LncRNA CCAT1 knockdown suppresses tongue squamous cell carcinoma progression by inhibiting the ubiquitination of PHLPP2.

Tongue squamous cell carcinoma (TSCC) is prevailing malignancy in the oral and maxillofacial region, characterized by its high frequency. LncRNA CCAT1 can promote tumorigenesis and progression in many cancers. Here, we investigated the regulatory mechanism by which CCAT1 influences growth and metastasis of TSCC. Levels of CCAT1, WTAP, TRIM46, PHLPP2, AKT, p-AKT, and Ki67 in TSCC tissues and cells were assessed utilizing qRT-PCR, Western blot and IHC. Cell proliferation, migration, and invasion were evaluated utilizing CCK8, colony formation, wound healing and transwell assays. Subcellular localization of CCAT1 was detected utilizing FISH assay. m6A level of CCAT1 was assessed using MeRIP. RNA immunoprecipitation (RIP), Co-immunoprecipitation (Co-IP) and RNA pull down elucidated binding relationship between molecules. Nude mouse tumorigenesis experiments were used to verify the TSCC regulatory function of CCAT1 in vivo. Metastatic pulmonary nodules were observed utilizing hematoxylin and eosin (HE) staining. CCAT1 silencing repressed TSCC cell proliferation, migration and invasion. Expression of CCAT1 was enhanced through N6-methyladenosine (m6A) modification of its RNA, facilitated by WTAP. Moreover, IGF2BP1 up-regulated CCAT1 expression by stabilizing its RNA transcript. CCAT1 bond to PHLPP2, inducing its ubiquitination and activating AKT signaling. CCAT1 mediated the ubiquitination and degradation of PHLPP2 by TRIM46, thereby promoting TSCC growth and metastasis. CCAT1/TRIM46/PHLPP2 axis regulated proliferation and invasion of TSCC cells, implying that CCAT1 would be a novel therapeutic target for TSCC patients.

In-Field Tobacco Leaf Maturity Detection with an Enhanced MobileNetV1: Incorporating a Feature Pyramid Network and Attention Mechanism.

The maturity of tobacco leaves plays a decisive role in tobacco production, affecting the quality of the leaves and production control. Traditional recognition of tobacco leaf maturity primarily relies on manual observation and judgment, which is not only inefficient but also susceptible to subjective interference. Particularly in complex field environments, there is limited research on in situ field maturity recognition of tobacco leaves, making maturity recognition a significant challenge. In response to this problem, this study proposed a MobileNetV1 model combined with a Feature Pyramid Network (FPN) and attention mechanism for in situ field maturity recognition of tobacco leaves. By introducing the FPN structure, the model fully exploits multi-scale features and, in combination with Spatial Attention and SE attention mechanisms, further enhances the expression ability of feature map channel features. The experimental results show that this model, with a size of 13.7 M and FPS of 128.12, performed outstandingly well on the task of field maturity recognition of tobacco leaves, achieving an accuracy of 96.3%, superior to classical models such as VGG16, VGG19, ResNet50, and EfficientNetB0, while maintaining excellent computational efficiency and small memory footprint. Experiments were conducted involving noise perturbations, changes in environmental brightness, and occlusions to validate the model's robustness in dealing with the complex environments that may be encountered in actual applications. Finally, the Score-CAM algorithm was used for result visualization. Heatmaps showed that the vein and color variations of the leaves provide key feature information for maturity recognition. This indirectly validates the importance of leaf texture and color features in maturity recognition and, to some extent, enhances the credibility of the model. The model proposed in this study maintains high performance while having low storage requirements and computational complexity, making it significant for in situ field maturity recognition of tobacco leaves.

Structural Elucidation and Cytotoxic Activity of New Monoterpenoid Indoles from Gelsemium elegans.

Two new monoterpenoid indole alkaloids, gelselegandines F (1) and G (2), were isolated from the aerial parts of Gelsemium elegans. Their structures were elucidated by means of spectroscopic techniques and quantum chemical calculations. The ECD calculations were conducted at the B3LYP/6-311G(d,p) level and NMR calculations were carried out using the Gauge-Including Atomic Orbitals (GIAO) method. Structurally, the two new compounds possessed rare, cage-like, monoterpenoid indole skeletons. All isolated compounds and the total alkaloids extract were tested for cytotoxicity against four different tumor cell lines. The total alkaloids extract of G. elegans exhibited significant antitumor activity with IC50 values ranging from 32.63 to 82.24 ug/mL. In order to discover anticancer leads from the active extraction, both new indole compounds (1-2) were then screened for cytotoxicity. Interestingly, compound 2 showed moderate cytotoxicity against K562 leukemia cells with an IC50 value of 57.02 uM.

