Significant Anticancer Effects Research Articles

Review of the Bioactivities and Mechanisms of Fungus Extracts and Compounds in Colon Cancer.

Colon cancer, a malignant tumor caused by a malignant lesion of the colonic mucosal epithelium, has seen a high incidence in recent years. Fungi contain polysaccharides, terpenes, flavonoids, and other chemical components, and the diversity of these components determines the strength of a fungus's biological activity. Studies have shown that the chemical components in fungi can be used as drugs to inhibit the growth of colon cancer. All available information about the bioactivities and mechanisms of fungus extracts and compounds in colon cancer in this review was supplied by library databases and electronic search (PubMed, ScienceDirect, CNKI, Web of Science, Google Scholar, etc.). Fungi exert significant anticancer effects on cell proliferation, cell cycle arrest, apoptosis, tumor growth, and protein expression. At present, most research focus is on cells and animal models. The inhibitory effects of the chemical components in fungi have been the subject of in vivo and in vitro studies, which are reviewed here. All reviewed studies reported significant improvements in humans and animals after intervention with fungal components. Here we provide a complete overview of this subject and summarize recent research findings.

Anti-colorectal cancer actions of Glycyrrhiza uralensis Fisch. and its underlying mechanism via HPLC integration and network pharmacological approaches.

The therapeutic and prognostic outcomes for colorectal cancer (CRC) remain unsatisfactory. Among multiple reported bioactive functionalities of Glycyrrhiza uralensis Fisch. one vital recently reported activity is its therapeutic role against numerous cancers but limited information is available related to its underlying key mechanisms and therapeutically active ingredients, especially against CRC treatment. The aim of current study aims is to reconnoiter G. uralensis pharmacological basis and primary molecular mode of action in treating CRC. For examining the G. uralensis active ingredients and underlying mechanism investigation against CRC including, potential anti-CRC phytochemicals, targets, and related signaling pathways, HPLC and Network-pharmacology analysis techniques was employed, respectively. Whereas, for binding capabilities of active components to their targets, molecular-docking, molecular dynamic simulation technique employed and cell proliferation assays screened the best anti-CRC components, followed by biological function experiments on SW480 cells for verification. Finally, the SW480-xenograft model and subsequent related experiments further confirmed the effect of Liquiritin on CRC. Seven compounds were identified from G. uralensis through HPLC. Network pharmacology and molecular docking results indicated that G. uralensis components exhibited significant anti-cancer effects. These effects were mediated through cancer and MAPK-related signaling pathways, targeting TP53, SRC, STAT3, and PIK3CA proteins. In-vitro experiments showed that liquiritin had better anti-CRC effects compared to other components as it significantly repressed the SW480 propagation, development of colony, relocation, and invasion. Additionally, liquiritin has been shown to significantly reduce tumor size in tumor-bearing mice by targeting p53 and inhibiting the p38 MAPK pathway. In G. uralensis, main API is liquiritin that target CRC tumorigeneses via inhibition of p53 and p38 MAPK, thus can be used for CRC therapy. The findings provide a solid pharmacological basis and potential therapeutic targets for G. uralensis in the treatment of CRC.

Anticancer effect of the antipsychotic agent penfluridol on epithelial ovarian cancer.

Chemoresistant-epithelial ovarian cancer (EOC) has a poor prognosis, prompting the search for new therapeutic drugs. The diphenylbutylpiperidine (DPBP) class of antipsychotic drugs used in schizophrenia has shown anticancer effects. This study aimed to investigate the preclinical efficacy of penfluridol, fluspirilene, and pimozide (DPBP) using in vitro and in vivo models of EOC. Human EOC cell lines A2780, HeyA8, SKOV3ip1, A2780-CP20, HeyA8-MDR, and SKOV3-TR were treated with penfluridol, fluspirilene, and pimozide, and cell proliferation, apoptosis, and migration were assessed. The preclinical efficacy of DPBP was also investigated using in vivo mouse models, including cell lines and patient-derived xenografts (PDX) of EOC. DPBP drugs significantly decreased cell proliferation in chemosensitive (A2780, HeyA8, and SKOV3ip1) and chemoresistant (A2780-CP20, HeyA8-MDR, and SKOV3-TR) cell lines. Among these drugs, penfluridol exerted a relatively stronger cytotoxic effect on all cell lines. Penfluridol significantly increased apoptosis and inhibited migration of EOC cells. In the cell line xenograft mouse model with HeyA8, the penfluridol group showed significantly decreased tumor weight compared with the control group. In the paclitaxel-resistant model with HeyA8-MDR, the penfluridol group had significantly decreased tumor weight compared with the paclitaxel or control groups. Penfluridol exerted anticancer effects on the PDX model. Penfluridol exerted significant anticancer effects on EOC cells and xenograft models, including PDX. Thus, penfluridol therapy, as a drug repurposing strategy, might be a potential therapeutic for EOCs.

