The advancements and prospective developments in anti-tumor targeted therapy.

Cancer poses a major threat to human health worldwide. The development of anti-tumor materials provides new modalities for cancer diagnosis and treatment. In this review, we comprehensively summarize the research progress and clinical applications of anti-tumor materials. First, we introduce the etiology and pathogenesis of cancer, and the significance and challenges of anti-tumor materials research. Then, we classify anti-tumor materials and discuss their mechanisms of action. After that, we elaborate the research advances and clinical applications of anti-tumor materials, including those targeting tumor cells and therapeutic instruments. Finally, we discuss the future perspectives and challenges in the field of anti-tumor materials. This review aims to provide an overview of the current status of anti-tumor materials research and application, and to offer insights into future directions in this rapidly evolving field, which holds promise for more precise, efficient and customized treatment of cancer.

Correction: Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents.

[This corrects the article DOI: 10.1039/D4MD00053F.].

Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents.

Inflammation is the body's response to defence against infection or injury, and is associated with the progression of many diseases, such as inflammatory bowel disease (IBD) and rheumatoid arthritis (RA). LCA, a dibenzylbutane lignan extracted from the roots of traditional medicinal plant Litsea cubeba (Lour.) Pers., has demonstrated promising anti-inflammatory activity. In this study, a series of novel LCA derivatives were designed, synthesized, and evaluated for anti-inflammatory activity. Lipopolysaccharide (LPS)-induced RAW 264.7 cell model experiments showed that compound 10h (at 20 µM of concentration) had the strongest inhibitory effect on NO release, and inhibited the secretion and gene expression levels of interleukin (IL)-1ß, IL-6, and tumor necrosis factor (TNF)-α in vitro. In addition, western blot, immunofluorescence, and molecular docking showed that the anti-inflammatory mechanism of compound 10h may be related to the nuclear factor (NF)-κB signalling pathway. In vivo studies based on a carrageenan-induced mouse paw edema model have shown significant anti-inflammatory activity of compound 10h at 20 mg kg-1. Preliminary in vitro and in vivo studies indicate that compound 10h has the potential to be developed as a novel anti-inflammatory agent.

Discovery of anti-inflammatory agents from 3, 4-dihydronaphthalene-1(2H)-one derivatives by inhibiting NLRP3 inflammasome activation.

NLRP3 inflammatory vesicles are a polymer of cellular innate immunity composed of a pair of proteins. The continuous activation of NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammatory vesicles induces the occurrence and enhancement of inflammatory response. In this study, a series of 3, 4-dihydronaphthalene-1(2H)-one derivatives (DHNs, 6a-u, 7a-e, 8a-n) were synthesized and characterized by NMR and HRMS. We evaluated the cytotoxicity and anti-inflammatory activity of all compounds in vitro, and selected 7a substituted by 7-Br in A-ring and 2-pyridylaldehyde in C-ring as effective lead compounds. Specifically, 7a can block the assembly and activation of NLRP3 inflammasome by down-regulating the expression of NLPR3 and apoptosis-associated speck-like protein containing a CARD (ASC), and inhibiting the production of reactive oxygen species (ROS) and other inflammatory mediators. In addition, 7a inhibits the phosphorylation of inhibitor kappa B alpha (IκBα) and NF-κB/p65 and the nuclear translocation of p65, thereby inhibiting nuclear factor kappa-B (NF-κB) signaling. Molecular docking analysis confirmed that 7a could reasonably bind the active sites of NLRP3, ASC and p65 proteins. Therefore, 7a is predicted as a potential NLRP3 inflammatory vesicle inhibitor and deserves further research and development.

Polysaccharide-Based Coating with Excellent Antibiofilm and Repeatable Antifouling-Bactericidal Properties for Treating Infected Hernia.

In recent years, the utilization of medical devices has gradually increased and implantation procedures have become common treatments. However, patients are susceptible to the risk of implant infections. This study utilized chemical grafting to immobilize polyethylenimine (QPEI) and hyaluronic acid (HA) on the surface of the mesh to improve biocompatibility while being able to achieve antifouling antimicrobial effects. From the in vitro testing, PP-PDA-Q-HA exhibited a high antibacterial ratio of 93% against S. aureus, 93% against E. coli, and 85% against C. albicans. In addition, after five rounds of antimicrobial testing, the coating continued to exhibit excellent antimicrobial properties; PP-PDA-Q-HA also inhibits the formation of bacterial biofilms. In addition, PP-PDA-Q-HA has good hemocompatibility and cytocompatibility. In vivo studies in animal implantation infection models also demonstrated the excellent antimicrobial properties of PP-PDA-Q-HA. Our study provides a promising strategy for the development of antimicrobial surface medical materials with excellent biocompatibility.

