Efficacy study of platelet-rich plasma combined with core decompression and bone grafting in the treatment of early-stage avascular necrosis of the femoral head: a retrospective study.

OBJECTIVE: This study aimed to evaluate the effectiveness of combined core decompression (CD), bone grafting (BG), and platelet-rich plasma (PRP) in treating early-stage avascular necrosis of the femoral head (ANFH). METHODS: A retrospective study was conducted on 74 patients (85 hips) with Ficat-Arlet stage I-II ANFH who were treated at our hospital between May 2015 and May 2018. The control group (20 patients, 22 hips) received symptomatic treatments, including weight-bearing reduction and oral analgesics. The CD + BG group (29 patients, 34 hips) underwent CD and ß-tricalcium phosphate bone grafting. The PRP combination group (25 patients, 29 hips) received PRP injections in addition to CD and BG. Patients were followed up for five years to assess the necessity for total hip arthroplasty (THA). Data analysis was performed on those from the CD + BG and PRP groups who did not require THA. Clinical outcomes were evaluated using the Visual Analog Scale (VAS), Harris Hip Score (HHS), and the proportion of patients not accepting THA. RESULTS: At the five-year follow-up, the rate of THA in the control group was 68.18% (15/22), while in the CD + BG group and the PRP combination group, the rates were 17.65% (6/34) and 10.34% (3/29), respectively. There was no statistically significant difference between the CD + BG group and the PRP combination group (P = 0.441), but both differed significantly from the control group (P < 0.001). Kaplan-Meier survival analysis showed that over time, the proportion of patients in the PRP combination group who did not require THA was consistently higher than that in the CD + BG group. Among patients who did not undergo THA, the proportion of Ficat-Arlet stage I-II patients in the PRP combination group was 88.46% (23/26), which was higher than the 64.29% (18/28) in the CD + BG group, showing a significant difference (P = 0.038). VAS score and HHS were compared between the two groups at 6 months, 12 months, and the last follow-up point, with patients in the PRP combination group showing better scores than those in the CD + BG group (p < 0.05) in both metrics. CONCLUSION: The combination therapy of CD, BG, and PRP demonstrates significant advantages in improving symptoms and delaying disease progression in early-stage ANFH.

Study on the efficacy of 3D printing technology combined with customized plates for the treatment of complex tibial plateau fractures.

BACKGROUND: Anatomical reduction and stable fixation of complex tibial plateau fractures remain challenging in clinical practice. This study examines the efficacy of using 3D printing technology combined with customized plates for treating these fractures. METHODS: We retrospectively analyzed 22 patients treated with 3D printing and customized plates at the Orthopedic Department of the Central Hospital affiliated with Shenyang Medical College from September 2020 to January 2023. These patients were matched with 22 patients treated with traditional plates with similar baseline characteristics. Patients were divided into an experimental group (3D-printed models and customized plates) and a control group (traditional plates). The control group underwent traditional surgical methods, while the experimental group had a preoperative 3D model and customized plates for surgical planning. We compared baseline characteristics and recorded various indicators, including preoperative preparation time, surgical time, intraoperative blood loss, number of intraoperative fluoroscopies, hospital stay duration, fracture healing time, complications, knee joint range of motion (ROM), Rasmussen anatomical and functional scores, and HSS scores. RESULTS: All surgeries were successful with effective follow-up. The experimental group had shorter surgical time, less intraoperative blood loss, and fewer intraoperative fluoroscopies (P < 0.05). At 6 months and 1 year postoperatively, the experimental group had better knee joint HSS scores than the control group. Preoperative preparation time and total hospital stay were shorter in the control group (P < 0.05). There were no significant differences in fracture healing time and follow-up duration between groups. The experimental group showed better knee joint flexion angles (P < 0.05). Rasmussen scores showed no statistical difference between groups (P > 0.05). The incidence of complications was slightly lower in the experimental group but not significantly different. CONCLUSION: 3D printing technology combined with customized plates for complex tibial plateau fractures enables precise articular surface reduction, significantly shortens surgical time, and reduces intraoperative blood loss. This method improves knee joint function, offering a more effective treatment option.

