-9,11-dien-8-one (2), (1R,4S,5S,7R,11R)-13-hydroxyepidaphnauran-9-en-8-one (3), and (4R,5S,7R,8S,10S,13R)-8,13-dihydroxyrotunda-1,11-dien-3-one (4), together with 13 known compounds (5–17) were isolated from the resinous heartwood of Aquilaria sinensis (Thymelaeaceae). The structures of the new compounds were elucidated based on the analysis of NMR and MS data and theoretical calculations their ECD spectra. The isolated compounds were evaluated for their protective activities against PC12 cell injury induced by corticosterone (CORT) and 1-methyl-4-phenylpyridine ion (MPP+), as well as inhibitory activities against BACE1. Compound 4, 5,6-dihydroxy-2-(2-phenylethyl)chromone (5), daphnauranol B (7), 6-methoxy-2-[2-(3-methyoxyphenyl)ethyl]chromone (10), isoagarotetrol (14), and 1-hydroxy-1,5-diphenylpentan-3-one (16) showed significant protective effects on CORT-induced injury in PC12 cells at a concentration of 20 μM (P 14) showed a significant protective effect on MPP+-induced injury in PC12 cells at a concentration of 20 μM (P 4 showed a moderate activity (P Graphic Abstract

Dendrobium Sw. is one of the largest genera in the orchidaceous family and includes 900–2000 species. Among them, more than 80 Dendrobium species have been reported in China. However, there are only six Dendrobium species, namely, D. bigibbum var. superbum (syn. D. phalaenopsis), D. chrysanthum, D. fimbriatum, D. loddigesii, D. nobile, and D. officinale (syn. D. candidum), listed in the New Inventory of Existing Cosmetic Ingredients in China Launched. Artificial planting of Dendrobium species has been a great success in China. To better utilize Dendrobium resources for medicinal and cosmetic purposes, we summarize their traditional uses and pharmacologically active compounds for treating dermatological disorders in this review. “Orchidaceae”, “Dendrobium”, “traditional use”, “ethnobotany”, “dermatological disorder”, and “skin disease” were used as search terms to screen the literature. Cited references were collected between 1970 and 2020 from the Web of Science, China National Knowledge Internet (CNKI), SciFinder, Google Scholar, and Chinese books. From the search, it was found that there are 22 Dendrobium species with traditional uses in dermatological disorders, and 131 compounds from Dendrobium plants have been reported to possess anti-inflammatory, antimicrobial, antioxidant, antiaging, anti-psoriasis, and tyrosinase-inhibitory activities, implying that Dendrobium plants are important resources for the discovery of active compounds and the development of new drugs and cosmetics. D. crepidatum, D. denneanum, D. loddigesii, D. nobile, and D. officinale have been extensively studied. More research on other Dendrobium species is needed. The major active compounds found in Dendrobium species are phenanthrenes, alkaloids, flavonoids, phenylpropanoids, and lignans. Several compounds, such as loddigesiinol A, (S)-5-methoxy-2,4,7,9-tetrahydroxy-9,10-dihydrophenanthrene, (S)-4-methoxy-2,5,7,9-tetrahydroxy-9,10-dihydrophenanthrene, 2,5-dihydroxy-4-methoxy-phenanthrene 2-O-β-d-glucopyranoside, (9R)-1,2,5,9-tetrahydroxy-9,10-dihydrophenanthrene 5-O-β-d-glucopyranoside, (+)-homocrepidine A, and vicenin 2, have significant anti-inflammatory activities and inhibit nitric oxide (NO) production with IC50 values less than 5 μM, and these compounds are worthy of further study. Graphic Abstract

