Research progress of nano-delivery systems for the active ingredients from traditional Chinese medicine.

INTRODUCTION: Traditional Chinese medicine (TCM) has been used for thousands of years in China, characterizing with novel pharmacological mechanisms, low toxicity, and limited side effects. However, the application of TCM active ingredients is often hindered by their physical and chemical properties, including poor solubility, low bioavailability, short half-life, toxic side effects within therapeutic doses, and instability in biological environments. Consequently, an increasing number of researchers are directing their attention towards the discovery of nano-delivery systems for TCM to overcome these clinical challenges. OBJECTIVES: This review aims to provide the latest knowledge and results concerning the studies on the nano-delivery systems for the active ingredients from TCM. MATERIALS AND METHODS: Recent literature relating to nano-delivery systems for the active ingredients from TCM is summarized to provide a fundamental understanding of how such systems can enhance the application of phytochemicals. RESULTS: The nano-delivery systems of six types of TCM monomers are summarized and categorized based on the skeletal structure of the natural compounds. These categories include terpenoids, flavonoids, alkaloids, quinones, polyphenols, and polysaccharides. The paper analyzes the characteristics, types, materials used, and the efficacy achieved by TCM-nano systems. Additionally, the advantages and disadvantages of nano-drug delivery systems for TCM are summarized in this paper. CONCLUSION: Nano-delivery systems represent a promising approach to overcoming clinical obstacles stemming from the physical and chemical properties of TCM active ingredients, thereby enhancing their clinical efficacy.

Synthesis of structurally diverse derivatives of aconitine-type diterpenoid alkaloids and their anti-proliferative effects on canine breast cancer cells.

As one of the most common malignancies in female dogs, no drugs have been developed specifically for the treatment of canine mammary carcinoma. In our previous study, a series of diterpenoid alkaloids derivatives were synthesized and exhibited good anti-proliferative activity in vitro against both normal and adriamycin-resistant human breast cancer cells lines. In this study, a series of structurally diverse aconitine-type alkaloids derivatives were also synthesized basing on the minimal modification principle, by modifying on A-ring, C-ring, D-ring, N-atom or salt formation on aconitine skeleton. Their anti-proliferative effects and mechanism on canine mammary cancer cells were investigated, exhibiting the importance of the substitution at A ring, the long chain ester at the C8, the hydroxyl group at the C13, the phenyl ring at the C14 and the N-ethyl group, while the methoxy group at the C1 and C16 showed little effect on the activity. The results of the proliferation, apoptosis and ultrastructure tests of the treated canine mammary carcinoma cells referred that the representative compound, aconitine linoleate (25) could block the cell cycle of canine mammary carcinoma cells in the G0/G1 phase, and exhibit the anti-proliferative effect by inducing apoptosis.

Response surface methodology for optimization of the extraction of polysaccharide from the roots of onosma hookeri clarke. var. longiforum duthie and its antioxidant capacity and immune activity.

Onosma hookeri Clarke. var. longiforum Duthie (OHC-LD), one of the traditional Tibetan medicine, has been found many functions, including removing heat to cool blood, nourishing lung and inhibiting bacteria. In order to study the polysaccharides in OHC-LD water extract, the optimal extraction progress of polysaccharides of the roots of OHC-LD by response surface method designed with three-factor three-level Box-Behnken method and the antioxidant capacity and immune activity of the crude polysaccharide were studied in this investigation. Under the best conditions, the extraction yield of polysaccharide was 3.19±0.09% (n = 3). After purification, the crude polysaccharide was obtained with polysaccharide contents of 42.57%, which demonstrated stronger DPPH scavenging activity than BHT at low concentrations (<625 µg/mL), and comparable ABTS radical scavenging activity as BHT at high concentrations (≥1250 µg/mL). Additionally, it also exhibited a certain cell proliferation activity and an enhancement of the phagocytic ability of RAW264.7 cells. This study revealed that the crude polysaccharide from the roots of OHC-LD might be exploited as a natural antioxidant and immune enhance agent in the future in both medical and food industry.

An update of new small-molecule anticancer drugs approved from 2015 to 2020.

A high incidence of cancer has given rise to the development of more anti-tumor drugs. From 2015 to 2020, fifty-six new small-molecule anticancer drugs, divided into ten categories according to their anti-tumor target activities, have been approved. These include TKIs (30 drugs), MAPK inhibitors (3 drugs), CDK inhibitors (3 drugs), PARP inhibitors (3 drugs), PI3K inhibitors (3 drugs), SMO receptor antagonists (2 drugs), AR antagonists (2 drugs), SSTR inhibitors (2 drugs), IDH inhibitors (2 drugs) and others (6 drugs). Among them, PTK inhibitors (30/56) have led to a paradigm shift in cancer treatment with less toxicity and more potency. Each of their structures, approval statuses, applications, SAR analyses, and original research synthesis routes have been summarized, giving us a more comprehensive map for further efforts to design more specific targeted agents for reducing cancer in the future. We believe this review will help further research of potential antitumor agents in clinical usage.