Publications by authors named "Hai-min Lei"

The processing of traditional Chinese medicine(TCM) is a core theory within TCM, embodying deep philosophical, cultural, and natural scientific wisdom. Among the various techniques, the "synergistic processing of medicinal materials and excipients" has garnered significant attention due to its uniqueness. This study explored the impact of the adjuvant Glycyrrhizae Radix et Rhizoma on the dynamic process of component transformation during the processing of Aconiti Lateralis Radix Praeparata using techniques such as acidic dye colorimetry, UPLC-Q-TOF-MS/MS, density functional theory(DFT), and molecular dynamics simulations(MDS).

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Ethnopharmacological Relevance: Niuhuang Shangqing Pill (NSP) is a renowned Chinese medicine prescription listed in the Chinese Pharmacopoeia (Edition, 2020; volume 1) and is utilized in clinical practice for treating headaches and acute pharyngitis (AP) associated with "Shanghuo". Despite its widespread use, the pharmacological mechanism and bioactive components underlying NSP in treating AP remain unclear.

Aim Of The Study: This study delved into evaluate the alleviation effect of NSP on AP and explore the mechanisms by analyzing multi-omics.

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Ethnopharmacological Relevance: Accumulation of heat in the lungs and stomach (AHLS) is an important syndrome within the realm of traditional Chinese medicine (TCM). It is the fundamental reason behind numerous illnesses, including mouth ulcers, dermatological conditions, acne, and pharyngitis. Jingzhi Niuhuang Jiedu tablet (JN) serves as the representative prescription for treatment of AHLS clinically.

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Background: Therapeutic approaches based on glycolysis and energy metabolism of tumor cells are new promising strategies for the treatment of cancer. Currently, researches on the inhibition of pyruvate kinase M2, a key rate limiting enzyme in glycolysis, have been corroborated as an effective cancer therapy. Alkannin is a potent pyruvate kinase M2 inhibitor.

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Article Synopsis
  • Ulcerative colitis (UC) is a chronic inflammatory condition treated using heat-clearing and toxin-removing substances like Coptidis Rhizoma and Bovis Calculus, which contain active compounds berberine (BBR) and ursodeoxycholic acid (UDCA).
  • Researchers developed a new treatment method using UDCA-BBR supramolecular nanoparticles, which were created through a co-decocting process and characterized as tetrahedral nanoparticles with an average size of 180 nm.
  • In experimental studies on mice with UC, these nanoparticles significantly improved various health metrics, including body weight and inflammation markers, while outperforming a standard mechanical mixture of the components.
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Chuanxiong, a traditional Chinese medicine, has been proved to treat a variety of cardiovascular and cerebrovascular diseases by promoting angiogenesis. However, the mechanisms of Chuanxiong's pro-angiogenesis is currently unknown. This study aimed to uncover the effect and mechanisms of Chuanxiong promoting angiogenesis and .

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We prepared 15 batches of Kaixin Powder benchmark samples with the decoction pieces of different batches. Further, we established the specific chromatograms and index component content determination method of Kaixin Powder benchmark samples and analyzed the peaks and similarity of the chromatograms. With sibiricose A5, sibiricose A6, polygalaxanthone Ⅲ, 3,6'-disinapoyl sucrose, ginsenoside Rb_1, β-asarone, α-asarone, and dehydropachymic acid as index components, the index component content determination method was established and 70%-130% of the mean content of each component was set as the range.

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Article Synopsis
  • The study focuses on developing new antibacterial agents to combat multidrug-resistant bacteria, particularly Staphylococcus aureus (MRSA).
  • A series of glycyrrhetinic acid (GA) derivatives were synthesized, with compound 11 demonstrating the strongest antibacterial activity against MRSA at an MIC of 3.125 μM, much more effective than traditional antibiotics like penicillin and norfloxacin.
  • The mechanism of compound 11 was found to obstruct arginine biosynthesis and metabolites, and it also showed good biocompatibility in various tests, highlighting its potential as a candidate for treating MRSA infections.
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The present study aimed to explore the material basis of Rhei Radix et Rhizoma-Coptidis Rhizoma combination in alleviating "bitter-cold" properties based on the supramolecular chemistry of Chinese medicine.Dynamic light scattering and scanning/transmission electron microscopy were used to characterize the morphological characteristics of supramolecules in the decoction of Rhei Radix et Rhizoma and Coptidis Rhizoma.The chemical composition of supramolecules, as well as the dissolution and release processes of supramolecules and the medicinal components of Coptidis Rhizoma decoction, was determined by the high-performance liquid chromatography-mass spectrometry.