Treatment of rheumatoid arthritis with curcumin analog 3,5-bis(arylidene)-4-piperidone.

Rheumatoid arthritis (RA) is an inflammatory disease. Curcumin can inhibit NF-κB and reduce the expression of inflammation-related genes. Aim: To evaluate the potential development of 6d in the clinical treatment of inflammatory diseases such as RA. Methods: Using a skeleton fusion strategy to synthesize curcumin analogues for 6d. This work evaluates anti-inflammatory activity by conducting anti-arthritis experiments (adjuvant-induced RA models) on rats. Western blot and ELISA were used to detect the expression of inflammatory-related proteins and cytokines. Molecular docking analysis confirmed the binding effect of 6d with active sites. Conclusion: 6d inhibits NF-κB has a protective effect on arthritis caused by RA.

Research Advances in Clinical Applications, Anticancer Mechanism, Total Chemical Synthesis, Semi-Synthesis and Biosynthesis of Paclitaxel.

Paclitaxel, a natural secondary metabolite isolated and purified from the bark of the Taxus tree, is considered one of the most successful natural anticancer drugs due to its low toxicity, high potency and broad-spectrum anticancer activity. Taxus trees are scarce and slow-growing, and with extremely low paclitaxel content, the contradiction between supply and demand in the market is becoming more and more intense. Therefore, researchers have tried to obtain paclitaxel by various methods such as chemical synthesis, artificial culture, microbial fermentation and tissue cell culture to meet the clinical demand for this drug. This paper provides a comprehensive overview of paclitaxel extraction, combination therapy, total synthesis, semi-synthesis and biosynthesis in recent years and provides an outlook, aiming to provide a theoretical basis and reference for further research on the production and application of paclitaxel in the future.

Preparative separation of iridoid glucosides and crocins from Gardeniae Fructus using sequential macroporous resin column chromatography and evaluation of their anti-inflammatory and antioxidant activities.

Iridoid glycosides (geniposide (GP), genipin-1-gentiobioside (GB), etc.) and crocins (crocin Ⅰ (CR1), crocin Ⅱ(CR2), etc.) are two main bioactive components in Gardeniae Fructus (GF), which is a famous traditional Chinese medicine. Iridoid glycosides exhibit many activities and are used to manufacture gardenia blue pigment for the food industry. Crocins are rare natural water-soluble carotenoids that are often used as food colorants. A sequential macroporous resin column chromatography technology composed of HC-500B and HC-900B resins was developed to selectively separate iridoid glucosides and crocins from GF. The adsorption of GP on HC-900B resin was an exothermic process. The adsorption of CR1 on HC-500B resin was an endothermic process. The two kinds of components were completely separated by a sequential resin column. GB and GP were mainly found in product 1 (P1) with purities of 11.38% and 46.83%, respectively, while CR1 and CR2 were mainly found in product 2 (P2) with purities of 12.32% and 1.40%, respectively. The recovery yields of all the compounds were more than 80%. The above results showed that sequential resin column chromatography technology achieved high selectivity and recovery yields. GF extract, P1 and P2 could significantly inhibit the secretion of nitric oxide (NO), tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-induced RAW264.7 cells, indicating that iridoid glycosides and crocins provide a greater contribution to the anti-inflammatory activity of GF. At the same time, compared to the GF extract and P1, P2 exhibited stronger scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, indicating that crocins may provide a significant contribution to the antioxidant activity of GF.

Discovery of anti-neuroinflammatory agents from 1,4,5,6-tetrahydrobenzo[2,3]oxepino[4,5-d]pyrimidin-2-amine derivatives by regulating microglia polarization.