Disappearance of femoral head shortly after femoral neck fracture: a case report and literature review.

This case report describes a woman in her 70s who presented with a 3-month history of hip pain and inability to walk. Upon admission, she was diagnosed with the extremely rare condition of complete femoral head disappearance. A comprehensive examination was conducted to determine the cause and devise an effective treatment strategy, taking the patient's medical history into account. Through interdisciplinary discussions, occult infection and other potential causes were ruled out. The femoral head disappearance was ultimately determined to be due to wear, ischemia, and absorption following a fracture. After informing the patient of the diagnosis and treatment plan, total hip arthroplasty was proposed. This case highlights the rarity and severity of femoral head disappearance in patients with femoral neck fractures, emphasizing the effectiveness of total hip arthroplasty and appropriate joint prostheses in managing such cases. This case has significant implications for clinical diagnosis, treatment, and complication prevention. The report also discusses the causes of acquired femoral head disappearance, relevant diagnostic assessments, and alternative treatment options.

The combined application of pulsed electromagnetic fields and platelet-rich plasma in the treatment of early-stage knee osteoarthritis: A randomized clinical trial.

BACKGROUND: This study aims to evaluate the therapeutic efficacy of combined treatment with pulsed electromagnetic fields (PEMFs) and platelet-rich plasma (PRP) injection in improving pain and functional mobility among patients with early-stage knee osteoarthritis (KOA). We hypothesize that this combined therapy can yield superior treatment outcomes. METHODS: Based on the different treatment regimens, we divided 48 patients diagnosed with Kellgren-Lawrence grades I-III KOA into 3 groups: the PRP group, the PEMFs group, and the PRP + PEMFs group. Each subtype of KOA patients was randomly assigned to different treatment groups. In the PRP group, patients received intra-articular injections of leukocyte-rich platelet-rich plasma once a month for 3 consecutive months. In the PEMFs group, patients receive low-frequency PEMFs irradiation therapy with a frequency of 30 Hz and intensity of 1.5 mT, once daily, 5 times a week, for a consecutive treatment period of 12 weeks. In the PRP + PEMFs group, patients receive both of the aforementioned treatment protocol. The treatment effects on patients are evaluated at baseline and at weeks 4, 8, and 12 post-treatment. Assessment parameters include visual analog scale for pain, Western Ontario and McMaster Universities Osteoarthritis Index, Lequesne Index score, and knee joint range of motion. RESULTS: From the 4th to the 12th week of treatment, the visual analog scale scores, Western Ontario and McMaster Universities Osteoarthritis Index scores, and Lequesne index scores of patients in all 3 groups gradually decreased, while knee joint mobility gradually increased (P < .05). At weeks 4, 8, and 12 after treatment, the PRP combined with PEMFs group showed significantly better scores compared to the PRP group and the PEMFs group, with statistically significant differences (P < .05). A total of 7 patients experienced adverse reactions such as knee joint swelling, low-grade fever, and worsening knee joint pain after treatment, all of which disappeared within 1 week after treatment. The incidence of complications did not differ significantly among the 3 groups (P = .67). CONCLUSION: PRP, PEMFs, and the combination of PRP and PEMFs therapy all effectively alleviate knee joint pain and improve joint function. However, compared to single treatment modalities, the combined therapy of PRP and PEMFs demonstrates more pronounced efficacy.

Meliasanines A-L, tirucallane-type triterpenoids from Melia toosendan with anti-inflammatory properties via NF-κB signaling pathway.