Fischer's base-triggered formal (3+2) cycloadditions with 3-isothiocyanato oxindoles as acceptor-donor synthons.

Herein, previously unreported Fischer's base reactants serving as useful 2C building blocks in (3+2) cycloaddition reactions to build a library of bispiro[Fischer's base-oxindole] hybrids are described. These structurally intriguing products containing three adjacent quaternary stereocentres were smoothly afforded in up to 82% yield and >20 : 1 dr under catalyst-free conditions. Notably, the present protocol firstly employs 3-isothiocyanato oxindole serving as an acceptor and then as a donor in the formal (3+2) cycloadditions, allowing practical, straightforward access to structurally diverse cycloadducts. This work expands the applicability scope of 3-isothiocyanato oxindoles, which have been limited to behaving as donor/acceptor-based synthons in cycloadditions in previous work.

Effect of Enhanced Recovery after Surgery (ERAS) Concept and Cluster Nursing on Psychological State and Pain of Oral Outpatients Undergoing Root Canal Therapy.

Objective: The effect of the concept of enhanced recovery after surgery (ERAS) and pain of patients undergoing root canal therapy in oral clinic. Methods: 200 participants in an oral clinic from March 2020 to March 2022 were enrolled in our study. The control group (n = 100) accepted ERAS-based care and the research group (n = 100) accepted ERAS concept and cluster nursing. Nursing satisfaction, comfort, self-efficacy, subjective well-being, self-rating anxiety scale (SAS), and self-rating depression scale (SDS) scores were compared. Results: The research group had 100% satisfaction rate; the control group had 87% satisfaction rate. After nursing, the scores of comforts and self-efficacy of the two groups increased and the scores of comforts and self-efficacy of the research group were higher than those of the control group. After nursing, the scores of subjective well-being of the two groups increased. Furthermore, the higher scores of life satisfaction, interpersonal harmony, and self-efficacy in the research group were found. There was no significant difference in the scores of SAS and SDS between the two groups before nursing (P > 0.05), but after nursing, the scores of SAS and SDS in the two groups decreased, and the scores of SAS and SDS in the research group were lower than those in the control group, and there are statistically significant differences between the groups (P < 0.05). The scores of visual analogue score (VAS) and numerical rating scale (NRS) following intervention decreased, and there are statistically significant differences between the groups (P < 0.05). The less physiological, psychological, social functions, and health self-cognition in the research group were displayed, and there are statistically significant differences between groups (P < 0.05). Conclusion: The adoption of the concept of ERAS and cluster nursing can effectively improve the psychological state and pain score of oral outpatients undergoing root canal therapy, improve comfort and self-efficacy, and enhance subjective well-being and quality of life. ERAS and cluster nursing is of great significance in relieving pain after root canal therapy in the outpatient department, reducing patients' pain and improving patients' quality of life.

Pralsetinib treatment for multiple RET fusions in lung adenocarcinoma: a case report.

Despite recent advances in treatments and knowledge of biomarkers, patients with metastatic lung cancer have a 5-year survival rate of 5%. Rearranged during transfection (RET) fusions occur in 1% to 2% of lung cancer patients. Pralsetinib has been used to treat non-small cell lung cancer with a single RET fusion; however, there have been no reports regarding its use in patients with multiple RET fusions. Genetic mutations in tumor tissues were tested using Amplification Refractory Mutation System-PCR and next-generation sequencing (NGS). Pleural fluids obtained from a male patient with non-small cell lung cancer were also used to detect genetic aberrations by NGS. Pleural fluid-based NGS revealed three RET rearrangements: CCDC6-RET (C2:R12), RET-NRG3 (R11:N3), and CCDC6-RET (C1:R12). All three rearrangements were targeted by pralsetinib, a RET fusion inhibitor. Pralsetinib drastically improved the patient's condition within 4 days, and a partial response was achieved 1 week after pralsetinib was administered. We report for the first time the important clinical observation of a patient with multiple RET fusions who was effectively treated with pralsetinib.

Macrophages induce the expression of lncRNA ATB via the secretion of TGF-ß to relieve ischemia-reperfusion injury in cardiomyocytes.