In the Qinba mountainous area of Central China, pig farming has a significant impact on the growth of the rural economy and has substantially increased farmer incomes. Traditional knowledge plays an important role in the selection of forage plant species for pig farming by local people. This study aimed to identify the forage plants used for pig feeding and to catalog indigenous knowledge regarding their use. During 2016 and 2017, ethnobotanical surveys and inventories were conducted in Zhuxi County, Hubei Province, China. Data were collected using semi-structured interviews, key informant reports, free listings, guided field walks, and participatory observations with 77 households in 16 villages in 13 towns/townships. The obtained data were analyzed using a relative frequency citation (RFC) index. Overall, 145 wild forage plants from 91 genera and 31 families were recorded. The most cited families were Asteraceae, Polygonaceae, Urticaceae, Amaranthaceae, Fabaceae, Cruciferae, Caryophyllaceae, and Lamiaceae. Whole plants (75.9%) and tender leaves (12.4%) were the most frequently used parts of the plants. Most of the forage plants were herbaceous (88.9%). Almost all forage plants could be collected throughout the year (62.7%). Raw and cooked were the two main preparation methods. The most frequently cited species were Taraxacum mongolicum, Bidens pilosa, Sonchus oleraceus, Pilea verrucosa, and Pilea pumila var. obtusifolia. A total of 14 species were identified as the top forage plants in Zhuxi County based on their RFC values (RFC value greater than 0.5). Local people possess rich traditional knowledge about the utilization and management of forage plants for pig feeding. However, the maintenance of this traditional knowledge may be seriously threatened by changes in pig feeding modes and the lack of successors. Appropriate strategies and action plans have been suggested for the conservation of traditional knowledge associated with biodiversity and the sustainable use of forage species resources. These include 1) taking targeted measures to protect forage resources and associated traditional knowledge; 2) strengthening research on the forage plants with the highest RFC values for nutritional value, digestibility, other functions, and ecological status; and 3) enhancing the identification of poisonous forage plants.

A comprehensive analytic strategy was performed to study the acaricidal activity ingredients of Bacillus velezensis W1, a strain for biological control of Tetranychus urticae. Through genome mining, 14 biosynthetic gene clusters were identified, which encode secondary metabolites, and these were further confirmed by MALDI-TOF-MS or LC-ESI-MS/MS, including bacillomycin D C13–C17, macrolactin A, 7-O-malonyl-macrolactin A, surfactin C14, and surfactin C15. Moreover, 27 volatile compounds were identified by GC-MS, mainly including cyclodipeptides, alkanes, organic acids, and esters. Finally, 43 compounds identified from W1 were used in the virtual screening of acaricidal activity. The results showed that 16 compounds, including cyclodipeptides, bacillomycins, macrolactins, and surfactins, have acaricidal potential. This work provides a base for studying the mechanism of acaricidal action of B. velezensis W1 and a comprehensive strategy for the study of active ingredients from biocontrol strains.

Two new compounds, named carpabrotalactone C (1) and methyl 8-[2(5H)-furanon-5-yl]octanoate (2), were isolated from the herbs of Carpesium abrotanoides L. The structures of these compounds were elucidated based on spectroscopic analysis, single crystal X-ray diffraction analysis and ECD calculation. Compound 1 exhibited potent cytotoxicity against the A549, SMMC-7721, MCF-7 and SW480 cell lines, with IC50 values from 11.46 to 23.68 μM. Meantime, compound 1 showed weak inhibitory eff ;ects on LPS-induced NO release in RAW 264.7 cell lines, with IC50 value of 63.23 ± 2.55 μM.

Our previous study demonstrated that the total saponins from Paris forristii (PCT3) had obvious inhibitory effect on the proliferation of adriamycin-resistant human breast adenocarcinoma cells (MCF-7/ADM), and this effect was significantly stronger than that in parental cells (MCF-7). This study was designed to test the reversal effect of PCT3 on MCF-7/ADM cells and to understand its mechanism of action. Results demonstrated that low cytotoxic concentrations of PCT3 (0.3, 1 and 3 µg/mL) reversed resistance of MCF-7/ADM cells to ADM, cisplatin (DDP) and 5-fluorouracil (5-FU), with reversal fold of 16.4, 19.5 and 31.7 for ADM, 1.6, 1.4 and 1.4 for DDP, 1.7, 1.8 and 5.6 for 5-FU, respectively. Moreover, PCT3 significantly increased the accumulation of ADM and Rhodamine 123 (Rh123) in MCF-7/ADM cells, suggesting that PCT3 may act by affecting the function of drug efflux pump P-glycoprotein (P-gp), which is encoded by MDR1 gene. Both MDR1 gene and P-gp protein expression was downregulated by PCT3 treatment. Further results demonstrated that p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinase (ERK) pathway was remarkably activated in MCF-7/ADM cells, inhibition of p38 or ERK attenuated P-gp expression. While, only the phosphorylation level of ERK was downregulated by PCT3, indicating that PCT3 sensitized P-gp overexpressed MCF-7/ADM cells to ADM via inhibition of ERK signaling pathway.