Meliasanines A-L, twelve previously unreported tirucallane-type triterpenoids, together with fifteen known ones, have been isolated from the stem bark of Melia toosendan. Their structures and absolute configurations were determined based on HRESIMS, and NMR, combined with calculated ECD and single-crystal X-ray diffraction analyses. Subsequently, all compounds except 10 were evaluated for their inhibitory effect on the production of nitric oxide induced by lipopolysaccharide in RAW264.7 macrophage cells. The results indicated that seven compounds (1, 13, 14, 16, 20, 22, and 23) exhibited significant NO inhibitory effects, with IC50 values ranging from 1.35 to 5.93 µM, which were more effective than the positive control indomethacin (IC50 = 13.18 µM). Moreover, the corresponding results of Western blot analysis revealed that meliasanine A (1) can significantly suppress the protein expression of inducible nitric oxide synthase and cyclooxygenase 2 in a concentration-dependent manner. The mechanism study suggested that meliasanine A exerts an anti-inflammatory effect via the nuclear factor-κB signaling pathway by suppressing phosphorylation of P65 and IκBα.

Study on the therapeutic effect of Kirschner wire tension band combined with anchor cross-stitch technique in the treatment of comminuted patellar inferopolar fractures.

PURPOSES: Fractures of the inferior patellar pole, unlike other patellar fractures, present challenges for traditional surgical fixation methods. This article introduces the clinical technique and outcomes of using Kirschner wire tension band combined with anchor screw cross-stitch fixation for comminuted inferior patellar pole fractures. METHODS: This retrospective case series study included 14 patients with comminuted inferior patellar pole fractures treated at our institution from September 1, 2020, to April 30, 2022. All patients underwent surgery using the Kirschner wire tension band with anchor screw cross-stitch technique. Follow-up assessments involved postoperative X-rays to evaluate fracture healing, as well as clinical parameters such as healing time, Visual Analog Scale (VAS) scores, range of motion (ROM), and Bostman scores. RESULTS: All patients were followed for an average of over 12 months, with no cases of internal fixation failure. Knee joint stability and function were excellent. X-rays revealed an average healing time of approximately 10.79 ± 1.53 weeks, hospitalization lasted 5.64 ± 1.15 days, surgery took approximately 37.86 ± 5.32 minutes, and intraoperative blood loss was 33.29 ± 8.15 ml. One patient experienced irritation from the internal fixation material. At the final follow-up, the Bostman score averaged 28.29 ± 0.83, knee joint flexion reached 131.07° ± 4.88°, all patients achieved full knee extension, and the VAS score was 0.36 ± 0.63. CONCLUSION: Kirschner wire tension band with anchor screw cross-stitch fixation for comminuted inferior patellar pole fractures delivered satisfactory clinical outcomes. This surgical method, characterized by its simplicity and reliability, is a valuable addition to clinical practice.

Treatment of complex limb fractures with 3D printing technology combined with personalized plates: a retrospective study of case series and literature review.

Background: In recent years, 3D printing technology has made significant strides in the medical field. With the advancement of orthopedics, there is an increasing pursuit of high surgical quality and optimal functional recovery. 3D printing enables the creation of precise physical models of fractures, and customized personalized steel plates can better realign and more comprehensively and securely fix fractures. These technologies improve preoperative diagnosis, simulation, and planning for complex limb fractures, providing patients with better treatment options. Patients and methods: Five typical cases were selected from a pool of numerous patients treated with 3D printing technology combined with personalized custom steel plates at our hospital. These cases were chosen to demonstrate the entire process of printing 3D models and customizing individualized steel plates, including details of the patients' surgeries and treatment procedures. Literature reviews were conducted, with a focus on highlighting the application of 3D printing technology combined with personalized custom steel plates in the treatment of complex limb fractures. Results: 3D printing technology can produce accurate physical models of fractures, and personalized custom plates can achieve better fracture realignment and more comprehensive and robust fixation. These technologies provide patients with better treatment options. Conclusion: The use of 3D printing models and personalized custom steel plates can improve preoperative diagnosis, simulation, and planning for complex limb fractures, realizing personalized medicine. This approach helps reduce surgical time, minimize trauma, enhance treatment outcomes, and improve patient functional recovery.

Synthesis and in†vitro Anti-Inflammatory Activity of Novel Dendrobine Amide/Sulfonamide Derivatives.