Cardiac ischemia-reperfusion can cause severe damage to cardiomyocytes. Previous studies have revealed that TGF-ß can alleviate ischemia-reperfusion injury in cardiomyocytes by inducing the expression of long non-coding RNA (lncRNA) activated by TGF-ß (ATB). However, M2 macrophages can secrete a large amount of TGF-ß. However, whether M2 macrophages alleviate the ischemia-reperfusion-induced injury of cardiomyocytes by secreting TGF-ß is unclear. In the present study, macrophages and cardiomyocytes were cultured under oxygen-glucose deprivation/reoxygenation (OGD/R) conditions to simulate ischemia-reperfusion injury. M2-type macrophage markers (IL-10, Arginase-1 and IL-13) were validated using reverse transcription-quantitative PCR and western blotting. Subsequently, the culture medium of M2-type macrophages was collected for the treatment of cardiomyocytes, which were cultured under OGD/R conditions. The levels of inflammatory factors and oxidase enzymes were detected with ELISA. The apoptotic rates of cardiomyocytes were detected by flow cytometry. The expression of cell apoptosis-related proteins and the phosphorylation levels of NF-κB were analyzed by western blotting. The expression levels of specific inflammatory cytokines and the levels of malondialdehyde and lactate dehydrogenase were suppressed in cardiomyocytes following treatment with culture medium derived from M2-type macrophages, which were cultured under OGD/R conditions. Furthermore, OGD/R-induced apoptosis of cardiomyocytes was also relieved following treatment of the cells with macrophage medium. It was found that M2-type macrophages could secrete TGF-ß and that the culture medium of M2-type macrophages could activate the expression of lncRNA ATB in cardiomyocytes. TGF-ß secreted by M2 macrophages relieved the inflammatory response, oxidative stress and apoptosis of cardiomyocytes by inducing the expression of lncRNA ATB.

Identification of compounds with antipyretic effects and anti-endotoxin activity in different species of Lonicera japonica using spectrum-effect correlation.

Liquid chromatography (LC) is a common and straight forward approach used in the evaluation of the quality of Traditional Chinese Medicines (TCMs). Quality control is a critical step when systematically assessing the efficacy of TCMs. In the present study, the spectrum-effect correlation method was used to identify pharmacologically active substances. The aim of the present study was to investigate the underlying correlations between common chemical compounds with antipyretic effects and the anti-endotoxin activity of Lonicera japonica. The common chemical constituents of Lonicera japonica were analyzed using LC, and the antipyretic effects and anti-endotoxin activity were determined using ELISAs. Combining the results of bivariate and principal component analysis methods, eight active constituents were qualitatively and quantitatively analyzed. The results of these analyses indicated that neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid and isochlorogenic acids A, B and C served a synergistic role with respect to antipyretic effects and anti-endotoxin activity. The present study lays a foundation for the future clinical use of Lonicera japonica.

Nanotoxic Effects of Silver Nanoparticles on Normal HEK-293 Cells in Comparison to Cancerous HeLa Cell Line.

PURPOSE: Biomimetic approaches for the synthesis of silver nanoparticles (AgNPs) had created a substantial impression among the research community that focuses on nano-bio interactions. In this study, an eco-friendly method using Rhizophora apiculata aqueous leaf extract as a reductant-rich hydrosol was followed to synthesize AgNPs and test its cytotoxicity. METHODS: To optimise the parameters for the synthesis of AgNPs, central composite design based on response surface methodology was used. The particles synthesized at a nano-scale were characterized in our previously published report. The present report further characterizes the nanoparticles by X-ray diffraction, SEM and TEM at varying sites and magnifications. The characterized AgNPs were tested for their cytotoxic effects on HEK-293 and HeLa cells. RESULTS: The cytotoxicity on the cell lines was dose-dependent. At a concentration of 2.5 µL/mL of the AgNPs-containing hydrosol, 100% inhibition of HEK-293 cells and 75% inhibition of the HeLa cells were observed. The IC50 value for AgNPs on HEK-293 was 0.622 µL/mL (12.135 ng), whereas, for HeLa cells, it was 1.98 µL/mL (38.629 ng). CONCLUSION: The nanoparticles were three-fold toxic towards the HEK-293 cells in comparison to the HeLa cells. Therefore, the therapeutic index is low for R. apiculata derived AgNPs on HeLa cells when tested in comparison with the HEK-293 cells. The nanotoxicity profile of the synthesized AgNPs seems more prominent than the nanotherapeutic index. According to our knowledge, this is the first-ever report on the optimization of synthesis of AgNPs using response surface methodology and identifying the therapeutic index of mangrove leaf-derived AgNPs.