Exploring anticancer properties of new triazole-linked benzenesulfonamide derivatives against colorectal carcinoma: Synthesis, cytotoxicity, and in silico insights.

This study reports the design, synthesis, and characterization of a novel series of benzene sulfonamide-triazole hybrid derivatives, to evaluate their anticancer potential against colorectal cancer. The synthesized compounds were characterized using NMR and HRMS spectroscopic techniques. In vitro cytotoxicity assessments revealed that compounds 5g and 5j exhibited significant anticancer effects. 5g showed the highest potency in the DLD-1 cell line (IC50=11.84µM), while 5j demonstrated robust activity in the HT-29 cell line (IC50=9.35µM). Apoptotic analysis indicated that compound 5g effectively induced early and total apoptosis, surpassing the chemotherapeutic agent 5-fluorouracil (5-FU), highlighting its therapeutic potential. Molecular docking studies showed strong binding interactions with key proteins involved in colorectal cancer progression, such as TGFβ2 and VEGFR1. 5j displayed a high binding affinity for TGFβ2 (MM-GBSA ΔG = -92.52kcal/mol) and 5g showed promising interactions with VEGFR1 (ΔG = -70.63kcal/mol). Molecular dynamics simulations confirmed the stability of the ligand-protein complexes, indicating potential as targeted therapeutic agents. Compounds 5g and 5j demonstrate significant promise for further development in colorectal cancer treatment.

Electrochemical Determination of Gallic Acid in Tea Samples Using Pyramidal Pt Nanoparticles

AbstractGallic acid (GA) is a natural phenolic compound with significant biological properties, including anti‐inflammatory, antioxidant, and anticancer effects. Detecting GA in biological matrices like food and beverages is essential but challenging due to the multitude of GA‐like molecules with similar proprieties and functional moieties. In this study, ultra‐small (≈4 nm) pyramidal platinum nanoparticles (PtNPs) with a high fraction of {111} surface domains are used to design a new electrochemical sensor for GA detection in tea, which is the most popular manufactured drink consumed in the world. PtNPs are deposited on a glassy carbon electrode (GCE) using a simple drop deposition method, requiring a minimal amount of nanoparticles and, hence, metal precursor. With just 2.7 µg of PtNPs, the sensor demonstrated a linear response in the concentration range from 50 to 600 µm, a detection limit of 16 µm, and a quantification limit of 49 µm. The sensor selectivity is tested against other antioxidant compounds commonly present in tea, consistently showing a higher response for GA. Furthermore, the sensor capability to detect GA in real green and black tea samples is further validated by high‐performance liquid chromatography (HPLC) analysis, with high correlation between chromatographic data and sensor response.

PNPO-Mediated Oxidation of DVL3 Promotes Multiple Myeloma Malignancy and Osteoclastogenesis by Activating the Wnt/β-Catenin Pathway.

Multiple myeloma (MM) is a cancer of plasma cells caused by abnormal gene expression and interactions within the bone marrow (BM) niche. The BM environment significantly influences the progression of MM. Celastrol, a natural compound derived from traditional Chinese medicine, exhibits significant anticancer effects. This study aimed to identify specific targets of celastrol and develop more effective and less toxic treatment options for MM. Celastrol is used as a probe to determine its specific target, pyridoxine-5'-phosphate oxidase (PNPO). Increased levels of PNPO are associated with poor outcomes in MM patients, and PNPO promotes MM cell proliferation and induces osteoclast differentiation through exosomes. Mechanistically, PNPO oxidizes disheveled 3M282 (DVL3), leading to abnormal activation of the Wnt/β-catenin pathway. Based on the critical sites of PNPOR95/K117, Eltrombopag is identified as a potential therapeutic candidate for MM. In addition, the experiments showed its efficacy in mouse models. Eltrombopag inhibited the growth of MM cells and reduced bone lesions by disrupting the interaction between PNPO and DVL3, as supported by preliminary clinical trials. The study highlights the importance of PNPO as a high-risk gene in the development of MM and suggests that Eltrombopag may be a promising treatment option.

