Astragali Radix: comprehensive review of its botany, phytochemistry, pharmacology and clinical application.

Astragali Radix (A. Radix) is the dried root of Astragalus membranaceus var. mongholicus (Bge) Hsiao or Astragalus membranaceus (Fisch.) Bge., belonging to the family Leguminosae, which is mainly distributed in China. A. Radix has been consumed as a tonic in China for more than 2000 years because of its medicinal effects of invigorating the spleen and replenishing qi. Currently, more than 400 natural compounds have been isolated and identified from A. Radix, mainly including saponins, flavonoids, phenylpropanoids, alkaloids, and others. Modern pharmacological studies have shown that A. Radix has anti-tumor, anti-inflammatory, immunomodulatory, anti-atherosclerotic, cardioprotective, anti-hypertensive, and anti-aging effects. It has been clinically used in the treatment of tumors, cardiovascular diseases, and cerebrovascular complications associated with diabetes with few side effects and high safety. This paper reviewed the progress of research on its chemical constituents, pharmacological effects, clinical applications, developing applications, and toxicology, which provides a basis for the better development and utilization of A. Radix.

Curcumae Radix: A Review of Traditional Use, Phytochemistry, Pharmacology, Toxicology and Quality Control.

Curcumae Radix (CuR) is a traditional Chinese medicine that has been used in China for more than 1,000 years. It has the traditional efficacy of activating blood and relieving pain, promoting qi and relieving depression, clearing heart and cooling blood, and promoting gallbladder and removing jaundice. Based on this, many domestic and foreign scholars have conducted systematic studies on its chemical composition, pharmacological effects, toxicity and quality control. Currently, 250 compounds, mainly including terpenoids and curcuminoids, have been isolated and identified from CuR, which has pharmacological activities, including antitumor, anti-inflammatory and analgesic, antidepressant, hepatoprotective, hemostatic, hematopoietic, and treatment of diabetes mellitus. In modern clinical practice, CuR is widely used in the treatment of tumors, breast hyperplasia, hepatitis, and stroke. However, the generation of toxicity and clinical application of CuR and Caryophylli Flos, the determination of the concoction process of artifacts, the determination of specific Quality Marker, and the establishment of the quality control system of CuR, are problems that need to be solved urgently at present.

[Phenolic derivatives from root bark of Schisandra sphenanthera].

This paper aimed to study the chemical constituents from the root bark of Schisandra sphenanthera. Silica, Sephadex LH-20 and RP-HPLC were used to separate and purify the 80% ethanol extract of S. sphenanthera. Eleven compounds were identified by ~1H-NMR, ~(13)C-NMR, ESI-MS, etc., which were 2-[2-hydroxy-5-(3-hydroxypropyl)-3-methoxyphenyl]-propane-1,3-diol(1), threo-7-methoxyguaiacylglycerol(2),4-O-(2-hydroxy-1-hydroxymethylethyl)-dihydroconiferylalcohol(3), morusin(4), sanggenol A(5), sanggenon I(6), sanggenon N(7), leachianone G(8),(+)-catechin(9), epicatechin(10), and 7,4'-dimethoxyisoflavone(11). Among them, compound 1 was a new compound, and compounds 2-9 were isolated from S. sphenanthera for the first time. Compounds 2-11 were subjected to cell viability assay, and the results revealed that compounds 4 and 5 had potential cytotoxicity, and compound 4 also had potential antiviral activity.

[Chemical constituents of Helleborus thibetanus].

The chemical constituents of Helleborus thibetanus were isolated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, and semi-preparative RP-HPLC, and the structures of all compounds were identified by modern spectrographic technology(MS, NMR). The MTT method was used to measure the cytotoxicity of compounds 1-8. Twelve compounds were isolated from the roots and rhizomes of H. thibetanus and were identified as(25R)-22ß,25-expoxy-26-[(O-ß-D-glucopyranosyl)oxy]-1ß,3ß-dihydroxyfurosta-5-en(1), ß-sitosterol myristate(2), ß-sitosterol lactate(3), ß-sitosterol 3-O-ß-D-glucopyrannoside(4), 4,6,8-trihydroxy-3,4-dihydronaphthalen-1(2H)-one(5), 1,3,5-trimethoxybenzene(6), 7,8-dimethylbenzo pteridine-2,4(1H,3H)-dione(7), 1H-indole-3-carboxylic acid(8), p-hydroxy cinnamic acid(9), lauric acid(10), n-butyl α-L-arabinofuranoside(11) and methyl-α-D-fructofuranoside(12), respectively. Among them, compound 1 is a new compound and named thibetanoside L; compounds 2, 5-8, 11 are first isolated from the family Ranunculaceae; compound 12 is isolated from the genus Helleborus for the first time. The results of MTT assay showed that the IC_(50) values of compounds 1-8 against HepG2 and HCT116 cells were greater than 100 µmol·L~(-1).