Correlation between the coexpression of zinc finger and SCAN domain-containing protein 31 and transcriptional activator with PDZ-binding motif and prognosis in hepatocellular carcinoma.

BACKGROUND: Transcriptional coactivator with PDZ binding motif (TAZ) regulates multiple biological processes and has been found to be related to hepatocellular carcinoma (HCC). However, common signaling pathways downstream after TAZ knockdown may also be important. METHODS: TAZ was knocked down in an HCC cell line, and its potential target genes were analyzed. A decrease in the expression of zinc finger and SCAN domain-containing protein 31 (ZSCAN31) was observed. The difference in ZSCAN31 expression was evaluated, and its effect on survival in HCC patients who received surgical resection was determined. RESULTS: ZSCAN31 was over-expressed in HCC tissues and was associated with low overall survival (OS) in HCC patients after surgical resection. Analysis of tissue samples from 83 HCC patients who underwent surgical resection in our hospital produced similar results. High ZSCAN31 expression was significantly associated with tumor size. High expression levels of both TAZ and ZSCAN31 were related to poor OS. A positive correlation was identified between ZSCAN31 expression and TAZ expression, and the protein binding of ZSCAN31 and TAZ was confirmed by co-immunoprecipitation (Co-IP) assay using an HCC cell line. CONCLUSIONS: ZSCAN31 is associated with TAZ expression in HCC cells, and the targeting of ZSCAN31 and TAZ may represent a novel therapeutic approach in HCC.

Genus Alangium - A review on its traditional uses, phytochemistry and pharmacological activities.

The species from Alangium have been used as folk medicine to treat rheumatism, skin diseases, diabetes by the people of Southeast Asia. Previous phytochemical studies have shown this genus are rich sources of alkaloids, glycosides, and terpenoids, which have attracted considerable attention of many researchers due to their markedly diverse and complex architecture. The crude extracts as well as the monomeric compounds from the title genus possess anti-tumor, anti-inflammatory, antibacterial, anti-oxidant pharmacological activities. Besides, some isolates from Alangium exhibited the effects on skeletal, smooth muscle and the nervous system. As a large genus of medicinal plants, the medicinal value of Alangium has been widely reported, but there is no review that provide a systematic summary towards its chemical constituents and pharmacological activities, to our knowledge. This work aims to present a comprehensive overview on the traditional uses, phytochemistry, and pharmacological activities of medicinal plants in the genus Alangium, and to explore the evidence supporting its ethnopharmacological effectiveness.

Study on antitumor activities of the chrysin-chromene-spirooxindole on Lewis lung carcinoma C57BL/6 mice in vivo.

The our previous study synthesized the chrysin-chromene-spirooxindole hybrids 3, and further found compound 3e had good antitumor activity against A549 cells in vitro through multi-target co-regulation of the p53 signalling pathway to inhibit the proliferation of A549 cells. This study was designed to evaluate the antitumor effects of compound 3e on Lewis lung carcinoma of C57BL/6 mice in vivo. Compound 3e significantly inhibited the growth of transplanted tumors in C57BL/6 mice and induced the apoptosis of tumor cells. Further studies showed that compound 3e activates and expands the anti-cancer activity of p53 by inhibiting the expression of MDM2, Akt and 5-Lox proteins, accordingly promotes the expressions Bax and inhibit the Bcl-2 protein, the release of Cyt c as well, which resulted in the activation of apoptotic pathway in tumor cells eventually. Moreover, Compound 3e inhibited tumor metastasis by down-regulating VEGF, ICAM-1 and MMP-2 protein expression and angiogenesis. These results suggested that compound 3e exerts an effective antitumor activity in vivo through activating the p53 signaling pathway, which could be exploited as a promising candidate for the development of new anti-tumour drugs.

Regioselective synthesis and evaluation of 2-amino 3-cyano chromene-chrysin hybrids as potential anticancer agents.