Two new 2H-pyran-2-one glucosides, cuscutarosides A (1) and B (2), and one new steroidal glucoside, 7β-methoxy-β-sitosterol 3-O-β-glucopyranoside (3), together with 12 known compounds (4–15) were isolated from the whole plant ofCuscuta reflexa(Convolvulaceae) collected from Myanmar. The chemical structures of these new compounds were elucidated based on extensive spectroscopic analysis. The antiobesity activity of these isolates was evaluated using porcine pancreatic lipase (PPL), and the antiplatelet aggregation activity was screened using rabbit platelets induced by thrombin, platelet-activating factor (PAF), arachidonate (AA), or collagen. 7β-Methoxy-β-sitosterol 3-O-β-glucopyranoside (3) showed weak PPL inhibitory activity. Cuscutaroside A (1), its acetylated derivative (1a), and scrophenoside B (8) showed weak inhibitory activity against rabbit platelet aggregation induced by collagen. Compound1aalso showed inhibitory activity against rabbit platelet aggregation induced by AA.Graphic Abstract

Two new amides tricholomines A (1) and B (2), along with nine known compounds, were isolated from the dried fruiting bodies of Tricholoma bakamatsutake. Their structures were determined on the basis of extensive spectroscopic analysis or comparison with the data in the literatures. The absolute configuration of 1 was confirmed by single crystal X-ray diffraction analysis.

Four undescribed and two known cucurbitane-type triterpenoids, including two heterodimers, elaeocarpudubins A and B, were isolated from the branches of Elaeocarpus dubius (Elaeocarpaceae). The chemical structures of these undescribed isolates were determined by analyses of 1D and 2D NMR and MS data, electronic circular dichroism (ECD) calculations, and chemical transformation. Biogenetically, elaeocarpudubins A and B might be derived from cucurbitacin F through Michael addition with vitamin C and (-)-catechin, respectively. These six isolates were evaluated for their cytotoxic activities against human leukemia HL-60, human lung adenocarcinoma A549, human hepatoma SMMC-7721, human breast cancer MCF-7, human colon cancer SW480, and paclitaxel-resistant A549 (A549/Taxol) cell lines, for their antioxidant properties using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, and for their differentiation effects on nerve growth factor (NGF)-mediated neurite outgrowth in rat pheochromocytoma PC12 cells. Cucurbitacins F (IC

Objectives. To explore the effective and safe medicines for treating diabetes. Methods. Hydroalcoholic extracts of 130 medicinal plants belonging to 66 families were evaluated using porcine pancreatic lipase (PPL) inhibition and glucose uptake methods together with a literature review. Results. The extracts of 22 species showed the PPL inhibition activity; 18 extracts of 15 species stimulated glucose uptake in 3T3-L1 adipocytes. Among them, Mansonia gagei J.R. Drumm., Mesua ferrea L., and Centella asiatica (L.) Urb. exhibited both activities. The extracts of Caladium lindenii (André) Madison rhizomes and Azadirachta indica A. Juss. leaves presented the utmost lipase inhibitory activity with IC50 of 6.86 ± 0.25 and 11.46 ± 0.06 μg/mL, respectively. The extracts of Coptis teeta Wall. rhizomes and Croton tiglium L. seeds stimulated the maximum glucose uptake. Ten species are reported to have antidiabetic activity for the first time. Flavonoids and triterpenoids are the dominant antidiabetic compounds in selected medicinal plants from Myanmar. Conclusions. P. zeylanica, L. cubeba, H. crenulate, M. gagei, C. teeta, and M. ferrea are worthy to advance further study according to their strong antidiabetic activities and limited research on effects in in vivo animal studies, unclear chemical constitutes, and safety.