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Podophyllotoxin's undifferentiated cytotoxicity and poor selectivity limit its clinical application. To improve above disadvantages, conjugation of bile acids with podophyllotoxin could improve cell line selectivity of liver cancer to achieve clinical translation further. Enlightened by the bile acids' moiety magic characters, thirty podophyllotoxin-linked bile acid derivatives had been designed and synthesized.

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Article Synopsis
  • A combination of network pharmacology and mass spectrometry was employed to analyze the antioxidant properties of Hippophae tibetana, identifying key quality markers (Q-markers) responsible for its antioxidant effects.
  • The study used ultra-high performance liquid chromatography to separate the chemical components of H. tibetana, revealing 51 different constituents, including various flavonoids, terpenoids, and alkaloids.
  • The antioxidant efficacy of different extract fractions was evaluated, finding that flavonoids like quercetin, luteolin, and kaempferol significantly influence the antioxidant activity, primarily through the PI3 K-Akt and FoxO signaling pathways.
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Objective: There are some anthraquinones, anthraquinones and flavonones in which exhibited significant acidity, such as sennoside A/B and sennoside C/D. The current strategies used in separating these components are mainly based on conventional column chromatography which is time consuming, laborious and costly. This study is aimed at exploring a method of precipitation extraction of acid components in .

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The ligustrazine - betulin derivative (TB), TB amino acids derivatives (TB-01 - TB-09) and TB dipeptide derivatives (TB-10 - TB-18) were designed and synthesized. And their in vitro cytotoxic activities were evaluated against four cancer cell lines (Hela, HepG2, BGC-823 and HT-29) and normal cells MDCK by standard methylthiazol tetrazolium (MTT) assay. Most of them demonstrated better antitumor activity than the relevant material betulin.

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As for complex brain diseases involved with multiple pathogenic factors, it is extremely difficult to achieve curative effect by acting on a single target. Multi-approach drugs provide a promising prospect in the treatment of complex brain diseases and have been attracting more and more interest. Enlightened by synergetic effect of combination in traditional herb medicines, forty-two novel cinnamic acid derivatives were designed and synthesized by introducing capsaicin and/or ligustrazine moieties to enhance biological activities in both neurological function and neurovascular protection.

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Glycyrrhetinic acid (GA) had been the star anticancer lead compound and appealed to many scientists all over the world; however, its antitumor activity was not potent enough. To improve GA's cytoxicity and explore the effect of bonding mode on antitumor activity, 32 compounds including GA-OH series (GO, esters in C-3 position) and GA-NH series (GN, with amide linkages in C-3 position) had been designed and synthesized. All the compounds were screened for in vitro cytotoxicity against A549, HepG2, MCF-7, Hela and MDCK cell lines.

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Clinical applications of camptothecin () have been heavily hindered due to its non-targeted toxicity, active lactone ring instability, and poor water solubility. Targeted drug delivery systems may offer the possibility to overcome the above issues as reported. In this research, a series of prostate-specific membrane antigen (PSMA)-activated prodrugs were designed and synthesized by coupling water-soluble pentapeptide, a PSMA hydrolyzing substrate, to through an appropriate linker.

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Hederagenin () is a novel triterpene template for the development of new antitumor compounds. In this study, 26 new ⁻pyrazine derivatives were synthetized in an attempt to develop potent antitumor agents; they were screened for in vitro cytotoxicity against tumor and non-tumor cell lines The majority of these derivatives showed much stronger cytotoxic activity than . Remarkably, the most potent was compound (half maximal inhibitory concentration (IC) was 3.

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To improve podophyllotoxin's cytotoxicity and selective effect, twenty-two podophyllotoxin derivatives had been designed and synthesized. The cytotoxicity of these compounds was evaluated on A549, MCF-7, HepG2 and L-02 cell lines. As a result, most of the compounds were more potent than the positive drugs Etoposide (VP-16) and Doxorubicin which were widely used in clinical for antitumor.