Neuroinflammation mediated by microglia activation leads to various neurodegenerative and neurological disorders. In order to develop more and better options for this disorders, a series of 3,4-dihydrobenzo[b]oxepin-5(2H)-one derivatives (BZPs, 6-19) and novel 1,4,5,6-tetrahydrobenzo[2,3]oxepino[4,5-d]pyrimidin-2-amine derivatives (BPMs, 20-33) were synthesized and screened the anti-neuroinflamamtion effects. 3,5-bis-trifluoromethylphenyl-substituted BPM 29 showed more potent anti-neuroinflammatory activity and no toxicity to BV2 microglia cells in vitro. 29 significantly reduced the number of M1 phenotype of microglia cells, but significantly increased the number of M2 phenotype of microglia cells in lipopolysaccharide (LPS)-induced BV2 microglia cells. 29 significantly reduced the secretion of inflammatory cytokines (IL-18, IL-1ß, TNF-α), but increased the secretion of anti-inflammatory cytokines (IL-10) from LPS-induced BV2 microglia cells. Also, 29 inhibited the NOD-like receptor NLRP3 inflammasome formation, and down-regulated the expression of M2 isoform of pyruvate kinase in LPS-induced BV2 microglia cells. In vivo, 29 reduced the neuroinflammation in cuprizone-induced inflammatory and demyelinating mice by reducing the expression of inducible nitric-oxide synthase, but increased the expression of CD206. Taken together, 29 might be a prospective anti-neuroinflammatory compound for neuroinflammatory and demyelinating disease by alleviating microglia activation.

Embryonic perfect repair inspired electrospun nanofibers dressing with temperature-sensitive and antibacterial properties for wound healing.

Introduction: The development of highly effective wound dressings is crucial for successful clinical applications. Achieving wound closure, preventing infection, and minimizing scarring are key objectives in wound healing. Drawing inspiration from the regenerative mechanisms observed in embryonic tissue repair, we designed a series of wound-contractible dressings with exceptional antibacterial properties. Methods: This was achieved by encapsulating quaternized silicone (QP12) and poly(N-isopropylacrylamide-co-N-hydroxymethylacrylamide-co-octadecyl acrylate) (PNNS) within electrospun nanofibers of poly(ε-caprolactone) (PCL). Results and discussion: The resulting nanofibrous dressings demonstrated remarkable thermo-responsive self-contraction and tissue adhesion capabilities, enabling secure adherence to the skin and active wound closure. Notably, these nanofibers exhibited potent antibacterial activity against both Gram-positive and Gram-negative bacteria. Furthermore, they possessed desirable properties such as hydrophilicity, biocompatibility and mechanical properties resembling human skin. A full-thickness skin defect model evaluation revealed that these temperature-sensitive nanofibers expedited wound closure, enhanced wound healing, and suppressed scar formation. This result was evidenced by reduced infiltration of inflammatory cells, well-organized collagen arrangement, and improved vascularization. In summary, we propose that these wound-contractible nanofibers, with their antibacterial and anti-scarring properties, hold great promise as an advanced solution for skin wound repair.

Phytochemistry, nutritional composition, health benefits and future prospects of Passiflora: A review.

Passiflora, also known as "passion fruit", is widely grown in tropical and subtropical regions. It is not only eaten raw but is also widely used in processed foods. Various extracts, juices and isolated compounds show a wide range of health effects and biological activities, such as antioxidant, anti-inflammatory, sedative, and neuroprotective effects. In this review, we not only review the phytochemical properties of Passiflora but also highlight the potential of Passiflora for food applications and the use of all parts as a source of ingredients for medicines and cosmetics that promote health and well-being. This will provide theoretical support for the integrated use of such natural products.

Multifunctional xyloglucan-containing electrospun nanofibrous dressings for accelerating infected wound healing.

Preventing wound infection is a major challenge in biomedicine. Conventional wound dressings often have poor moisturizing and antimicrobial properties unfavorable for wound healing. In this study, we prepared a multifunctional electrospun nanofiber dressing (PCQX-M) containing xyloglucan, quaternized chitosan, Polyvinyl alcohol, and collagen. By applying the concept of wet healing, xyloglucan and quaternized chitosan polysaccharides with excellent water solubility were employed to improve the absorption and moisturizing properties and maintain a moist microenvironment for the wound healing process. PCQX-M demonstrated high mechanical, thermodynamic, and biocompatible properties, providing suitable healing conditions for wounds. In addition, PCQX-M showed exceptional antibacterial properties and a potential inhibitory effect on the growth of microorganisms in infected wounds. More intriguingly, the restorative healing effect was investigated on a mouse model of whole skin injury infected with Staphylococcus aureus. Wound healing, collagen deposition, and immunofluorescence results showed that PCQX-M significantly promoted cell proliferation and angiogenesis at the injury site and facilitated the healing of the infected wound. Our study suggests that PCQX-M has excellent potential for clinical application in infected wound healing.