In Vitro Evaluation, Chemical Profiling, and In Silico ADMET Prediction of the Pharmacological Activities of Artemisia absinthium Root Extract.

Artemisia absinthium L., is a plant with established pharmacological properties, but the A. absinthium root extract (AARE) remains unexplored. The aim of this study was to examine the chemical composition of AARE and assess its biological activity, which included antidiabetic, antibacterial, anticancer, and antioxidant properties. GC-MS was used to analyze the chemical components. The antioxidant activity of the total phenolic and flavonoid content was evaluated. Antibacterial activity and cytotoxic effects were identified. Enzyme inhibition experiments were performed to determine its antidiabetic potential. Molecular docking was utilized to evaluate the potential antioxidant, antibacterial, and anticancer activities of the compounds from AARE using Maestro 11.5 from the Schrödinger suite. AARE exhibited moderate antioxidant activity in DPPH (IC50: 172.41 ± 3.15 μg/mL) and ABTS (IC50: 378.94 ± 2.18 μg/mL) assays. Cytotoxicity tests on MCF-7 and HepG2 cancer cells demonstrated significant anticancer effects, with IC50 values of 150.12 ± 0.74 μg/mL and 137.11 ± 1.33 μg/mL, respectively. Apoptotic studies indicated an upregulation of pro-apoptotic genes (caspase-3, 8, 9, Bax) and a downregulation of anti-apoptotic markers (Bcl-2 and Bcl-Xl). AARE also inhibited α-amylase and α-glucosidase, suggesting potential antidiabetic effects, with IC50 values of 224.12 ± 1.17 μg/mL and 243.35 ± 1.51 μg/mL. Antibacterial assays revealed strong activity against Gram-positive bacteria. Molecular docking and pharmacokinetic analysis identified promising inhibitory effects of key AARE compounds on NADPH oxidase, E. coli Gyrase B, and Topoisomerase IIα, with favorable drug-like properties. These findings suggest AARE's potential in treating cancer, diabetes, and bacterial infections, warranting further in vivo and clinical studies.

Combination of Vitex pseudo-negundo methanolic-extract with cisplatin can induce antioxidant activity and apoptosis in HeLa and Caski cells.

Cisplatin-based chemotherapy as a common therapeutic regimen for cervical cancer patients, is becoming more and more ineffective due to high resistance. This urges the need for introducing novel metabolics such as botanical drugs with the capacity to increase the cisplatin effectiveness. In that regard, here we investigated the anticancer effects of the Cisplatin-Vitex pseudo-Negundo combination in cervical cancer cell lines. V. pseudo-Negundo fruits were dried and extracted methanolic fraction. The MTT assay was performed to evaluate cytotoxicity of both drugs in CaSki and HeLa cells. Then, apoptosis, ROS production, and cell cycling were assessed by flow cytometry assay in cells treated with V. pseudo-Negundo and Cisplatin and their combination. Also, the rate of cell migration and colony formation were measured, using wound healing and colony formation assay, respectively. Also, the expression level of related genes (CD133, BAX, BCL2, Casp-3/8/9, MMP-3) was evaluated using the RT-PCR method. The obtained results established that the V. pseudo-Negundo plant has medicinal properties to induce apoptotic and antioxidant signals. The combination treatment of methanol extraction and Cisplatin had a cytotoxic effect on cervical cancer cell lines (HeLa and CaSki) compared to monotherapy. Also, combination therapy resulted in an increased apoptosis rate and diminished ROS production in both CaSki and HeLa cell lines. Furthermore, V. pseudo-Negundo and Cisplatin combination therapy leads to cell cycle arrest in the G2-M and G0-G1 phase in HeLa and CaSki cell lines, respectively. Moreover, combination therapy decreased the colony formation and cell motility in both cell lines and upregulated caspases gene expression. The combination of V. pseudo-Negundo with Cisplatin therapy results in a significant anti-cancer and antioxidant effect compared to cisplatin, representing a promising candidate for future clinical investigations.

Ascorbate/methionine-based CH4 delivery nanomedicine for tumor-targeted therapy.

