Natural Products Journal, The - Volume 14, Issue 4, 2024

Sophora japonica, a species of Sophora, one of the prominent genera, belongs to the family Fabaceae, native to China, which is commonly known as a pagoda tree. Sophora, includes nearly 52 species, nineteen varieties and many of these species have been used in traditional Chinese medicine to cure various ailments. This review compiles its ethnomedical uses, diverse phytochemicals reported from the various parts of S. japonica, and their pharmacological effects to elucidate its therapeutic potential against a wide range of diseases. Traditionally it is used to treat various hematic disorders such as hypertension, hemorrhoids, hemorrhage, hematuria, hematochezia, dysentery, arteriosclerosis, etc. Moreover, each and every part of this plant, including the flowers, buds, leaves, bark, fruits, seeds, pericarp, stems, and roots are used as medicine, particularly in China, Japan, Korea, and Asia. Chinese Pharmacopoeia and European Pharmacopoeia describe the utility of this plant since ancient times. The enhanced use of S. japonica in Chinese medicine resulted in the exploration of various phytochemicals and their pharmacological properties includes in vitro, in vivo, and clinical studies. It is enchanted with steroids, phospholipids, flavonoids, isoflavonoids, alkaloids, triterpenes, and other phenolic compounds that are characterized by therapeutic activities such as anti-oxidant, anticancer, anti-asthmatic, anti-neoplastic, antimicrobial, antiviral, antidote, anti-pyretic, cardiotonic, anti-inflammatory, diuretic, anti-platelet, anti-hyperglycemic, immunomodulatory, anti-diabetic, estrogenic, and anti-osteoporotic activity in post-menopausal women etc. and this is also used as a remedy for skin diseases like eczema, colpitis, and psoriasis. Despite its health benefits, supplementary data is still required in order to bridge the gaps and ensure the possible safety profile by conducting clinical studies for its therapeutic applications as a natural and eminent safe drug.

Phosphodiesterases (PDEs) function to hydrolyze intracellular cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), regulating a variety of intracellular signal transduction and physiological activities. PDEs can be divided into 11 families (PDE1~11) and the diversity and complex expression of PDE family genes suggest that different subtypes may have different mechanisms. PDEs are involved in various disease pathologies such as inflammation, asthma, depression, and erectile dysfunction and are thus targets of interest for several drug discovery campaigns. Natural products have always been an important source of bioactive compounds for drug discovery, over the years several natural compounds have shown potential as inhibitors of PDEs. In this article, phosphodiesterase inhibitors of natural origin have been reviewed with emphasis on their chemistry and biological activities.

Osthole is a coumarin derived natural compound which is an essential ingredient of Traditional Chinese Medicine (TMC) and is widely distributed in nature in plants like Cnidium monnieri (L) Cusson and Angelica pubescens. Current study presents a critical review on description of pharmacological importance of osthole, which is reported to exhibit anticancer, antioxidant, osteogenic, hepatoprotective, neuroprotective, cardiovascular protective, antimicrobial, immuno-modulatory and anti-inflammatory activities. Till date, the reports include pharmacological properties, brief chemistry of advanced methods to explore osthole content in variety of plants. Present review seeks to highlight the sources, biosynthesis, extraction methods, pharmacological properties of the molecule and its derivatives. A brief discussion on patents recently published and granted on the molecule has also been highlighted. Thus the overview of the literature presents the analysis about future possible modalities of the research on this molecule.