The first example of Ca(OH)2-activated p-regioselective synthesis of chrysin-fused chromene was reported through a cascade Michael/cyclization of chrysin and arylidenemalononitrile. The newly synthesized structurally diverse 2-amino 3-cyano chromene-chrysin hybrids 3 were evaluated for their in vitro anticancer activity, and some of the compounds showed stronger anti-proliferative activity against K562, PC-3, A549 and NCI-H1299 than parent compound chrysin, and demonstrated equipotent potency compared with the reference drug of cisplatin. In particular, compound 3h had the highest cytotoxicity towards K562 cells (IC50 = 6.41 µM). Furthermore, compound 3h induced apoptosis of K562 cells in a concentration-dependent manner, as well as induced the apoptosis possibly through promoting the formation of apoptotic DNA of cancer cell via the intrinsic apoptotic pathway. Thus, our results provide in vitro evidence that compound 3h may be a potential candidate for the development of new anti-tumour drugs.

Melatonin suppresses epithelial­to­mesenchymal transition in the MG­63 cell line.

Epithelial­to­mesenchymal transition (EMT) is a major process involved in tumor progression and metastasis. Melatonin is secreted by the pineal gland and has been documented as a potential therapeutic agent for multiple tumors. However, the effects of melatonin on EMT during osteosarcoma (OA) development remain undefined. The present study explored the biological functions and effects of melatonin on EMT induced by transforming growth factor ß1 (TGF­ß1) and its underlying mechanisms in MG­63 cells. Using western­blotting and immunofluorescence, it was found that the switch in E­cadherin/N­cadherin and vimentin expression was induced by TGF­ß1, which was reversed by melatonin through the suppression of Snail and matrix metalloproteinase 9 (MMP­9), through hypoxia­inducible factor 1α (HIF­1α) inhibition. These findings demonstrated that the anticancer effects of melatonin against OA MG­63 cells is through the suppression of EMT via HIF­1α/Snail/MMP­9 signaling.

Thermal-mediated [1,3]-hydrogen transfer as the key step: access to oxindole-chromone hybrid collection with structural diversity.

Inspired by the chemistry and biology of chromone and oxindole derivatives, herein we report the first example of thermal-mediated [1,3]-hydrogen transfer as the key step for the efficient synthesis of oxindole-chromone hybrid collections 2, which avoids additional catalyst and solvent conditions. All the oxindole-chromones 2 are smoothly obtained in >99% yields in all cases, avoiding column chromatography purification. In particular, the products 2 can act as potential synthons for further elaboration in structural diversity, which might be valuable in organic and medicinal chemistry.

The potential value of CDV3 in the prognosis evaluation in Hepatocellular carcinoma.

CDV3 is correlated with tumorigenesis and may affect some biological process in cancer. In this study, we explore the role of CDV3 in HCC. According to the TCGA data base, CDV3 is over-expressed in HCC tissues. Up-regulation of CDV3 is correlated with lower over-all survival rate in HCC patients. In HCC samples from our hospital, CDV3 is also enriched in cancer tissues and CDV3 expression associated with HCC pathological T stage. What is more, higher CDV3 expression could forecast poor survival rate in HCC patients. In conclusion, CDV3 is a biomarker of HCC and could be a potential therapeutic target.

Packed-Nanofiber solid phase extraction coupled with gas chromatography-mass spectrometry for the determination of phthalate esters in urines from children.

In this paper, we developed a rapid and safe method based on packed-fiber solid-phase extraction (PFSPE) system coupled with gas chromatography-mass spectrometry for the determination of four phthalate esters (PAEs), diethyl-o-phthalate (DEP), dibutyl-o-phthalate (DBP), di (2-ethylhexyl) phathalate (DEHP), di-n-octyl phthalate (DNOP), in urine samples. The PAEs in urine samples (500µL) were rapidly cleaned up from urines using polystyrene (PS) nanofibers packed micro-columns fitted on a PFSPE pretreatment device, which can process up to 12 samples simultaneously in 5min. Under optimum conditions, satisfied recovery and relative standard deviation values (RSDs) were in the range of 80.4-111.7% and 1.5-10.9%, respectively. The limits of detection (LOD) and the limits of quantification (LOQ) were ranged from 0.1 to 0.5ngmL-1 and 0.5-2ngmL-1, respectively. The well controlled matrix effect was also evaluated by comparing the signal response of the pure PAEs standards dissolved in methanol with the signal response of PAEs in the urine matrix. This new method was successfully applied to determine four PAEs in urine samples of overweight and normal-weight children, and an association between phthalates in urines and obesity was observed. Thus, the method seems to be a useful tool for monitoring of the level of urinary phthalate esters and also to support an evidence for further reasearch of obesity.