Methane (CH4) is identified to be an emerging anti-inflammation and anti-cancer molecule with high bio-safety, but the targeted delivery of CH4 is a thorny challenge. Herein, we propose a CH4 delivery strategy based on an intratumoral H2O2-triggered cascade reaction of ascorbic acid (AA)/methionine (Met), and have constructed a new nanomedicine (AMN) for tumor-targeted CH4 therapy. Encouragingly, AMN realizes the effective tumor-targeted delivery and intratumoral H2O2-responsive release of CH4, and exhibits significant anti-cancer effects and high bio-safety. Mechanistically, we have discovered that intratumoral released CH4 can not only induce the apoptosis of 4T1 tumor cells by inhibiting their mitochondrial metabolism, but also activate tumor immunotherapy by reprogramming tumor-associated macrophages (TAMs) phenotype (M2 to M1). The combination of the above anti-cancer pathways by virtue of tumor-targeted CH4 delivery makes contribution to outstanding anti-cancer efficacy of AMN. The proposed CH4 delivery strategy opens a new window for safe and effective tumor therapy.

Therapeutic role of naringin in cancer: molecular pathways, synergy with other agents, and nanocarrier innovations.

Naringin, a flavanone glycoside found abundantly in citrus fruits, is well-known for its various pharmacological properties, particularly its significant anticancer effects. Research, both in vitro and in vivo, has shown that naringin is effective against several types of cancer, including liver, breast, thyroid, prostate, colon, bladder, cervical, lung, ovarian, brain, melanoma, and leukemia. Its anticancer properties are mediated through multiple mechanisms, such as apoptosis induction, inhibition of cell proliferation, cell cycle arrest, and suppression of angiogenesis, metastasis, and invasion, all while exhibiting minimal toxicity and adverse effects. Naringin's molecular mechanisms involve the modulation of essential signaling pathways, including PI3K/Akt/mTOR, FAK/MMPs, FAK/bads, FAKp-Try397, IKKs/IB/NF-κB, JNK, ERK, β-catenin, p21CIPI/WAFI, and p38-MAPK. Additionally, it targets several signaling proteins, such as Bax, TNF-α, Zeb1, Bcl-2, caspases, VEGF, COX-2, VCAM-1, and interleukins, contributing to its wide-ranging antitumor effects. The remarkable therapeutic potential of naringin, along with its favorable safety profile, highlights its promise as a candidate for cancer treatment. This comprehensive review examines the molecular mechanisms behind naringin's chemopreventive and anticancer effects, including its pharmacokinetics and bioavailability. Furthermore, it discusses advancements in nanocarrier technologies designed to enhance these characteristics and explores the synergistic benefits of combining naringin with other anticancer agents, focusing on improved therapeutic efficacy and drug bioavailability.

Enzymatically catalyzed molecular aggregation.

The dynamic modulation of the aggregation process of small molecules represents an important research objective for scientists. However, the complex and dynamic nature of internal environments in vivo impedes controllable aggregation processes of single molecules. In this study, we successfully achieve tumor-targeted aggregation of an aggregation-induced emission photosensitizer (AIE-PS), TBmA, with the catalysis of a tumor-overexpressed enzyme, γ-Glutamyl Transferase (GGT). Mechanistic investigations reveal that TBmA-Glu can be activated by GGT through cleavage of the γ-glutamyl bond and releasing TBmA. The poor water solubility of TBmA induces its aggregation, leading to aggregation-enhanced emission and photodynamic activities. The TBmA-Glu not only induces glutathione (GSH) depletion through GGT photo-degradation but also triggers lipid peroxidation accumulation and ferroptosis in cancer cells through photodynamic therapy. Finally, the in vivo studies conducted on female mice using both tumor xenograft and orthotopic liver cancer models have also demonstrated the significant anti-cancer effects of TBmA-Glu. The exceptional cancer-targeting ability and therapeutic efficiency demonstrated by this GGT activatable AIE-PS highlights enzymatic-mediated modulation as an effective approach for regulating small molecule aggregation intracellularly, thereby advancing innovative therapeutic strategies for various diseases.