Nine new alkaloids, (+)-1, (-)-1, 2, (+)-3, (-)-3, and 4-7, along with five known compounds (8-12), were obtained from the branches and leaves of Elaeocarpus angustifolius. The alkaloids were structurally characterized by NMR and MS data. The absolute configurations of (+)-1, (-)-1, (+)-3, and (-)-3 were determined by comparing their experimental and computed electronic circular dichroism spectra. (±)-8,9-Dehydroelaeocarpine (5), (±)-9-epielaeocarpine cis-N-oxide trifluoroacetate (6), and (±)-elaeocarpine trifluoroacetate (9) exerted weak inhibitory activities against butyrylcholinesterase with IC50 values of 39, 29, and 35 μM, respectively, while that of tacrine, the positive control, was 0.07 ± 0.01 μM. This is the first report of the cholinesterase inhibitory activities of Elaeocarpus alkaloids.

A new p-terphenyl, 2',3'-diacetoxy-4,5,5',6',4'',5''-hexahydroxy-p-terphenyl (1), along with 12 known compounds were isolated from the fruiting bodies of Sarcodon imbricatus (Bankeraceae). Their st...

Objective To clarify the active constituents of the heartwoods of Caesalpinia sappan, a traditional Chinese medicine with the functions of promoting blood circulation (Huoxue in Chinese) and removing blood stasis (Quyu in Chinese). Methods The chemical constituents were isolated and purified by combination of silica gel and Sephadex LH-20 column chromatography, along with semipreparative HPLC. Their chemical structures were established by multiple spectroscopic methods and comparison with literature data. The in vitro antiplatelet aggregation activities were evaluated using mouse platelet induced by AYPGKF-NH2, a gold agonist of protease-activated receptor 4 (PAR4). Results Two new phenols, methyl 2-(4,4′,5′-trihydroxy-2′-(methoxymethyl) biphenyl-2-yloxy) acetate (1) and 1′-methylcaesalpin J (2), together with 24 known compounds (3-26), were isolated from the heartwoods of C. sappan. Among them, sappanchalcone (16) and brazilin (20) showed inhibitory activities against mouse platelet aggregation with IC50 values of 114.8 μmol/L and 100.8 μmol/L, respectively. Conclusion Antiplatelet compounds from C. sappan targeting at PAR4 are reported for the first time.

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.

Background Douyu Village, inhabited by the Lhoba people, is situated within the Eastern Himalayas, in southeastern Tibet, China. The village is located among high mountains and valleys, which feature complex terrain with cold and dry climates and distinctive vegetation types and species. The Lhoba people in this village are isolated from other groups in China. The Lhoba people have lived in this village since the 15th century and mainly depended on gathering, hunting, and swidden agriculture before the 1960s. Because they have a long history and live under extreme climatic, geographical, and ecological conditions, the Lhoba people in Douyu Village may have unique traditional knowledge about wild plants. Thus, this research aims to record the traditional botanical knowledge of the Lhoba people in Douyu. Methods An ethnobotanical study was conducted on the Lhoba people in Douyu Village in Longzi County, Tibet, China. Semi-structured interviews and group discussions with informed consent were used in the study. We interviewed 41 informants (14 key informants) between 18 and 75 years of age. All information was collected, organized, and compiled into “use reports” for quantitative analysis. The informant consensus factor (ICF) was used to determine the homogeneity of the informants’ knowledge of medicinal plants, while the cultural importance index (CI) was used to estimate the cultural importance of shared species. Results A total of 91 wild species (90 vascular plants and 1 fungus) belonging to 71 genera and 39 families utilized by the Lhoba people in Douyu were documented. Of these species, Pimpinella xizangense and Wikstroemia lungtzeensis are endemic to Longzi County, while Sinopodophyllum hexandrum and Paeonia ludlowii are endangered species in China. All habitats, from the field vegetation at the valley bottoms to the alpine shrubland and meadows, were used for plant collection, and the numbers of species of plants collected from the various vegetation types (except for fields) decreased with increasing altitude. Our study found that 55 species are edible plants and fungi, 29 species are medicinal plants, and 38 species are used for other purposes. Medicinal plants are used for 11 categories of diseases, among which diseases of blood-forming organs (ICF = 0.96) and gastrointestinal diseases (ICF = 0.95) exhibited the highest ICF values. Based on the CI values, the most important plants in this study area are Berberis xanthophloea, B. kongboensis, Sinopodophyllum hexandrum, Vicatia thibetica, and Hippophae rhamnoides subsp. gyantsensis. Moreover, a comparison of the wild plants used by Lhoba ethnic groups in three counties in China showed significant differences among these regions. Conclusions Our study demonstrates that the wild plants utilized by the Lhoba people in Douyu Village are highly diverse, at 90 plant and one fungal species, which reflects not only the number of species but also their diversified functions. The extreme climatic, geographical, and ecological conditions of Douyu within the high mountains and valleys of the Eastern Himalayas potentially affect the Lhoba people’s culture, including plant utilization practices, and contribute to the rich diversity of the wild plants used by the local people.