A traditional Chinese medicine ingredient, dendrobine, has been demonstrated to have anti-inflammatory properties. However, due to its poor anti-inflammatory properties, its clinical use is limited. Consequently, we have designed and synthesized 32 new amide/sulfonamide dendrobine derivatives and screened their anti-inflammatory activities in vitro. Experiments showed that nitric oxide (NO) generation in lipopolysaccharide (LPS)-induced RAW264.7 cells was strongly reduced by derivative 14, with an IC50 of 2.96 µM. Western blot research revealed that 14 decreased the concentration-dependent expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (INOS). Molecular docking was used to predict the binding of the inflammation-associated proteins COX-2 and INOS to compound 14.

Structurally Diverse Coumarins from Peucedanum praeruptorum and their Anti-Inflammatory Activities via NF-κB Signaling Pathway.

The phytochemical study of Peucedanum praeruptorum led to the isolation of twenty-five coumarins (1-25). Of which, (±) praeruptol A (±1), one pair of previous undescribed seco-coumarin enantiomers were obtained. Their structures were established according to HR-ESI-MS, NMR, X-ray single crystal diffraction analysis, as well as ECD calculation. All compounds were tested for anti-inflammatory activity in the RAW264.7 macrophage model, and eight compounds (7-10, and 13-16) exhibited significant inhibitory effects with IC50 values ranging from 9.48 to 34.66 µM. Among them, compound 7 showed the strongest inhibitory effect, which significantly suppressed the production of IL-6, IL-1ß, and TNF-α, as well as iNOS and COX-2 in a concentration-dependent manner. Further investigated results showed that compound 7 exerted an anti-inflammatory effect via the NF-κB signaling pathway.

New clerodane diterpenoids from Callicarpa pseudorubella and their antitumor proliferative activity.

Six previously undescribed clerodane diterpenes, cardorubellas A-F (1-6), along with seven known ones (7-13), were isolated from the aerial parts of Callicarpa pseudorubella. Their chemical structures were established by analysis of 1D and 2D NMR, HR-ESI-MS, X-ray diffraction, and electronic circular dichroism (ECD) data. Notably, cardorubella B (2) represented the first examples of naturally occurring succinic anhydride-containing clerodane diterpenes derivatives. The anti-proliferative activities of these compounds were assessed. Remarkably, compound 2 exhibited comparable inhibitory activity against HEL cell lines, surpassing the positive control with an IC50 value of 14.01 ± 0.77 µM, compared to 17.02 ± 4.70 µM for 5-fluorouracil.

Limonoids from the Branches and Leaves of Aglaia lawii and Their Cytotoxic Activities.

Three undescribed limonoids (1-3), named aglaians G-I, and one new natural product azedaralide (4), together with nine known analogues (5-13) were isolated from the branches and leaves of Aglaia lawii by RP C18 column, silica gel column, Sephadex LH-20 column chromatography and preparative HPLC. The structures of the new compounds were elucidated by IR, HRESIMS, 1D, 2D NMR, electronic circular dichroism (ECD) calculations and X-ray crystallography diffraction analysis. The results of bioassay showed that the compound 12 exhibited potential inhibitory activity against six human tumor cell lines (MDA-MB-231, MCF-7, Ln-cap, A549, HeLa and HepG-2) with IC50 values as 8.0-18.6 µM.

A novel L-shaped ortho-quinone analog as PLK1 inhibitor blocks prostate cancer cells in G2 phase.

Prostate cancer is the most common malignant tumor among men worldwide. Currently, the main treatments are radical prostatectomy, radiotherapy, chemotherapy, and endocrine therapy. However, most of them are poorly effective and induce side effects. Polo-like kinase 1 (PLK1) regulates cell cycle and mitosis. Its inhibitor BI2536 promotes the therapeutic effect of nilotinib in chronic myeloid leukemia, enhances the sensitivity of neural tube cell tumors to radiation therapy and PLK1 silencing enhances the sensitivity of squamous cell carcinoma to cisplatin. Therefore, the aim of this study was to evaluate the effect of the PLK1 inhibitor L-shaped ortho-quinone analog TE6 on prostate cancer. In vitro on prostate cancer cells showed that TE6 inhibited PLK1 protein expression and consequently cell proliferation by blocking the cell cycle at G2 phase. In vivo on a subcutaneous tumor model in nude mice confirmed that TE6 effectively inhibited tumor growth in nude mice, inhibited PLK1 expression and regulated the expression of cell cycle proteins such as p21, p53, CDK1, Cdc25C, and cyclinB1. Thus, PLK1 was identified as the target protein of TE6, these results reveal the critical role of PLK1 in the growth and survival of prostate cancer and point out the ability of TE6 on targeting PLK1, being a potential drug for prostate cancer therapy.