Plasma‐Activated Hydrogel Synergies With Paclitaxel to Enhance the Anticancer Efficacy

ABSTRACTCold atmospheric plasma‐activated hydrogel (PAH) exhibits excellent loading and slow‐release capacity for plasma‐generated reactive species. In this study, plasma‐activated pluronic F127 hydrogel (PAH‐PF127) was obtained using surface dielectric barrier discharge (SDBD), and the anticancer effects of PAH‐F127 synergies with the clinical drug paclitaxel (PTX) were investigated. The results indicated that PAH‐PF127 could load plasma‐generated long‐lived reactive species efficiently, and in vitro research revealed that PAH‐PF127 exerts significant anticancer effects by inducing intracellular oxidative stress, and synergies with 50 μg/mL (low‐dose) PTX could easily replace 200 μg/mL (high‐dose) PTX alone. These results suggested that PAH‐PF127 has the potential to address the toxic side effects of high‐dose drugs and expand the application of plasma technology in anticancer treatment.

A Review of Anticancer Potential of Conferone, Diversin and Ferutinin; Which One is Stronger for Cancer Therapy?

One of the growing diseases in today's human societies is cancer, which has become a major challenge, especially in industrialized and developing countries. Cancer treatments are diverse, but they usually use surgery, chemotherapy, and radiotherapy to improve patients. Existing drugs are usually expensive and, in some cases, are not effective due to drug resistance and side effects. Finding compounds of natural origin can be somewhat effective and useful in helping doctors to treat this disease. Ferula plants, which are traditionally used as spices or for medicinal purposes, can be a good source for finding anti-cancer compounds due to their various compounds, such as monoterpenes, sulfide compounds, and polyphenols. Several studies have shown that compounds found in Ferula plants have significant anticancer effects on various types of cancer cells. This article was compiled with the aim of collecting evidence and articles related to the anti-cancer effects of three compounds obtained from these plants, namely Conferone, Diversin, and Ferutinin. This review article was prepared by searching the terms Conferone, Diversin, Ferutinin and cancer and related information was collected through searching electronic databases such as ISI Web of Knowledge, PubMed and Google Scholar until the March of 2024. The results of this review showed that relatively comprehensive studies have been conducted in this field and these studies have shown that these compounds can be used in the design of future anticancer drugs. Among the examined compounds, conferone showed that it has the best effect on cancer cells.

A Marine-Derived Small Molecule Inhibits Prostate Cancer Growth by Promoting Endoplasmic Reticulum Stress Induced Apoptosis and Autophagy.

MHO7 (6-epi-ophiobolin G), a novel component extracted from a mangrove fungus, exhibits significant anticancer effects against breast cancer. However, the precise mechanism underlying the anticancer effects of MHO7 in prostate cancer (PCa) is yet to be fully elucidated. Therefore, this study was undertaken to assess the effect of MHO7 on PCa cells and elucidate its underlying mechanism. A series of in vitro experiments were conducted, including Cell Counting Kit-8, and plate clone formation assays, flow cytometry analysis, electron microscopy, immunofluorescence staining, western blotting, and molecular dynamics simulation. Additionally, in vivo tumor xenograft models were employed. Our findings revealed that MHO7 could induce cellular autophagy at low concentration (2 μM) and apoptosis at relatively high concentration (4 and 8 μM), leading to significant PCa cell growth inhibition. Furthermore, MHO7 triggered endoplasmic reticulum (ER) stress, which subsequently stimulated autophagy and apoptosis via IRE1α/XBP-1s signaling pathway activation. Notably, IRE1α knockdown markedly reduced MHO7-induced autophagy and apoptosis. Moreover, MHO7 targeted the IRE1α protein, thereby enhancing its stability. MHO7 also exhibited substantial anticancer activity in tumor xenograft models. Our study revealed that MHO7 holds considerable potential as an anticancer agent against PCa, attributable to its activation of ER stress-induced autophagy and apoptosis at different concentrations, facilitated by the upregulation of IRE1α expression.

Isolation and Characterization of Stigmasterol from Psidium guajava Leaves: A Promising Bioactive Compound with Therapeutic Potential

This study aimed to isolate and characterize bioactive compounds from the leaves of Psidium guajava Linn. The hydroethanolic extract yielded 32% (80 g) from the crude material, which was subjected to column chromatography for fractionation. Structural elucidation of the isolated compound was performed using 1D and 2D Nuclear Magnetic Resonance (NMR) spectroscopy, including COSY, HSQC, and HMBC experiments. The spectral data confirmed the presence of stigmasterol, characterized by its distinct chemical shifts and long-range correlations between carbon and proton atoms. Stigmasterol was isolated as a white, crystalline solid and identified by its unique physio-chemical properties, such as solubility in organic solvents, a melting point of 163-164°C, and molecular formula C29H48O. This compound is known for its significant biological activities, including antibacterial, antimalarial, anti-inflammatory, antioxidant, and anticancer effects. By employing advanced techniques like 1D and 2D NMR spectroscopy, the study provides precise structural elucidation of stigmasterol, contributing to natural product research and reinforcing the medicinal potential of guava leaves as a source of pharmacologically active compounds. This adds to the existing knowledge of the plant’s bioactive components and their applications in medicinal chemistry

