Journal of Holistic Integrative Pharmacy最新文献

Cardiovascular diseases are the leading causes of death globally. Their pathological mechanisms are complex and have not yet been fully clarified. With the development of epigenetics research in recent years, the epigenetic modification N⁶-methyladenosine (m⁶A) has been demonstrated to play an important role in the occurrence and development of cardiovascular diseases. Moreover, m⁶A methyltransferases, demethylases, and recognition proteins can regulate m⁶A methylation levels in the RNA, affecting various biological processes such as RNA splicing, nuclear export, protein translation, and degradation. In this paper, we focus on the biological functions of m⁶A and investigate its role in the biological processes of apoptosis, inflammation, oxidative stress, energy metabolism, and lipid metabolism. Furthermore, we describe the current findings on the mechanisms involving m⁶A in cardiovascular diseases and discuss potential drugs targeting m⁶A for therapy.

Objective

The aim of this study is to search for potent analgesics from the stems of Gelsemium elegans.

Methods

Alkaloids were isolated from the samples of G. elegans and purified using column chromatograph and High-Performance Liquid Chromatography. The chemical structures of the isolated alkaloids were determined using extensive high resolution electrospray ionization mass spectroscopy (HRESIMS) and nuclear magnetic resonance (NMR) spectroscopic data analyses, ¹³C NMR DP4+ analysis and electronic circular dichroism (ECD) calculations, and Rh₂(OCOCF₃)₄-induced ECD data analysis. The analgesic activities of all the isolates were analyzed using an acetic acid-induced writhing test in mice.

Results

Two new monoterpene indole alkaloids, elegansine A (1) and 14-hydroxysempervirine (2), and seven known monoterpene indole alkaloids were isolated from the stems of G. elegans. Elegansine A (1) represents the first example of sarpagine-type alkaloids with a Δ¹⁵⁽²⁰⁾ double bond. All the alkaloids (1–9) showed potential analgesic activities. Three alkaloids, namely 14-hydroxysempervirine (2), 14β,20α-dihydroxydihydrorankinidine (4), and 14-hydroxygelsenicine (6), exhibited significant analgesic activities in the acetic acid-induced writhing test in mice at a dose of 5.0 mg/kg with the writhing inhibition rates of 69.5%, 69.2%, and 72.7%, respectively.

Conclusion

These results enlarged the diversity of monoterpene indole alkaloids and also provided a new basis to develop novel potent analgesics.

Two undescribed phenylacetate derivatives (compounds 1 and 2) with a known analog were isolated from a soil-derived fungus Penicillium canescens through the “one strain-many compounds” method. The new structures were assigned using extensive 1D and 2D NMR spectra, high-resolution electrospray ionization mass spectrometry, and the comparison of coupling cleavages of known compounds, which are two pairs of racemic mixtures of aromatic polyketides with a terminal butan-2,3-diol group. In the bioassay, the biological screening signifies no cytotoxic activities against several human cancer cell lines (HL-60, A549, SMMC-7721, MCF-7, and SW480) at a concentration of 40.0 µM.

Objective

This study aims to search for structurally novel, natural bioactive products from mangrove-derived fungi.

Methods

Compounds were isolated and purified by column chromatography on HP20 macroreticular resin, silica gel, Sephadex LH-20 gel, and high performance liquid chromatography. The structures of the isolates were analyzed using NMR and MS data, and the absolute configuration of 1 was determined by calculated ECD spectroscopic methods. The cytotoxicity of all the isolates was tested against HCT-116, HepG2, HEK 293t, and 5637 cancer cell lines using CCK-8 assay.

Results

A new tetrahydroisoquinoline named peniciisoquinoline A (1) was obtained from Penicillium sp. DM27 along with five known compounds. Peniciisoquinoline A (1) was inactive against the four cancer cell lines.

Conclusion

This study conducted chemical research on Penicillium sp. DM27 and tested the cytotoxic activity of the new alkaloid (1), which will assist in the further development and utilization of mangrove-derived fungi.

The mangrove soil-derived microbes, especially genus Streptomyces strains, have proven to be a rich source of bioactive secondary metabolites and play a critical role in the development of pharmaceutical researches. To understand the structural diversity and bioactivities of the metabolites from the mangrove soil-derived Streptomyces strains, this review for the first time provides a comprehensive overview of 168 natural products isolated from the mangrove soil-derived Streptomyces strains with their bioactivities, up to the end of 2021. Most of the structural types of these compounds are alkaloids, lactones, xanthones, and quinones. The pharmacological mechanisms of some representative lead compounds are well studied, revealing that they have important medicinal potential. This review provides an important reference for the research status of natural products isolated from mangrove soil-derived genus Streptomyces, and reveals that mangrove soil-derived Streptomyces is an important resource of pharmaceutical molecules.