A comprehensive review of traditional uses, phytochemistry and pharmacology of Reynoutria genus.

OBJECTIVES: The genus Reynoutria belonging to the family Polygonaceae is widely distributed in the north temperate zone and used in folk medicine. It is administered as a sedative, tonic and digestive, also as a treatment for canities and alopecia. Herein, we reported a review on traditional uses, phytochemistry and pharmacology reported from 1985 up to early 2022. All the information and studies concerning Reynoutria plants were summarized from the library and digital databases (e.g. ScienceDirect, SciFinder, Medline PubMed, Google Scholar, and CNKI). KEY FINDINGS: A total of 185 articles on the genus Reynoutria have been collected. The phytochemical investigations of Reynoutria species revealed the presence of more than 277 chemical components, including stilbenoids, quinones, flavonoids, phenylpropanoids, phospholipids, lactones, phenolics and phenolic acids. Moreover, the compounds isolated from the genus Reynoutria possess a wide spectrum of pharmacology such as anti-atherosclerosis, anti-inflammatory, antioxidative, anticancer, neuroprotective, anti-virus and heart protection. SUMMARY: In this paper, the traditional uses, phytochemistry and pharmacology of genus Reynoutria were reviewed. As a source of traditional folk medicine, the Reynoutria genus have high medicinal value and they are widely used in medicine. Therefore, we hope our review can help genus Reynoutria get better development and utilization.

Steroidal constituents from Helleborus thibetanus and their cytotoxicities.

Thibetanosides E-H (1-4), four new steroidal constituents including three rare sulfonates (2-4), were isolated from the roots and rhizomes of Helleborus thibetanus, together with nine known steroidal compounds (5-13). Their structures were elucidated by detailed spectroscopic analysis, including 1D and 2D NMR techniques and chemical evidence. In this study, compounds 2-13 were evaluated for their cytotoxic activities against HCT116, A549 and HepG2 tumor cell lines in vitro. Among them, compound 8 (thibetanoside C) showed cytotoxicities against A549 cells(IC50 39.6 ± 1.9 µmol·L-1) and HepG2 cells(IC50 41.5 ± 1.1 µmol·L-1), respectively. Compound 9 (23S, 24S)-24-[(O-ß-D-fucopyranosyl)oxy]-3ß, 23-dihydroxy-spirosta-5, 25(27)-diene-1ß-ylO-(4-O-acetyl- α-L-rhamnopyranosyl)-(1→2)-O-[ß-D-xylopyranosyl-(1→3)]-α-L-arabinopyranoside) showed cytotoxicity against HCT116 cells(IC50 33.6 ± 2.1 µmol·L-1).

Five new polyhydroxylated furostanol saponins from the rhizomes of Tupistra chinensis.

Five new polyhydroxylated furostanol saponins were isolated from the roots and rhizomes of Tupistra chinensis, and their structures were determined as tupistrosides J-N (1-5), together with four known furostanol saponins (6-9), on the basis of physico-chemical properties and spectral analysis. Among them, compounds 3 and 5 showed cytotoxicity against human cancer cell lines SW620 with IC50 values of 72.5 ± 2.4 and 77.3 ± 2.5 µmol·L-1, respectively. Compound 4 showed cytotoxicity against human cancer cell line HepG2 with IC50 value of 88.6 ± 2.1 µmol·L-1.

Cytotoxic activity of a synthetic deoxypodophyllotoxin derivative with an opened D-ring.

Podophyllotoxin and its synthetic derivatives are valuable medicinal agents that have antitumor, insecticidal, and antifungal properties. We previously synthesized a deoxypodophyllotoxin derivative with an opened D-ring (DPD) exhibiting potent insecticidal activity. This article was firstly performed to identify the cytotoxicity of DPD toward human cancer cell lines (SGC7901, HeLa, and A549) and normal cell line (HEK293T) using MTT assay. DPD showed potent cytotoxicity against human cancer lines (HeLa and A549) and less cytotoxicity against normal cell lines HEK293T. DPD could also induce the cell cycle arrest at G2/M phase in HeLa cells and significantly increase the phosphorylation (Tyr 15) of CDC2 leading to inactivation of CDC2. The effects of DPD on cellular microtubule networks were detected using immunofluorescence technique in HeLa cells. The immunofluorescence results showed DPD influenced the arrangement and organization of cellular microtubule networks in HeLa cells. Microtubules are long, hollow cylinders made up of polymerized tubulin dimers. Total microtubules were separated after DPD treatment. Western blot results showed that the free polymerized tubulin dimers were obviously increased after DPD treatment. DPD may be a good drug candidate with the therapeutic potential to human cancer by affecting microtubule polymerization.

