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Mulberry silkworm cocoon (MSC) carbonisata has been used for the treatment of inflammatory diseases for hundreds of years; however, after years of research efforts, little information is available on its anti-inflammatory components and underlying mechanism. We developed novel carbon dots (CDs) derived from MSC carbonisata (MSC-CDs), for the first time, with an average diameter of 2.26-9.35 nm and a quantum yield (QY) of 6.32%. The MSC-CDs were prepared using a modified pyrolysis method, and no further modification and external surface passivation agent was required. With abundant surface groups, MSC-CDs showed distinct solubility and bioactivity. In this study, we innovatively used three classical experimental models of inflammation to evaluate the anti-inflammatory bioactivity of MSC-CDs. The results indicated that MSC-CDs exhibited marked anti-inflammatory bioactivity which was likely mediated by inhibition of the expression of interleukin-6 and tumour necrosis factor-α. These results suggest that MSC-CDs possess a remarkable anti-inflammatory property, which provides evidence to support further investigation of the considerable potential and effective material basis of this traditional Chinese medicine.

Baicalin (BA) has gained considerable attention in recent years for its multiple pharmacological activities. However, its optimum pharmaceutical potential has been limited by its poor solubility in water. In this study, for the first time, we discovered that novel water-soluble carbon dots (CDs, named RPC-CDs) from aqueous extracts of Radix Puerariae Carbonisata (RPC). The chemical composition and morphological features of the RPC-CDs we obtained were characterized using various spectroscopies and transmission electron microscopy and the CDs have a low toxicity against RAW 264.7 cells by the CCK-8 assay. Most importantly, the RPC-CDs were able to greatly increase the solubility of baicalin in water, which could be related to the glucuronide structure of baicalin. Moreover, the result of indirect competitive enzyme-linked immunosorbent assays (icELISA) indicated that the area under the baicalin concentration-time curve value of baicalin-RPC-CDs (BA-CDs) was 1.7-fold greater than those of a baicalin suspension liquid (BA control) after oral administration at a dose of 72 mg/kg. This study not only provides evidence to support further investigation of the considerable potential of carbon dots, but also offers support for the future clinical application of baicalin.

Background As an emerging nanomaterial, carbon dots (CDs) have been the focus of tremendous attention for biomedical applications. However, little information is available on their bioactivity of inhibiting acute kidney injury (AKI) induced by snake venom. Methods This study reports the development of a green, one-step pyrolysis process to synthesize CDs using Phellodendri Chinensis Cortex (PCC) as the sole precursor, and their potential application as a protectant against Deinagkistrodon acutus (D. acutus) venom-induced AKI was investigated for the first time. The AKI model was established by injecting D. acutus venom into the abdominal cavity of mice and the potential protective effects of PCC Carbonisata-CDs (PCCC-CDs) on renal abnormalities including dysfunction, inflammatory reactions, tissue damage, and thrombocytopenia at six time points (1, 3, and 12 h, and 1, 2, and 5 days) were investigated. Results These results demonstrated that PCCC-CDs significantly inhibited the kidney dysfunction (reduced serum creatinine (SCR), blood urea nitrogen (BUN), urinary total protein (UTP), and microalbuminuria (MALB) concentrations) and the production of chemoattractant (monocyte chemotactic protein 1 (MCP-1)), proinflammatory cytokines (interleukin (IL)-1β), and anti-inflammatory cytokine (IL-10) in response to intraperitoneal injection of D. acutus venom. The beneficial effect of PCCC-CDs on the envenomed mice was similar to that on the change in renal histology and thrombocytopenia. Conclusions These results demonstrated the remarkable protective effects of PCCC-CDs against AKI induced by D. acutus venom, which would not only broaden the biomedical applications of CDs but also provide a potential target for the development of new therapeutic drugs for AKI induced by D. acutus snakebite envenomation.

Schizonepetae Spica Carbonisata (SSC) has pronounced haemostatic effects for hundreds of years and has been acknowledged in the 2015 Pharmacopoeia of the People's Republic of China (PPRC) as a haemostatic charcoal drug. However, after years of efforts, the underlying mechanism and the material basis is still less defined. In this research, we developed a novel CDs derived from SSC (SSC-CDs) with an average diameter of 1.29-6.87 nm and a quantum yield of 6.31%. SSC was prepared using a modified pyrolysis method and no further modification and external surface passivation agent is required. With abundant surface groups, SSC-CDs showed distinct solubility and bioactivity. In this study, we innovatively used the Deinagkistrodon acutus (D. acutus) venom model as well as the classical haemorrhagic animal model to evaluate the haemostatic bioactivity of SSC-CDs. The results indicated that SSC-CDs had outstanding haemostatic bioactivity and might inhibit the haemorrhagic activity via PLT elevation. According to the results of this study and our previous work, we discovered that CDs derived from different kinds of charcoal drugs presented similarities and differences in the structural feature, physicochemical property and bioactivity. In order to further explore the self-bioactivities, we first named this kind of CDs as "Chinese Medicine charcoal drug nanoparticles" (CMNP). These results may not only provide evidence for further researches of self-bioactivities of CDs but give new insights into potential biomedical and healthcare applications of CDs, therefore, make contributions to future drug discovery.

We have been looking for a faster and simpler method for traditional Chinese medicine and natural product assay. In this study, we developed a fluorescent immunoassay approach to detect icariin (ICA) using a fluorescently labelled monoclonal antibody. The ICA-specific antibody was purified by the caprylic acid-ammonium sulphate method and then labelled with rhodamine B isothiocyanate (RBITC). Subsequently, an indirect competitive fluorescence-linked immunosorbent assay (icFLISA) was developed to detect ICA using RBITC-labelled anti-ICA MAbs. The RBITC-labelled monoclonal antibody was highly specific for ICA. The fluorescence assay demonstrated an effective ICA measurement range of 1.28 ng/mL to 20 μg/mL (R2 = 0.9946) with relative standard deviations below 10% for both intra-assay and inter-assay repeatability and precision. This icFLISA for ICA is simple, rapid, and sensitive, with a 20-fold greater linear range and a 10-fold lower limit of detection than with the previously developed indirect competitive enzyme-linked immunosorbent assay (ELISA). Thus, this study establishes a useful method for detecting ICA, enabling in vivo visualization research. In the future, FLISA can be also used to assay the concentrations of ICA in biological samples, as well as to investigate the pharmacokinetics of ICA in different tissues to explore the targets of ICA in vivo.