Synthesis and in vitro Anti-proliferative Activities on LNCaP, LS180 and MKN45 of Novel 20(R)-Panaxadiol Derivatives.

BACKGROUND: 20(R)-PD, a tetracyclic triterpenoid, is a non-natural saponin present in the form of protopanaxadiol. Because of its essential biological activities, especially anti-tumor activity, structural modification of 20(R)-PD and the development of innovative and novel 20(R)-PD derivatives with better anti-tumor activity are increasingly relevant. AIMS: 20(R)-Panaxadiol (20(R)-PD) can inhibit tumor proliferation. Three series of novel 20(R-PD derivatives were synthesized by modifying the A-ring. OBJECTIVE: The objective of this work was to synthesize and evaluate the in vitro anti-proliferative activities of 20(R)- PD derivatives in LNCaP, LS180, and MKN45 cancer cells. Structural modifications were performed at the C-3 position and A-ring. METHODS: The in vitro anti-proliferative activities of novel derivatives in LNCaP, LS180, and MKN45 cells were evaluated by the MTT assay. The effects of compounds 5 and C9 on apoptosis were determined by flow cytometry. RESULTS: Compounds 5, B2, C2, C4, C7, C8, C9, C10, and C11 exhibited good anti-proliferative activities in LNCaP, LS180, and MKN45 cells in vitro. The best anti-proliferative activity was observed for the C-series derivatives with the introduction of amino acids at the C-3 position. C9 exhibited good potent activity with an IC50 of 2.89 µM. CONCLUSION: Compound C9 is a potential candidate with potent anti-proliferative activity.

Dioscorea spp.: Bioactive Compounds and Potential for the Treatment of Inflammatory and Metabolic Diseases.

Dioscorea spp. belongs to the Dioscoreaceae family, known as "yams", and contains approximately 600 species with a wide distribution. It is a major food source for millions of people in tropical and subtropical regions. Dioscorea has great medicinal and therapeutic capabilities and is a potential source of bioactive substances for the prevention and treatment of many diseases. In recent years, increasing attention has been paid to the phytochemicals of Dioscorea, such as steroidal saponins, polyphenols, allantoin, and, in particular, polysaccharides and diosgenin. These bioactive compounds possess anti-inflammatory activity and are protective against a variety of inflammatory diseases, such as enteritis, arthritis, dermatitis, acute pancreatitis, and neuroinflammation. In addition, they play an important role in the prevention and treatment of metabolic diseases, including obesity, dyslipidemia, diabetes, and non-alcoholic fatty liver disease. Their mechanisms of action are related to the modulation of a number of key signaling pathways and molecular targets. This review mainly summarizes recent studies on the bioactive compounds of Dioscorea and its treatment of inflammatory and metabolic diseases, and highlights the underlying molecular mechanisms. In conclusion, Dioscorea is a promising source of bioactive components and has the potential to develop novel natural bioactive compounds for the prevention and treatment of inflammatory and metabolic diseases.

Self-Healing Hydrogels Fabricated by Introducing Antibacterial Long-Chain Alkyl Quaternary Ammonium Salt into Marine-Derived Polysaccharides for Wound Healing.

The development of hydrogels as wound dressings has gained considerable attention due to their promising ability to promote wound healing. However, in many cases of clinical relevance, repeated bacterial infection, which might obstruct wound healing, usually occurs due to the lack of antibacterial properties of these hydrogels. In this study, we fabricated a new class of self-healing hydrogel with enhanced antibacterial properties based on dodecyl quaternary ammonium salt (Q12)-modified carboxymethyl chitosan (Q12-CMC), aldehyde group- modified sodium alginate (ASA), Fe3+ via Schiff bases and coordination bonds (QAF hydrogels). The dynamic Schiff bases and coordination interactions conferred excellent self-healing abilities to the hydrogels, while the incorporation of dodecyl quaternary ammonium salt gave the hydrogels superior antibacterial properties. Additionally, the hydrogels displayed ideal hemocompatibility and cytocompatibility, crucial for wound healing. Our full-thickness skin wound studies demonstrated that QAF hydrogels could result in rapid wound healing with reduced inflammatory response, increased collagen disposition and improved vascularization. We anticipate that the proposed hydrogels, possessing both antibacterial and self-healing properties, will emerge as a highly desirable material for skin wound repair.