[Chemical constituents of Jasminum giraldii and their antioxidant activity].

Ten compounds were isolated from the barks of Jasminum giraldii by means of various of chromatographic techniques such as silica gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by spectroscopic data analysis as (+)-medioresinol (1), (+) -syringaresinol (2), syringaresinol-4'-O-beta-D-glucopyranoside (3), oleanic acid (4), 3-methoxy-4-hydroxy-trans-cinnamaldehyde (5), trans-sinapaldehyde (6), syringaldehyde (7), 1-(4-methoxy -phenyl) -ethanol (8), trans-cinnamic acid (9), and 4-(1-methoxyethyl) -phenol (10). Among them, compounds 1-3, 5-8 and 10 were isolated from the J. genus for the first time and compounds 4 and 9 were obtained from J. giraldii for the first time. In the DPPH free radical scavenging assay, compound 1 exhibited significant activity (IC50 55.1 micromol x L(-1)), compared with vitamin C(IC50 59.9 micromol x L(-1)); and compound 2 showed moderate activity (IC50 79.0 micromol x L(-1)), compared with 2, 6-di-tert-butyl4-methylphenol (IC50 236 micromol x L(-1)).

[Chemical constituents of leaves of Panax japonicus var. major].

Seven compounds were isolated from the leaves of Panax japonicus var. major by chromatographic methods including silica gel, Sephadex LH-20, ODS and semi-preparative HPLC. Their structures were elucidated by their physical and chemical properties and spectral data analysis as 5, 7-dihydroxy-8-methoxyl flavone (1), ginsenoside Rs2 (2), quinquenoside R1 (3), ginsenoside Rs1 (4), notoginsenoside Fe (5), ginsenoside Rd2 (6) and gypenosiden IX (7). Among them, compound 1 was obtained from the Panax genus for the first time, and compounds 2-7 were isolated from this plant for the first time.

[Chemical constituents of leaf of Eucommia ulmoides].

Ten compounds were isolated from the leaf of Eucommia ulmoides by means of recrystallization and chromatographic techniques such as D-101 macroporous resin, MCI resin, ODS gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by NMR spectral analyses as kaempferide 3-O-beta-D-glucoside (1), quercetin-3-O-beta-D-glucoside (2), quercetin (3), quercetin-3-O-beta-D-xylosyl-(1-->2)-beta-D-galactoside (4), kaempferol-3-O-alpha-L-rhamnosyl-(1-->6)-beta-D-glucoside (5), (2S,3S)-taxifolin 3-O-beta-D-glucoside (6) ,4-hydroxy cinnamic acid (7), (+)-cycloolivil (8), pinoresinol beta-D-glucoside (9), squalene (10). Among them compounds 1,5-7,10 were isolated from the Eucommia genus for the first time. In the DPPH free radical scavenging assay, compound 2 exhibited significant activity (IC50 13.7 micromol x L(-1)), compared with vitamin C (IC50 59.9 micromol x L(-1)); compounds 1, 3 and 9 showed moderate activity (IC50 161,137, 214 micromol x L(-1)), compared with 2,6-di-tert-butyl-4-methylphenol (IC50 236 micromol x L(-1)); compound 4 and 6 showed weak activity (IC50 264, 299 micromol x L(-1)).

Study on the effects of sulfur fumigation on chemical constituents and antioxidant activity of Chrysanthemum morifolium cv. Hang-ju.

The traditional after-harvesting drying method of C. morifolium cv. Hang-ju (HJ) is sun drying, but recently sulfur fumigation is increasingly used as a cheap and convenient method. However, the effects of sulfur fumigation on chemical constituents and potential activities of HJ were unknown. A comprehensively comparison of the chemical profiles between non-fumigated HJ (NHJ) and sulfur-fumigated HJ (SHJ) was conducted by HPLC fingerprints analysis and the discrepant peaks were identified or tentatively assigned by HPLC-ESI/MS(n). Dramatic chemical changes were found that the contents of 4 flavonoid aglycones remarkably increased while those of 7 glycosides significantly reduced which suggested that sulfur-fumigation induced flavonoid glycosides transformed into aglycons by hydrolysis reaction. A significant loss of hydroxycinnamoylquinic acids showed the sulfur fumigation was a destructive effect on HJ. Principal component analysis (PCA) was employed to rapidly discriminate NHJ and SHJ samples. By ICP-OES analysis, it was found that the residue of sulfur of SHJ were three times higher than NHJ (p<0.05). The antioxidant activity of NHJ and SHJ were evaluated by DPPH and FRAP assay, and the results showed that NHJ had much stronger antioxidant activities than SCF (p<0.05). Combining the results of chemical analysis, residue of sulfur and pharmacological evaluation, it showed that the sulfur fumigation was a destructive effect on HJ.