Microorganisms are a seemingly inexhaustible source of bioactive secondary metabolites, which play a crucial role in discovering potential drug candidates and expanding the structural diversity of natural products. Polyketides are a large group of secondary metabolites mainly derived from microorganisms, harboring architecturally distinct scaffolds and diverse bioactivities. This review highlights the roles of macrocyclic polyketides isolated from bacteria and fungi, as well as their sources, structure diversity, and biological activities. Total 242 macrocyclic polyketides mainly reported in recent two decades were covered in this review, including 165 ones from bacteria and 77 ones from fungi. Their structures could be divided into macrolactams, macrolides in bacteria, and macrolides, polyesters in fungi. And these compounds displayed cytotoxic, antibacterial, antifungal, and also some other activities, such as antimalarial and antitrypanosomal activities.

Objective

To study the chemical compositions from Selaginella doederleinii Hieron.

Methods

The petroleum ether and ethyl acetate fractions of 80% ethanol extract of S. doederleinii were separated and purified by macroporous resin, silica gel, Sephadex LH-20 and semi-preparative HPLC, and then the structures of obtained compounds were identified by physicochemical properties and spectroscopical data.

Results

A total of 7 compounds were isolated and identified as seladoeneolignan A (1), ethoxy-ferulate (2), 11-dien-19-oic acid (3), aurantiamide (4), 9,16-dioxo-10,12,14-octadeca-trienoic acid (5), amentoflavone (6), and 7,4’-di-0-methylrobustaflavone (7).

Conclusion

Compound 1 was a new neolignan obtaind from S. doederleinii for the first time. Compounds 1, 6 and 7 were screened for antitumor activity in vitro, and the testing results showed that 3 compounds had low inhibitory activity on Hep-2 and Eca-109 tumor cells.

Objective

Study on the non-alkaloid chemical constituents with novel structure and their biological activities from the w-butanol fraction of the leaves of Rauvolfia vomitoria.

Methods

The w-butanol fraction of R. vomitoria was separated by silica gel, ODS, and Sephadex LH-20 chromatography column, as well as semi-preparative HPLC to obtain five compounds. Their structures were identified by extensive spectroscopic analysis, including HRESIMS, 1D and 2D NMR, and ECD analysis. All the isolated compounds were evaluated their AChE inhibitory activities by Ellman’s method with slight modification, their vasorelaxant activities against phenylephrine-induced contraction of rat mesenteric arteries, and their inhibitory activity of a-glucosidase employing pNPG as substrate.

Results

Two new phenylpropanoids (1-2) along with three known compounds, methyl trans-3,4,5-trimethoxycinnamate (3), methyl cis-3,4,5-trimethoxycinnamate (4), and 3,4,5-trimethoxybenzoic acid methyl ester (5), were isolated from the leaves of R.vomitoria. The five isolated compounds did not show significant tested activity.

Conclusion

Chemical investigation of the leaves of R. vomitoria led to the isolation and identification of two new phenylpropanoids (1–2), expanding the study of non-alkaloids in the genus of Rauvolfia and enriching the chemical diversity of this genus.

Objective

To study the chemical constituents of the roots of Ephedra sinica Stapf.

Methods

The roots of E. sinica were extracted with 90% ethanol and isolated and purified by column chromatography on silica gel, Sephadex LH 20, and semipreparative RP-HPLC. All the compounds were identified based on spectral analysis (including MS, ¹H-NMR and ¹³C-NMR, and 2D NMR) and compared with the reported literature. Their cytotoxicities were evaluated against three human cancer cell lines.

Results

Two compounds were isolated from the roots of E. sinica and identified as (E)-eicosyl 3,4-dihydroxy-5-methoxycinnamate (1) and (E)-hexadecyl-ferulate (2).

Conclusion

Compound 1 was a new phenol named ephedrate A, and compound 2 was newly isolated from this plant. These two compounds showed no obvious cytotoxic activity, and their medicinal activities need to be studied further.

Objective

To obtain structurally novel and bioactive secondary metabolites from the marine fungus Xylariaceae sp. SCSIO41212.

Methods

Compounds were purified by comprehensive chromatography methods of silica gel column, Sephadex LH-20, Ostade-cylsilane (ODS) and semi-preparative HPLC, and their structures were elucidated by means of physical and chemical properties, magnefic resonance imaging, spectroscopic analysis, and comparison with the reported literatures.

Results

Chemical investigation of the fungus Xylariaceae sp. SCSIO41212 has led to the isolation of two new compounds, xylaolide B (1) and xylaolide C (2), together with nine known compounds (3–11). Their structures were determined on the basis of detailed analysis of the 1D and 2D NMR as well as MS data. Compounds 1–6 were evaluated for their antiviral, and cytotoxic activities, respectively. Compound 1 showed weak cytotoxicities against K562, MCF-7 and SGC7901 respectively.

Conclusion

This study enriches the diversity of secondary metabolites of marine-derived fungi and provides an important reference for novel promising drug leads research.