ß-elemene regulates endoplasmic reticulum stress to induce the apoptosis of NSCLC cells through PERK/IRE1α/ATF6 pathway.

Endoplasmic reticulum stress (ERs) has been regarded as an important cause for the pathogenesis of non-small-cell lung cancer (NSCLC). ß-elemene is an active component in the essential oil extracted from a medicinal herb, Curcuma wenyujin, and has been reported to be effective against non-small-cell lung cancer (NSCLC). However, the potential effect and underlying mechanisms of ß-elemene on regulating ERs to inhibit NSCLC are still unclear. In the present study, A549 cells and Lewis tumor-bearing C57BL/6J mice were established to evaluate this effect. Visualsonics Vevo 2100 Small Animal Dedicated High-frequency Color Ultrasound was performed to observe tumor volume in vivo. 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) was used to evaluate cell vitality of A549 cells. Furthermore, western blotting (WB), immunohistochemistry (IHC) and quantitative reverse transcription polymerase chain reaction (q-PCR) were applied to detect the ERs-related proteins. Flow cytometry was also applied to detect cell apoptosis and assay kit for reactive oxygen species (ROS) generation. Our results showed that ß-elemene inhibited lung cancer tumor growth and cell vitality in a dose- and time-dependent manner. Not only that, ß-elemene could up-regulate ERs-related proteins like PERK, IRE1α, ATF6, ATF4, CHOP and down-regulate the Bcl-2 expression. More importantly, ERs inhibitor 4-PBA, IRE1α inhibitor STF-083010, ATF6 inhibitor Anti-ATF6 and PERK inhibitor GSK2656157 can all reduce the amplitude of protein expression changes and apoptosis rates, then weaken the anti-tumor effect of ß-elemene. Therefore, the present in vivo and in vitro study revealed that the anti-NSCLC effect of ß-elemene is closely related to the activation of ERs through PERK/IRE1α/ATF6 pathway, and this might be beneficial for clinical therapy of NSCLC.

Simultaneous quantification of cortisol and cortisone in urines from infants with packed-fiber solid-phase extraction coupled to HPLC-MS/MS.

Cortisol and cortisone are two important glucocorticoids in human body, their interconversion is controlled by two isotypes of 11ß-hydroxy steroid dehydrogenase (11ß-HSD1 and 11ß-HSD2). The ratio of urinary cortisol to cortisone can be used to assess the activity of 11ß-HSDs. An analytical method to quantify urinary cortisol and cortisone using high performance liquid chromatographic tandem mass spectrometry following a packed-fiber solid-phase extraction (PFSPE) was developed. The proposed method was validated and applied to determine the urinary cortisol and cortisone concentrations in infants. Linearity was observed in the range of 0.6-150ng/mL for cortisol and 0.8-200ng/mL for cortisone. The intra-day RSD was 2.4-4.5% for cortisol and 3.3-6.2% for cortisone. Inter-day RSD was 3.7-6.6% for cortisol and 4.3-8.2% for cortisone. The recovery was 97.8±4.6% for cortisol and 98.9±4.4% for cortisone. The established method is simple and efficient for the quantification of urinary cortisol and cortisone and for indirectly assessing the activity of 11ß-hydroxy steroid dehydrogenase.

Rapid, microwave-accelerated synthesis and anti-osteoporosis activities evaluation of Morusin scaffolds and Morusignin L scaffolds.

Described herein is a facile and efficient methodology toward the synthesis of Morusin scaffolds and Morusignin L scaffolds 4-9 and 12via a novel three-step approach (Michael addition or prenylation, cyclization and cyclization) and use a rapid, microwave-accelerated cyclization as the key step. Furthermore, their biological activities have been preliminarily demonstrated by in vitro evaluation for anti-osteoporosis activity. These Morusin, Morusignin L and newly synthesized compounds 5b, 6a, 8e, 8f greatly exhibited the highest potency, especially at the 10-5mol/L (P<0.01), and had good in vitro anti-osteoporosis activities using the commercially available standard drug Ipriflavone as a positive control. The mechanisms associated with anti-osteoporosis effects of these compounds may be through the inhibition of TRAP enzyme activity and bone resorption in osteoclasts, and promotion effect of osteoblast proliferation in vitro. The results indicated that Morusin scaffolds and Morusignin L scaffolds may be useful leads for further anti-osteoporosis activity screenings.