Design, Synthesis, anti-inflammatory activity Evaluation, preliminary exploration of the Mechanism, molecule Docking, and structure-activity relationship analysis of batatasin III analogs.

Most clinical drugs used to treat inflammation have serious gastrointestinal, renal, and cardiovascular side effects during long-term treatment. The development of new anti-inflammatory agents from natural products and their derivatives is a powerful approach to overcome these adverse effects. Batatasin III, a bibenzyl natural product, has been found to have anti-inflammatory activity. Compared with other anti-inflammatory agents, batatasin III has a simple and unique structure. Therefore, batatasin III and its analogs might have the potential to treat inflammation with only mild adverse effects as a new type of anti-inflammatory agent. Herein, we synthesized 26 batatasin III analogs and evaluated the anti-inflammatory activity in vitro. Analog 21 significantly inhibited (p < 0.01) nitric oxide production with an IC50 value of 12.95 µM. Western blot analysis further revealed that 21 reduced iNOS, phosphorylated p65, and ß-catenin expression in a concentration-dependent manner. These results indicated that 21 could be a potential lead compound for developing a drug candidate for ulcerative colitis. Molecular docking analysis showed that p65 might be a potential target of 21 for the treatment of inflammatory disease. In addition, we analyzed the structure-activity relationship of the analogs, which provides a basis for future structural modifications.

Unusual triterpenoids and steroids from Cipadessa baccifera and their biological activities.

Five undescribed triterpenoids and steroids (1-5), as well as ten known compounds, were purified from the branches and leaves of Cipadessa baccifera. Notably, 1 and 2 are rare cipadesin-type limonoids with an unusual 8,30-epoxide ring and 1,8-ether linkage, respectively. Compound 5 possessed pregnane steroid skeleton with an uncommon 5/6/6/6/5-fused ring system. Their structures were constructed by extensive spectroscopic analysis (NMR, IR, UV, and HRESIMS), and their absolute configurations were confirmed by ECD calculations and quantum chemical calculations. All the isolates were in vitro assayed for their antimicrobial potentials against 6 pathogenic microorganisms and antiproliferation activities against five human cancer cell lines. As a result, compounds 5, 12, 13, and 14 exhibited moderate antibacterial activities (MIC: 25-50 µg/mL). Moreover, 5 showed cytotoxicity against five cancer cell lines with IC50 values ranging from 8.0 to 19.9 µM.

Vascular endothelium is the basic way for stem cells to treat erectile dysfunction: a bibliometric study.

Vascular endothelial is considered to be a key factor in the pathogenesis of erectile dysfunction (ED). The purpose is to reveal the research trend of the field of ED and vascular endothelium. In addition, the goal is to discover the role and mechanism of vascular endothelium in ED. Bibliometrics and visualization methods based on CiteSpace were selected. We conducted the co-authorship analysis of countries, institutions and authors, co-occurrence analysis of keywords, and co-citation analysis of literature and authors through CiteSpace 6.1.R3. 1431 articles from Web of Science Core Collection (WOSCC) were included in the analysis from 1991 to 2022. We found some influential and cutting-edge nodes in each map, including countries, institutions, authors, articles, etc. Stem cell, therapy, oxidative stress, cavernous nerve injury, radical prostatectomy, fibrosis, erectile function, mesenchymal stem cell, and apoptosis may be hot keywords. In conclusion, the efficacy and mechanisms of stem cells and their derivatives in the treatment of diabetes (DM) ED and cavernous nerve injury (CNI) ED are the future research trends. Stem cells therapy for ED is a hot spot in this field, which side notes that stem cells may work mainly through improving endothelial function. Vascular endothelial cells and VEGF may repair nerve and cavernous smooth muscle directly or indirectly, and finally polish up erectile function.