Ethnopharmacological relevance In China, shi hu (stems of Dendrobium chrysotoxum Lindl, D. fimbriatum Hook. D. huoshanense Z.Z. Tang & S.J. Cheng, or D. nobile Lindl) and tie pi shi hu (stems of D. officinale Kimura et Migo) are famous traditional medicines and are listed in the Chinese Pharmacopoeia. However, the leaves of these Dendrobium plants are largely discarded. Aim of the study To better utilize Dendrobium leaves, we summarize their traditional uses, chemical constituents, pharmacological activities, and toxicological effects. Materials and methods “Orchidaceae”, “Dendrobium”, “leaf”, “traditional use”, and “ethnobotany” were used as search terms to screen the literature. Cited references were collected between 1960 and 2020 from the Web of Science, China National Knowledge Internet (CNKI), SciFinder, and Google Scholar, primarily in English and Chinese. Results Traditional uses of leaves from 16 Dendrobium species were identified in the literature. The major uses of Dendrobium leaves include treatments for dermatologic disorders, metabolic syndromes, nervous system disorders, and musculoskeletal system disorders. More than 50 chemical compounds have been identified in the leaves of 10 Dendrobium species, which primarily include flavonoids, bibenzyls, coumarins, N-containing compounds, and polysaccharides. Antihyperlipidemia, antihypertensive, antihyperuricemia, anti-inflammatory, antimicrobial, antioxidant, cytotoxic and antitumor, hepatoprotective, immunomodulatory, lipase-inhibitory, and/or tyrosinase-inhibitory activities have been reported for the leaves of six Dendrobium species. D. officinale leaves have been shown to exhibit no reproductive toxicity against male rats, while D. speciosum Sm. leaves have been observed to exhibit slight genotoxicity in an in vitro study. Among Dendrobium species, D. officinale leaves are the most widely studied. Conclusions D. officinale leaves represent a good example of the utilization of leaf resources of the Dendrobium genus. In the future, more extensive research for the development of Dendrobium leaves is needed.

One new sesquineolignan, piperneolignan A (1), four new neolignans, piperneolignans B–E (2–5), and eight known compounds were isolated from the leaves of Piper betle (Piperaceae) collected from Myanmar. These new structures were determined by analysis of MS and NMR data, and the absolute configuration of piperneolignan A was elucidated by electronic circular dichroism (ECD) calculations. Piperneolignan A (1), piperneolignan B (2), hydroxychavicol (6), p-hydroxycinnamaldehyde (10), and diallylcatechol (13) possessed anti-inflammatory activity against nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine macrophage RAW 264.7 cells with IC50 values of 9.87, 45.94, 4.80, 26.40, and 40.45 μM, respectively, compared with the positive control NG-monomethyl- l -arginine ( l -NMMA, IC50 = 33.84 μM). The two hydroxy groups in the structure of hydroxychavicol are essential for activity, and dimerization or trimerization of hydroxychavicol decreases activity.

Six undescribed compounds, including three sesquiterpenoids [(4S,5S,7S,8S,11R)-7-hydroxyguai-1(10)-en-8,12-olide, aquilarisinone, and 2Z,7(13),9E-humulatrien-12-ol-5-one], one diphenylpentanone [1-(2-hydroxyphenyl)-5-phenylpentan-3-one], and two 2-(2-phenylethyl)chromones (6-epiagarotetrol and triepoxyhexahydrochromone A), along with 15 known compounds, were isolated from the resinous heartwood of Aquilaria sinensis (Thymelaeaceae). Their structures were determined by mass (MS) and nuclear magnetic resonance (NMR) spectroscopic data. The absolute configuration of (4S,5S,7S,8S,11R)-7-hydroxyguai-1(10)-en-8,12-olide was confirmed by X-ray diffraction analysis, and the configurations of (4S,7S,8S,10R,11R)-7,10-epoxyguai-1(5)-en-8,12-olide, aquilarisinone, 6-epiagarotetrol, and triepoxyhexahydrochromone A were confirmed by electronic circular dichroism (ECD) calculations. The neuroprotective activities of the compounds were evaluated using models of BACE1 inhibition and PC12 cells with corticosterone- and 1-methyl-4-phenylpyridine ion (MPP+)-induced damage. At concentrations of 1, 2, and 5 μM, triepoxyhexahydrochromone A, (+)-(7R,10R)-selina-4,11(13)-diene-12,15-dial, (−)-(5R,7R,10R)-12,15-dioxo-α-selinene, and (+)-(1R,4S,5R)-1β-hydroxyeremophila-7(11),9-dien-8-one exerted significant protective effects (p