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It has been focused on that there will be precipitates when decoction of Scutellariat Radix mixed with Coptidis Rhizoma. Precipitation was derived from interaction between acidic and basic compounds. This study was based on the interaction between active ingredients after compatibility, strived to explore whether it was feasible to judge the qualities of different Scutellariat Radix by isothermal titration calorimetry (ITC), build a new method established to characterize the qualities of traditional Chinese medicine by taking a series of active ingredients as index.

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Glycyrrhetinic Acid (), a triterpenoid aglycone component of the natural product glycyrrhizinic acid, was found to possess remarkable anti-proliferative and apoptosis-inducing activity in various cancer cell lines. Though was not as active as other triterpenes, such as betulinic acid and oleanolic acid, it could trigger apoptosis in tumor cells and it can be obtained easily and cheaply, which has stimulated scientific interest in using as a scaffold to synthesize new antitumor agents. The structural modifications of reported in recent decades can be divided into four groups, which include structural modifications on ring-A, ring-C, ring-E and multiple ring modifications.

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Qingwen Baidu Decoction (QBD) is an extraordinarily "cold" formula. It was traditionally used to cure epidemic hemorrhagic fever, intestinal typhoid fever, influenza, sepsis and so on. The purpose of this study was to discover relationships between the change of the constituents in different extracts of QBD and the pharmacological effect in a rat model of acute lung injury (ALI) induced by lipopolysaccharide (LPS).

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The lead compound TBA, 3β-Hydroxy-lup-20(29)-ene-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester, which exhibited promising antitumor activity and induced tumor cell apoptosis in various cancer cell lines, had previously been reported. Moreover, reports have revealed that the introduction of amino acid to betulinic acid could improve selective cytotoxicity as well as water solubility. Thus, a series of novel TBA amino acid and dipeptide derivatives were designed, synthesized and screened for selective cytotoxic activity against five cancer cell lines (HepG2, HT-29, Hela, BCG-823 and A549) and the not malignant cell line MDCK by standard MTT assay.

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Ischemic brain injury is a major disease which threatens human health and safety. (3, 5, 6-trimethylpyrazin-2-yl) methyl 3-methoxy-4-[(3, 5, 6-trimethylpyrazin-2-yl) methoxy] benzoate (VA-T), a newly discovered lead compound, is effective for the treatment of ischemic brain injury and its sequelae. But the poor solubility of VA-T leads to poor dissolution and limited clinical application.

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This research is to study the relationship between HPLC fingerprints of Moutan Cortex, Paeoniae Radix Rubra and Paeoniae Radix Alba and their activity on lipopolysaccharide-induced acute lung injury. HPLC fingerprints of each extract of Moutan Cortex,Paeoniae Radix Rubra and Paeoniae Radix Alba were established by an optimized HPLC-MS method. The activities of all samples against protein and tumor necrosis a factor were tested by the model of lipopolysaccharide-induced acute lung injury.

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Background: Porcine reproductive and respiratory syndrome virus (PRRSV) is one of the major swine pathogens. This virus causes immune suppression and other secondary infections, leading to significant economic losses in the swine industry. Tea seed saponins (TS) are a natural extract from tea seeds with anti-cancer, anti-inflammatory and antiviral activity.

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Synopsis of recent research by authors named "Hai-min Lei"

  • - Hai-Min Lei's research focuses on the integration of traditional Chinese medicine with modern pharmacological approaches, such as network pharmacology and supramolecular chemistry, to uncover the mechanisms behind herbal treatments and develop novel therapeutic agents.
  • - Recent findings include the effects of Jingzhi Niuhuang Jiedu tablet on treating heat accumulation syndromes, anti-tumor activities of alkannin derivatives, and the enhancement of therapeutic effects for ulcerative colitis using supramolecular nanoparticles, showcasing the efficacy of traditional formulations combined with advanced methodologies.
  • - Lei's studies emphasize the importance of understanding chemical composition and structural modifications in natural compounds to optimize their biological activities, which could lead to innovative solutions for complex diseases including cancer and inflammatory conditions.