First report of tobacco anthracnose caused by Colletotrichum nymphaeae in China.

Tobacco (Nicotiana tabacum L.) is one of the most widely cultivated economic crops in approximately 120 countries (Peedin 2011). In July 2020 and 2021, typical symptoms of tobacco anthracnose were widely found in the flue-cured tobacco-planted areas of Wufeng, Xuan'en, and Xianfeng, Hubei Province, China. The disease incidence reached up to 60% in some fields at that time, with estimated 10,000 ha of the cultivated area affected. On tobacco leaves, lesions were initially water soaked and yellow green, and these enlarged to produce dark-brown necrosis which became cracked after drying, extending until the leaves withered. After surface-sterilization with 75% ethanol for 45 s and 5% sodium hypochlorite for 60 s, diseased leaf tissues were washed with sterilized water for 60 s three times and then cultured on potato dextrose agar (PDA) plates for seven days at 25°C in the dark. Isolates of Colletotrichum sp. were consistently recovered with isolation rate of 71%, and the five isolates BB005ES1, BB005ES2, BB005ES3, BB005ES4 and BB005ES5 were used to further evaluate characteristics of the pathogen. On PDA medium for seven days, the aerial hyphae of cultures were dense and blanket-like. The aerial surface of the colony was dark gray to white, and the center of the basal surface of the colony was orange-red. Conidia were transparent, aseptate, smooth-walled, straight, cylindrical with one end obtuse and the other end funnel-shaped, and the size was 11.8-12.0 µm×2.7-2.9 µm (n=100). Appressoria were single, smooth, black, oval or irregular shapes with size of 4.6-4.9 µm×8.5-8.7 µm (n=100). The most typical feature of Colletotrichum acutatum species complex is the shape of conidia which have at least one acute end (Damm et al., 2012). Thus, the five strains were identified as part of the Acutatum complex. The sequences of ACT, TUB2, CHS-1, GAPDH and ITS were then amplified from the five strains (Damm et al., 2012), and all the five strains had the similar sequence for each gene (Accession numbers in GeneBank: ON637946, ON637947, ON637945, ON637948 and ON394623). The combined sequences ACT-TUB2-CHS-1-GAPDH-ITS of the five strains were used for constructing multigene phylogenetic tree using Maximum Parsimony method (Prihastuti et al. 2009), and C. gloeosporioides (IMI356878) was selected as an outgroup. The five strains were found to be closely related to the type strains of C. nymphaeae. Hence, the five isolated strains were identified as C. nymphaeae. Pathogenicity of the five strains was determined by placing seven-day-old fungal plugs on attached leaves of 20-day-old tobacco plants in lab. After inoculation, plants were incubated in a 28°C and 95% RH incubator in the dark for five days. The five strains caused the typical dark brown lesions on all inoculated tobacco leaves, whereas no disease symptoms were found on the healthy tobacco leaves for agar-plug inoculation controls. Koch's postulates were fulfilled by re-isolating C. nymphaeae from diseased leaves. Previously, only C. fructicola, C. nicotiance, C. orbiculare and C. cliviicola were documented as causal agents of tobacco anthracnose (Wang et al. 2016；Wang et al. 2022). To our knowledge, this is the first report of C. nymphaeae causing tobacco anthracnose worldwide.

Bioactivities of Steroids and Sesquiterpenes from the Branches and Leaves of Aglaia lawii.

Five undescribed steroids and one sesquiterpene, named Aglaians A-F, along with sixteen known analogs, have been isolated from the branches and leaves of Aglaia lawii. Its structure was elucidated by IR, HRESIMS, 1D and 2D NMR, quantum-chemical calculations, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. The cytotoxic and antibacterial activities of six human tumor cell lines were evaluated (MDA-MB-231, MCF-7, Ln-cap, A549, HeLa, and HepG-2), and four strains of bacteria (Bacterium subtilis, Phytophthora cinnamomic, Acrogenic bacterium, and Ralstonia solanacearum). The bioassay results indicated that compounds 3 and 5 exhibited moderate antitumor activity with IC50 values ranging from 16.72 to 36.14 µM. Furthermore, compounds 3-5 possess antibacterial activities against four bacteria with MIC values of 25-100 µM.