One undescribed amide, pipermullesine A, two undescribed isoquinoline alkaloids, pipermullesines B and C, and six undescribed dipeptides, pipermullamides A–F, along with 28 known compounds, were isolated from the aerial parts of Piper mullesua. The structures of the undescribed compounds were elucidated based on the analysis of 1D and 2D NMR and MS data. Furthermore, the structures of pipermullesines A–C were confirmed by single crystal X-ray diffraction analysis. All isolates were evaluated for inhibitory activity against platelet aggregation induced by thrombin (IIa) or platelet-activating factor (PAF). (-)-Mangochinine, pellitorine, and (2E,4E)-N-isobutyl-2,4-dodecadienamide showed weak inhibitory activity against rabbit platelet aggregation induced by PAF, with IC50 values of 470.3 µg/mL, 614.9 µg/mL, and 579.7 µg/mL, respectively. Graphical Abstract Electronic supplementary material The online version of this article (10.1007/s13659-018-0180-z) contains supplementary material, which is available to authorized users.

Ethnopharmacological relevance Chong-lou (Paris polyphylla var. yunnanensis or P. polyphylla var. chinensis) is traditionally used as an anticancer medicine in China. It is also the material basis of some Chinese patent anticancer medicines, such as Gan-Fu-Le capsules, Bo-Er-Ning capsules, Lou-Lian capsules, Ruan-Jian oral liquid, and Qi-Zhen capsules. P. forrestii, a substitute for Chong-lou, is planted at a large scale in the Yunnan Province of China. Aim of the study To clarify the active chemical constituents of P. forrestii and evaluate the in vitro and in vivo anticancer activities of the total saponins from P. forrestii. Materials and methods The total saponins of P. forrestii were extracted and separated to yield pure compounds by chromatographic techniques, and the structures of the isolates were elucidated by spectroscopic methods. The cytotoxicity of the crude extracts, total saponins, and chemical constituents were evaluated using an MTS assay. In vivo antitumor activities of the total saponins from P. forrestii were measured using H22 tumor-bearing mice by intraperitoneal (ip) administration. Results Eight compounds, including polyphyllin D (1), formosanin C (2), dioscin (3), diosgenin-3-O-α- l -rhamnopyranosyl-(1→2)-β- d -glucopyranoside (4), paris saponin H (5), pennogenin-3-O-α- l -rhamnopyranosyl-(1→2)-[α- l -rhamnopyranosyl-(1→4)]-β- d -glucopyranoside (6), pariposide A (7), and crustecdysone (8), were isolated from the total saponins of P. forrestii. The total saponins and compounds 1–6 showed significant inhibitory activity against the growth of the HL-60, SMMC-7721, A-549, MCF-7, and SW480 cell lines. The total saponins from P. forrestii had a tumor-inhibitory effect in H22 tumor-bearing mice upon ip (2.25 mg/kg dose) administration, with an inhibition rate of 42.6% compared with cisplatin (ip, 2 mg/kg dose, 53.9% inhibition rate). Conclusion The results support that P. forrestii could be a substitute for P. polyphylla var. yunnanensis as an anticancer medicine.