Current Perspectives on Paclitaxel: Focus on Its Production, Delivery and Combination Therapy.

Paclitaxel is an anticancer drug first isolated from the bark of the Pacific yew tree. It has been widely used for the treatment of ovarian, breast, uterine and other cancers because of its low toxicity, high efficiency and broad-spectrum anticancer activity, and it is considered to be one of the most successful natural anticancer drugs available. Paclitaxel is a microtubule-targeting drug whose main molecular mechanism is to disrupt microtubule dynamics and induce mitotic arrest and cell death. Despite the many clinical successes of paclitaxel, the extraction of natural paclitaxel from Taxus species has proven to be environmentally unsustainable and economically unviable. As a result, researchers are constantly working to find innovative ways to meet society's need for this drug. Currently, many methods, including artificial cultivation, microbial fermentation, chemical synthesis, and tissue and cell culture, have been explored and developed to obtain paclitaxel. In addition, the poor water solubility of paclitaxel has led to significant limitations in its clinical application. Conventional paclitaxel formulations use Cremophor EL and ethanol to dissolve paclitaxel, which can lead to serious side effects. In recent decades, a series of new nanotechnology-based paclitaxel dosage forms have been developed, including albumin-bound paclitaxel, polymeric micellar paclitaxel, polymer-paclitaxel couples, and liposome-encapsulated paclitaxel. These nanoformulations can significantly reduce the toxicity of paclitaxel and greatly improve its anti-tumor efficiency. This paper reviews the development of the production, dosage form and combination therapy of paclitaxel in recent years and presents an outlook, with the aim of providing a theoretical basis and reference for further research on the production and application of paclitaxel in the future.

Conductive Polyaniline Particles Regulating In Vitro Hydrolytic Degradation and Erosion of Hydroxyapatite/Poly(lactide-co-glycolide) Porous Scaffolds for Bone Tissue Engineering.

In addition to biocompatibility and bioactivity, scaffolds with superior bone tissue regenerative capacity should possess excellent functionality (e.g., electroactivity and conductivity) and biodegradability matching with the rate of bone reconstruction. However, current conductive scaffolds display a reduced biodegradability rate and weakened biocompatibility. In this study, injectable conductive porous scaffolds were fabricated, incorporating camphor sulfonic acid-doped polyaniline (PANI) into hydroxyapatite/poly(lactide-co-glycolide) (HA/PLGA) scaffolds, using solvent-casting/particulate-leaching methodology. These scaffolds demonstrated excellent electroactivity, conductivity, hydrophilicity, thermodynamic properties, antibacterial properties, and biocompatibility. Their degradation behavior was explored by regulating the PANI content. The results demonstrated that adding an appropriate content of PANI would increase the pore size, porosity, and water absorption of the conductive scaffold and promote the formation of filamentous fiber byproducts with acidic hydrolysates, which accelerated the degradation rate of the scaffold. Owing to π-π stacking and hydrogen bonding, the conductive scaffold with 10 wt % PANI efficiently retarded the decrease in the thermal and mechanical properties of the scaffolds during a 16 week degradation. Thus, better regulation of degradation behavior and correlation would allow conductive porous scaffolds, such as bone implants, to achieve better bone ingrowth and restoration.

A nanofiber/sponge double-layered composite membrane capable of inhibiting infection and promoting blood coagulation during wound healing.