Diverse Flavonoids from the Roots of Indigofera stachyodes.

Three new flavonoids, 4'-O-ß-D-glucopyranosyl-2S,3R-3,7-dihydroxy-3'-methoxyflavan (1), (3R)-7,4'-dihydroxy-5,3'-methoxychalcone (2), (3S)-7,2',3'-trihydroxy-6,4'-dimethoxylisoflavan (3), and one new natural occurring product, (3S)-6,2',3'-trihydroxy-7,4'-dimethoxylisoflavan (4), together with eleven known ones (5-15), were isolated from the roots of Indigofera stachyodes. The structures of these compounds were confirmed by UV, IR, MS, and NMR spectroscopic analysis. The absolute configurations of new compounds were elucidated by ECD spectra and chemical method. All the isolated flavonoids were screened for their antioxidant abilities to scavenge DPPH and ABTS+ . As results, compounds 2-4, 10, and 15 exhibited remarkable scavenging activity against both ABTS+ and DPPH, with the IC50 values less than 20 µM. In addition, compounds 1, 6-9, and 13 exhibited potential antioxidant scavenging activities, IC50 values were in the range of 17.96∼85.91 µM.

Bioactive Bibenzyl Enantiomers From the Tubers of Bletilla striata.

Six new bibenzyls (three pairs of enantiomers), bletstrins D-F (1-3), were isolated from the ethyl acetate-soluble (EtOAc) extract of tubers of Bletilla striata (Thunb.) Rchb f. Their structures, including absolute configurations, were determined by 1D/2D NMR spectroscopy, optical rotation value, and experimental electronic circular dichroism (ECD) data analyses, respectively. Compounds 1-3 possess a hydroxyl-substituted chiral center on the aliphatic bibenzyl bridge, which represented the first examples of natural bibenzyl enantiomers from the genus of Bletilla. The antibacterial, antitumor necrosis factor (anti-TNF-α), and neuroprotective effects of the isolates have been evaluated. Compounds 3a and 3b were effective against three Gram-positive bacteria with minimum inhibitory concentrations (MICs) of 52-105 µg/ml. Compounds 2a and 2b exhibited significant inhibitory effects on TNF-α-mediated cytotoxicity in L929 cells with IC50 values of 25.7 ± 2.3 µM and 21.7 ± 1.7 µM, respectively. Subsequently, the possible anti-TNF-α mechanism of 2 was investigated by molecular docking simulation. Furthermore, the neuroprotective activities were tested on the H2O2-induced PC12 cell injury model, and compounds 2b, 3a, and 3b (10 µM) could obviously protect the cells with the cell viabilities of 57.86 ± 2.08%, 64.82 ± 2.84%, and 64.11 ± 2.52%, respectively.

Cipacinerasins A-K, structurally diverse limonoids from Cipadessa baccifera.

Eleven undescribed limonoids, cipacinerasins A-K, involving of four diverse carbon skeletal types, along with fifteen known analogues, were isolated from the branches and leaves of Cipadessa baccifera. Within them, cipacinerasins A and B feature a rearranged tetrahydropyranyl ring B formed between C-8 and C-30, are unusual miscellaneous-type limonoids. Cipacinerasins E and F are rare trijugin-type limonoids, of which the D-ring δ-lactone is cleaved. Their structures were elucidated on the basis of extensive spectroscopic data (HRESIMS, NMR, UV and IR), electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. All compounds were evaluated in vitro cytotoxicity against five human tumor cell lines (K562, HeLa, PC3, LN-Cap and Hell), and cipacinerasin E showed moderate antitumor activity with IC50 values ranging from 8.0 to 24.8 µM.