A new modified abietane diterpenoid, (3S,4S,5R,10S)-18(4→3)-abeo-3,4,12,18-tetrahydroxy-8,11,13-abietatrien-7-one (1), and two novel dimers, selaginedorffones A (2) and B (3), featuring a new cyclohexene moiety that was biogenetically constructed from two modified abietane diterpenoids through a Diels–Alder reaction were obtained from a methanolic extract of Selaginella moellendorffii, a traditional Chinese herb. The structures of 1–3 were identified by a combination of NMR spectroscopic analysis and ECD calculations. In the present study, diterpenoids were identified from S. moellendorffii for the first time, which supports the presence of diterpene synthases in this plant. These three diterpenoids (1–3) were evaluated for their growth-inhibitory activities against several human cancer cell lines. Of these substances, selaginedorffone B (3) showed cytotoxicity against the MCF-7 human-breast-cancer-cell line (IC50 9.0 μM).

There are many methods describing defects induced by ion implantation, but none are capable of describing it quantitatively. In order to solve this problem, we studied the magnetic change of silicon carbide (SiC) after ion implantation, and found that even if the implantation intensity and defects were increased, we found that all samples have the same paramagnetic background. In this paper, we use the paramagnetic characteristics shown by part of the defects to characterize the degree of defects. We studied how to characterize the concentration of the defect, using the Brillouin function to fit the data, validated the experimental results and analyzed the relationship between paramagnetic center concentration and defects.

Nine new alkaloids, (+)

A new

Paris forrestii is a unique plant found in Tibet and Yunnan, China, and total saponins from Paris forrestii (PCT3) contain anticancer steroid glycosides. RNA expression plays an important role in various biological processes. However, the cytotoxicity effects and mechanisms of PCT3 in relation to prostate cancer (PCa) cells have not yet been reported. In the present study, the antitumor activity of PCT3 on PCa cells was evaluated. PCT3 displayed potent anticancer effects toward PCa cells that were similar to the effects of pure saponins from P. forrestii, but PCT3 had less activity in suppressing the prostate epithelial cell line RWPE. Furthermore, using CCK-8 assays, Edu incorporation, colony formation assays, Annexin V/PI assays and western blotting, we found that treatment with 4 μg/mL PCT3 significantly decreased proliferation and induced apoptosis in PCa cells. Using wound healing and transwell assays, we demonstrated that treatment with 2 μg/mL PCT3 significantly suppressed the migration and invasion of PCa cells. To explore the molecular mechanisms behind the anticancer effect of PCT3, PCT3 (5 μg/mL) treated and untreated PCa cells (LNCAP and PC3 cell lines) were analyzed using transcriptomics. Taking the commonly differentially expressed genes (log2FC > 0.585) in both cell lines, 41 mRNAs and 5 lncRNAs were eventually identified. Bioinformatics analysis (GO and KEGG analyses) revealed that some genes involved in classical cell proliferation and apoptosis pathways were aberrantly expressed after PCT3 treatment of PCa cells. By using q-PCR, the expression levels of NEAT1, MALAT1, TIPIN, LYAR, IQGAP3, GINS2, and ZGRF1 were validated as consistent with microarray data, suggesting that these genes might participate in the PCT3 anticancer effect. The present study suggests that PCT3 exhibits an anticancer effect on PCa and reveals some crucial lncRNAs and mRNAs that are involved in the anticancer mechanisms of PCT3 on Pca.

The medicinal plant Tirpitzia sinensis has been used by the Zhuang ethnic people in mountainous areas of Southwest China to stop bleeding, invigorate blood circulation, and treat inflammation and wounds. In order to further explore its traditional medicinal uses, the phytochemical constituents of this species were examined. Three new compounds, the lignan tirpitzin (1), the flavonoid tirpitzoside (2), and the furan-glycoside tirpitziol (3), along with five known compounds were isolated from the aerial part of T. sinensis for the first time. The structures of these compounds were elucidated by 1D and 2D NMR, LC/MS, IR spectrometric methods and compared with published data. The results of an in silico pharmacophore-based analysis showed potential targets of the new compounds, including ERBB2, IRAK4, LCK, JAK2, MAPK14, and MMP-12. These targets suggested that 1–3 may be involved with wound-healing and/or inflammation, leading to an in vitro assay of nitric oxide (NO) inhibition assays with lipopolysaccharide-induced BV-2 cells. All three new compounds displayed moderate NO inhibitory activity with the IC50 values of 14.97 ± 0.87, 26.63 ± 1.32, and 17.09 ± 2.3 μM, respectively.