Uncontrolled bleeding and bacterial infections cause severe damage to the wounds and remain a clinical challenge. Here, we developed a nanofiber/sponge bilayered composite membrane (QCP) containing quaternized silicone (QP12) and quaternized chitosan (QCS12) by joint approaches of electrospinning and freeze-drying and investigated their potential for wound dressing. The QCP was composed of a sponge (QCC) containing collagen (COL) and QCS12 and a nanofibrous membrane (MQP) containing poly-ε-caprolactone (PCL) and QP12. The QCP composite membrane possessed feasible permeability (0.22 ± 0.01 g/(cm2·24 h)), available thermal stability, suitable mechanical properties with natural skin, and in vivo hemostatic efficiency. The bonds of the N-quaternary and Schiff base endow composite membranes with significant anti-microbial invasion, potentially enhancing the wound healing process with an eligible microenvironment. Meanwhile, QCP evinced fine hemocompatibility, low cytotoxicity, negligible skin irritation, and other desirable biosafety as an excellent wound dressing. QCP promoted collagen deposition and re-epithelization to accelerate healing and suppress scars in the full-thickness acute wound models. Furthermore, the evaluation in the chronic skin incision model of diabetes mellitus manifested high healing efficiency with a certain resistance to bacterial infection of the composite membrane. Taken together, the QCP composite membrane may be a potential antibacterial and hemostatic wound dressing.

Anti-inflammatory activity of fluorine-substituted benzo[h]quinazoline-2-amine derivatives as NF-κB inhibitors.

Excessive inflammation can cause loss of tissue or organ function, leading to a number of chronic diseases and sometimes even death. Traditional treatment strategies for inflammation have mainly involved steroidal and non-steroidal anti-inflammatory drugs, but both have increasingly prominent side effects. Nuclear factor kappa B (NF-κB) inhibitors with anti-inflammatory properties and low toxicity are a new therapeutic strategy for the treatment of inflammatory diseases. To obtain novel NF-κB inhibitors, a series of 3,4-dihydronaphthalen-1(2H)-one derivatives (DHNs 6a-s), 1,4,5,6-tetrahydrobenzo[h]quinazolin-2-amine derivatives (BQAs 7a-c) and 5,6-dihydrobenzo[h]quinazolin-2-amine derivatives (BQAs 8a-p) were designed and synthesized, and characterized by NMR and HRMS. By evaluating toxicity and anti-inflammatory properties, fluorine-substituted 8c showed more potential anti-inflammatory activity and lower toxicity. 8c significantly reduced the phosphorylation of IκBα and p65, thereby inhibiting the NF-κB signaling pathway. In addition, 8c markedly decreased reactive oxygen species (ROS) production and downregulated the expression of NOD-like receptor pyrin domain-containing protein 3 (NLRP3), apoptosis-associated speck-like protein containing a CARD (ASC) and cysteine aspartate protein hydrolase-1 (caspase-1). Therefore, compound 8c is expected to be a candidate compound for NF-κB inhibition and deserves further research and development.

Stereoscopic Differences in the Identification, Bioactivity, and Metabolism of C-20 and C-24 Epimeric Ginseng Saponins.

Ginseng, the roots and/or rhizomes of Panax spp.(Araliaceae), has been used as a popular herbal medicine in East Asia for at least two millennia. As a functional food and healthenhancing supplement, ginseng has been shown to have a wide range of pharmacological effects on cognition and blood circulation as well as antioxidant, antitumor, and anti-fatigue effects. The main active properties of ginseng are considered to be the triterpene saponins, often referred to as ginsenosides, which are the basis for their wide-ranging pharmacological effects. Four of these glycosides, including protopanaxadiol, protopanaxatriol, ocotillol, and oleanolic acid, are the most common saponins found in ginseng. Compared to other ginsenosides, the C-20 chimeric ginsenosides, including Rg3, Rh2, Rg2, Rh1, PF11, C-20, and C-24, as well as epimeric ocotillol-type saponins and their derivatives exhibit significant, steric differences in biological activity and metabolism. 20(R)-ginseng saponins, one class of important rare ginsenosides, have antitumor, antioxidative, antifatigue, neuroprotective and osteoclastogenesis inhibitory effects. However, 20(R)- ginsenosides are rare in natural products and are usually prepared from 20(S)-isomers through chemical differential isomerization and microbial transformation. The C20 configuration of 20(R)-ginseng saponins is usually determined by 13C NMR and X-ray single-crystal diffraction. There are regular differences in the chemical shift values of some of the carbons of the 20(S)- and 20(R)-epimers, including C-17, C-21, and C-22. Owing to their chemical structure and pharmacological and stereoselective properties, 20(R)-ginseng saponins have attracted a great deal of attention in recent years. Herein, the stereoscopic differences in the identification, bioactivity, and metabolism of C-20 and C-24 epimeric ginseng saponins are summarized.