Machine learning-assisted identification of potential cancer inhibitors: Multifunctional biomineralized CaCO3-polyethyleneimine nanoparticle carriers and their application in lung cancer therapy

Cancer, as a prevalent phenomenon among malignant tumors, has a late-stage diagnosis rate approaching half, significantly limiting treatment efficacy and imposing substantial physiological and psychological burdens on patients. Therefore, developing innovative therapeutic platforms that simultaneously optimize diagnostic accuracy, enhance therapeutic efficacy, and minimize side effects is a critical scientific challenge in the field of precision cancer medicine. In this study, we employed a simple and efficient one-pot synthesis method combined with polyethyleneimine (PEI)-mediated biomineralization technology to successfully prepare calcium carbonate-polyethyleneimine (CaCO3-PEI) composite nanoparticles. These nanoparticles exhibit high pH sensitivity and can rapidly degrade under the mildly acidic conditions that mimic the tumor microenvironment, providing potential for targeted tumor therapy. Subsequently, we encapsulated compound 1, which has potential for lung cancer treatment, within the CaCO3-PEI nanoparticles, successfully constructing the CaCO3-PEI@1 composite system. Structural analysis of this composite system was conducted through characterization techniques. In vitro cell experiments demonstrated that the CaCO3-PEI@1 composite system exhibited significant anticancer effects by effectively inhibiting cancer cell proliferation through the regulation of apoptosis-related protein Bax expression. This provides new insights and experimental evidence for the development of cancer treatment strategies. Based on the experiment and molecular docking identified activity against lung cancer, the compound 1 was used as the initiator for the machine learning model, and up to 10,000 episodes were generated, after thorough examination, it was found about two-thirds of the generated episodes were entirely different from each other, which demonstrated that the machine learning model was a powerful tool for designing of potential inhibitors against lung cancer.

Anticancer Efficacy of Biosynthesized Zinc Oxide and Gold Nanoparticles

Abstract Introduction/Objective Introduction: Advancements in nanoscale materials have led to the exploration of metal oxides for cancer diagnosis and therapy. Zinc oxide nanoparticles (ZnO NPs) and gold nanoparticles (Au NPs) are particularly promising due to their biocompatibility and anticancer properties demonstrated across various cancer cell lines. Objectives This study aimed to isolate fungal endophytes from Eucalyptus sideroxylon leaves and utilize them for the biosynthesis of nanoparticles (ZnO NPs and Au NPs) to assess their anticancer activity. Methods/Case Report Methods: Healthy Eucalyptus sideroxylon samples were collected from a desert research center, and endophytes were isolated and cultivated. The fungal biomass was processed to synthesize ZnO NPs and Au NPs. Cell lines were propagated for cytotoxicity experiments using the MTT assay in a 96-well plate format. Results (if a Case Study enter NA) Results: Biosynthesized ZnO and Au NPs exhibited anticancer activity against HCT-116 and CACO2 cell lines. The IC50 values for ZnO NPs were 5.06 μg/mL for HCT-116 and 6.07 μg/mL for CACO2, while Au NPs showed IC50 values of 5.9 μg/mL for HCT-116 and 1.1 μg/mL for CACO2. ZnO NPs demonstrated dose-dependent toxicity on HCT-116 cells, with increasing concentrations leading to a reduction in cell viability. Similarly, Au NPs exhibited dose-dependent cytotoxicity on both cell lines. Conclusion Conclusion: This study underscores the potential of endophytic fungi for biosynthesizing metal nanoparticles with significant anticancer effects. ZnO NPs displayed superior efficacy against colon cancer cells compared to Au NPs, indicating their potential as therapeutic agents. The findings highlight the importance of exploring natural sources for nanoparticle synthesis and their application in cancer therapy.

Research Progress on the Quality, Extraction Technology, Food Application, and Physiological Function of Rice Bran Oil.