[Characteristics of inorganic elements in Panacis Majoris Rhizoma and relationship with its Daodi habitat].

OBJECTIVE: To investigate the Daodi habitat of Panacis Majoris Rhizoma by analyzing the characteristics of inorganic elements in Panacis Majoris Rhizoma from different habitats. METHODS: The contents of inorganic elements in Panacis Majoris Rhizoma from different habitats were determined by ICP-AES. The characteristics of inorganic elements in Panacis Majoris Rhizoma were analyzed by correlation analysis, principal component analysis and cluster analysis. RESULTS: It was showed that there was a correlation between the contents of inorganic elements and the medicine quality of Panacis Majoris Rhizoma; Fe, Cr, Al, Mg, Cd, Ca and Zn were principal components of Panacis Majoris Rhizoma; and the contents of inorganic elements in Panacis Majoris Rhizoma existed regional differences. CONCLUSION: The contents of inorganic elements Ca, Fe and Zn,especially the content of the essential trace elements Fe and Zn, can be used as one of the key reference for medicinal quality evaluation of Panacis Majoris Rhizoma; as well, Shaanxi Province is probably the Daodi habitat of Panacis Majoris Rhizoma.

[Analysis on chemical components from water extract of paeoniae radix alba by high performance liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry].

This experiment was performed to establish a qualitative analysis on chemical composition in water extract of Paeoniae Radix Alba by HPLC-ESI-Q-TOF-MS. The analysis was conducted on a C18 (Hanbon Lichrospher, 4.6 mm x 250 mm, 5 microm) column with methanol-0.1% formic acid as the mobile phase for gradient elution; ESI ion source was used for mass spectra, and data were collected in both positive and negative modes. The results showed that eleven compounds from water extract of Paeoniae Radix Alba had been identified by analyzing positive and negative ion mass data including element composition and by comparing with data from literatures. Since efficient separation of HPLC and the high sensitive detection of MS was used, this experiment, it will provide evidences for elucidation of the effective substance in the water extract of Paeoniae Radix Alba.

Insulin-secretagogue activity of eleven plant extracts and twelve pure compounds isolated from Aralia taibaiensis.

AIMS: To investigate the insulinogenic activities of the eleven saponins enriched traditional Chinese medicine (TCM) extracts. MAIN METHODS: Radioimmunoassay and trypan blue exclusion assay were used to investigate the insulinogenic activity and cytotoxic effects respectively. KEY FINDINGS: The total saponin extract of Aralia taibaiensis (sAT) exhibited highest insulinogenic activity and no cytotoxicity was recorded. Twelve pure compounds from sAT stimulated insulin secretion from a mouse insulinoma ßTC3 cells in a concentration-dependent manner. TA35 outperformed the other compounds which suggested that the active insulinogenic ingredient of sAT was probably TA35. In addition, both sAT and TA35 markedly potentiated glucose-induced insulin secretion. SIGNIFICANCE: Our study is the first to show that sAT dramatically stimulated insulin secretion and its antidiabetic activity may be related to its high saponin content. These findings suggested that sAT and the compound TA35 isolated from sAT may provide novel therapeutic tools for the treatment of non-insulin dependent diabetes mellitus (NIDDM).

A new compound from the leaves of Panax ginseng.

Two compounds were isolated from the leaves of Panax ginseng. Their structures were identified as 3beta,6alpha,12beta-triol-22,23,24,25,26,27-hexanordammaran-20-one, and dammar-20(22),24-diene-3beta,6alpha,12beta-triol by spectral and chemical methods. The complete signal assignments of the two compounds were carried out by means of 2D NMR spectral analysis.

[Determination of loniceroside A and C in Lonicerae japonicae by RP-HPLC].

OBJECTIVE: To develop an HPLC method for determination of loniceroside A and loniceroside C in Lonicerae japonicae. METHOD: The analysis was carried out on an Alltech C18 column (4.6 mm x 250 mm, 5 microm) evaluated with methanol-acetonitrile-0.1% glacial acetic acid as mobile phase. Flow rate was at 1.0 mL x min(-1) and the detection wavelength was at 210 nm for UV detection. RESULT: The calibration curves were linear over the range from 0.15 to 2.25 microg (r = 0.999 9) for loniceroside A and 0.11 to 1.65 microg (r = 0.999 1) for loniceroside C. The average recoveries were 99.9% and 98.3%, respectively. CONCLUSION: The contents of Loniceroside A&C are diverse in Flos Lonicerae japonicae in different regions.