Background: Accumulated investigations have demonstrated that the Mariana Trench is enriched in microorganisms. However, the diversity of structures and bioactivities of the secondary metabolites produced by the Mariana Trench-associated microorganisms is poorly known, which needs to be intensively investigated. Objective: This study aimed to investigate the bioactive secondary metabolites produced by a Mariana Trench-derived actinomycete Streptomyces sp. SY1414 that was cultured in BY medium, which was chosen from four different media based on the diversity of secondary metabolites. Methods: A combination of different column chromatographs and HPLC was applied for the separation and purification of the secondary metabolites. The structures of the isolated compounds were determined mainly based on their NMR data, optical rotation values, and the comparison with the reference data, and the Sulforhodamine B (SRB) method was used to evaluate their anti-glioma activities. Results: Four different types of compounds were isolated from the large culture of strain Streptomyces sp. SY1414 in BY medium, including a benzoquinoline alkaloid, actinophenanthroline C (1), a benzamide, (2E,4E)-5-(3-hydroxyphenyl)-penta-2,4-dienamide (2), a cyclopeptide, valinomycin (3), and four macrolides of bafilomycin D (4), bafilomycin A2 (5), bafilomycin W (6), and C(19), C(21)- O-methyl-bafilomycin A1 (7). Actinophenanthroline C (1), bafilomycin D (4), bafilomycin A2 (5), and bafilomycin W (6) displayed significant anti-glioma activities with IC50 values ranging from 1.62 to 8.20 μM for U87MG cells and 2.45 to 3.89 μM for U251. The anti-gliomas of actinophenanthroline C (1) was reported for the first time. Conclusion: The hadal actinomycete Streptomyces sp. SY1414 in BY medium produced four different types of secondary metabolites with significant anti-glioma activity, which enriched the diversity of structures and bioactivities of the Mariana Trench-associated natural products.

Background: Cancer is a serious disease severely endangering human health and life in the world in the world, and conventional anticancer drugs have frequently suffered from severe side effects and resistance. Therefore, developing novel and effective therapeutic strategies is urgently needed. As a Chinese herbal medicine with important medical values, Hedyotis chrysotricha has been suggested to be useful for the treatment of many diseases, especially cancer. Objective: Our aim was to investigate the antioxidant and antitumor activities of the phytochemical extracts of H. chrysotricha. Methods: 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay was applied to determine antioxidant property. 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazoliumromide assay, wound healing assay, transwell matrix assay, flow cytometry and cell morphology were established to observe anti-proliferative, anti-migration, anti-invasion and apoptosis induction effects. The intracellular reactive oxygen species generation was detected by reactive oxygen species detection assay. Results: The ethyl acetate fraction showed promising antioxidant activity with IC50 of 98.67±0.49 μg/ml, and petroleum ether fraction exhibited the most potent antiproliferative effect on various human cancer cell lines, especially MDA-MB-231 (IC50 = 8.90±1.23 μg/ml) and HCT-116 (IC50 = 9.69±3.69 μg/ml) cancer cells. Further investigation revealed that the petroleum ether fraction suppressed the proliferation, migration and invasion of the cancer cells significantly. Additionally, it promoted cell apoptosis by increasing reactive oxygen species levels. Conclusion: H. chrysotricha extract possessed excellent antioxidant and antitumor activities. Therefore, it could be useful as a source of antioxidants and compounds for cancer therapy.

Background: Some Alstonia species are used in traditional medicine to treat diseases such as cancer, dysentery, diarrhea, jaundice, malaria, gastrointestinal troubles, and snake-bites. Objective: In this study, we aim to evaluate the ethanol leaf extract of Alstonia scholaris for anticancer constituents and structural modification to introduce a privilege medicinal α,β-unsaturated scaffold. Methods: The relative viability of the MDA-MB-231 breast cancer cell line exposed to isolated compounds at different concentrations was assayed. Chemical analysis was carried out by high resolution mass spectrometry and one and two-dimensional NMR techniques. Results: Structures of purified compounds were determined as betulin 1, α-amyrin acetate 2, mixture of β-sitosterol 3 and stigmasterol 4, tetratriacontyl-trans-p-coumarate 5, ursolic acid 6, β-sitosterol glucoside 7, picralstonine 8 and scholaricine 9. To introduce privilege medicinal scaffold, compounds 1 and 2 under SeO2 oxidation condition afford new acrylaldehye derivatines. Compound 1 afforded Betulin acrylaldehyde 10 while compound 2 afforded lupeolacetate acryl aldehyde 11 in an intriguing mechanism with the conversion of ursane to lupane scafford. Compound 11 equally showed interesting activity against MDA MB 231 breast cancer cell line with an IC50 of 4.63 ± 0.09 μg/ml. Conclusion: From these findings, the medicinal α,β-unsaturated scaffold could have pharmacological effects in treating MDA-MB-231 breast cancer.