Rice bran oil is recommended by the World Health Organization as one of the three major healthy edible oils (along with corn and sesame oils), owing to its unique fatty acid composition and functional components. This study screened, organized, and analyzed a large number of studies retrieved through keyword searches, and investigated the nutritional value and safety of rice bran oil. It reviews the stability of raw rice bran materials and the extraction and refining process of rice bran oil and discusses food applications and sub-health regulations. Research has found that a delayed stabilization treatment of rice bran seriously affects the overall quality of rice bran oil. Compared with traditional solvent extraction, the new extraction technologies have improved the yield and nutritional value of rice bran oil, but most of them are still in the research stage. Owing to the lack of economical and applicable supporting production equipment, extraction is difficult to industrialize, which is a challenging research area for the future. Rice bran oil has stronger antioxidant stability than other edible oils and is more beneficial to human health; however, its application scope and consumption are limited owing to the product price and lack of understanding. Rice bran oil has significant antioxidant, anti-inflammatory, anti-cancer, hypoglycemic, lipid-lowering, and neuroprotective effects. Further exploratory research on other unknown functions is required to lay a scientific basis for the application and development of rice bran oil.

Computer-Aided Design of VEGFR-2 Inhibitors as Anticancer Agents: A Review.

Due to its intricate molecular and structural characteristics, vascular endothelial growth factor receptor 2 (VEGFR-2) is essential for the development of new blood vessels in various pathological processes and conditions, especially in cancers. VEGFR-2 inhibitors have demonstrated significant anticancer effects by blocking many signaling pathways linked to tumor growth, metastasis, and angiogenesis. Several small compounds, including the well-tolerated sunitinib and sorafenib, have been approved as VEGFR-2 inhibitors. However, the widespread side effects linked to these VEGFR-2 inhibitors-hypertension, epistaxis, proteinuria, and upper respiratory infection-motivate researchers to search for new VEGFR-2 inhibitors with better pharmacokinetic profiles. The key molecular interactions required for the interaction of the small molecules with the protein target to produce the desired pharmacological effects are identified using computer-aided drug design (CADD) methods such as pharmacophore and QSAR modeling, structure-based virtual screening, molecular docking, molecular dynamics (MD) simulation coupled with MM/PB(GB)SA, and other computational strategies. This review discusses the applications of these methods for VEGFR-2 inhibitor design. Future VEGFR-2 inhibitor designs may be influenced by this review, which focuses on the current trends of using multiple screening layers to design better inhibitors.

Molecular Actions of Enicostemma hyssopifolium Whole Plant Extract on HPV18-Infected Human Cervical Cancer (HeLa) Cells.

Enicostemma hyssopifolium (E. hyssopifolium) contains several bioactive compounds with anti-cancer activities. This study was performed to investigate the molecular effects of E. hyssopifolium on HPV18-containing HeLa cells. The methanol extract of E. hyssopifolium whole plant was tested for cytotoxicity by MTT assay. A lower and higher dose (80 and 160 μg/mL) to IC50 were analyzed for colonization inhibition (Clonogenic assay), cell cycle arrest (FACS analysis), and induction of apoptosis (AO/EtBr staining fluorescent microscopy and FACS analysis) and DNA fragmentation (comet assay). The HPV 18 E6 gene expression in treated cells was analyzed using RT-PCR and qPCR. A significant dose-dependent anti-proliferative activity (IC50 - 108.25±2 μg/mL) and inhibition of colony formation cell line were observed using both treatments. Treatment with 80 μg/mL of extract was found to result in a higher percent of cell cycle arrest at G0/G1 and G2M phases with more early apoptosis, while 160 μg/mL resulted in more cell cycle arrest at SUBG0 and S phases with late apoptosis for control. The comet assay also demonstrated a highly significant increase in DNA fragmentation after treatment with 160 μg/mL of extract (tail moments-19.536 ± 17.8), while 80 μg/mL of extract treatment showed non-significant tail moment (8.152 ± 13.0) compared to control (8.038 ± 12.0). The RT-PCR and qPCR results showed a significant reduction in the expression of the HPV18 E6 gene in HeLa cells treated with 160 μg/mL of extract, while 80 μg/mL did not show a significant reduction. The 160 μg/mL methanol extract of E. hyssopifolium demonstrated highly significant anti-cancer molecular effects in HeLa cells.