Cynanchum atratum Bunge (C. atratum) and Cynanchum versicolor Bunge (C. versicolor) are two related species that have been used as "Baiwei" (Cynanchi Atrati Radix Et Rhizoma) in traditional medicine in China and other Asian countries for a long time. However, to date, no comprehensive review of C. atratum and C. versicolor has been published. This review provides a comprehensive summary on the botany, phytochemistry, traditional uses and pharmacology of Baiwei; The authors focus especially on the revision of errors in previous articles and reviews, updating information and providing a comparison of C. atratum and C. versicolor. Furthermore, current research reveals significant disparities in the chemical composition and pharmacological effects between C. atratum and C. versicolor. Up to November 2023, 178 compounds have been isolated from C. atratum and C. versicolor, including C₂₁ steroids, acetophenones, alkaloids and volatile oils. These compounds and extracts have been proven to exhibit significant pharmacological activities, including anti-inflammatory, anti-tumor, anti-virus, anti-fungal, memory-enhancing and anti-pyretic action, immune modulatory effects, reducing blood lipid, inhibition of melanin production, and anti-parasitic effects. Therefore, this review presents new insights into these two herbs used as "Baiwei" and further study is warranted to enhance their clinical application. Please cite this article as: Xie W, Liu XY, Li X, Jin YS. Cynanchum atratum Bunge and Cynanchum versicolor Bunge for Baiwei: An updated review of their botany, phytochemistry, traditional uses and pharmacological activities. J Integr Med. 2025; 23(3): 230-255.
Cynanchum/chemistry* ; Humans ; Drugs, Chinese Herbal/chemistry* ; Phytochemicals/pharmacology* ; Animals ; Medicine, Chinese Traditional ; Plant Extracts/chemistry*

The study aimed to investigate the mechanism of hepatoprotective effect of C-21 steroidal glucosides from Cynanchum auriculatum( Baishouwu) on oxidative stress in mice with liver injury. Mice were randomly divided into normal group,model group,positive control group,Baishouwu high group and Baishouwu low group. The liver injury model was induced by intraperitoneal injection of CCl4 peanut oil solution. All mice were sacrificed to collect blood and liver specimens. The activities of serum levels of ALT and AST were detected. The content of MDA and the activity of SOD in liver homogenate were examined by colorimetry method. Tissues were stained with hematoxylin-eosin for histological examination. The hepatic protein expressions of NF-κB p65,p-IκBα,i NOS and COX-2 were detected by Western blot. The mRNA expressions of TNF-α and IL-6 were determined by RT-PCR. It was found that treatment with C-21 steroidal glucosides from Baishouwu successfully attenuated liver injury induced by CCl4,as shown by decreased levels of serum biochemical indicators( AST,ALT)( P<0. 01). Administration of total C-21 steroidal glucosides enhanced the activity of SOD( P<0. 01) and decreased the content of MDA( P<0. 01) in liver homogenate. Microscopic features suggested that treatment with C-21 steroidal glucosides from Baishouwu was effective in inhibiting CCl4-induced hepatocyte edema and degeneration. Further studies showed that NF-κB p65 overexpression induced by CCl4 was decreased by C-21 steroidal glucosides,leading to the markedly down-regulated protein expression levels of p-IκBα,i NOS and COX-2,as well as the depression of TNF-α and IL-6 mRNA expressions. In conclusion,total C-21 steroidal glucosides from Baishouwu exhibited potent effect on oxidative stress pathway in mice with liver injury induced by CCl4,with enhanced activity of SOD,decreased content of MDA,and down-regulated levels of NF-κB p65,p-IκBα,i NOS and COX-2.
Animals ; Carbon Tetrachloride ; Chemical and Drug Induced Liver Injury ; drug therapy ; Cynanchum ; chemistry ; Glucosides ; pharmacology ; Hepatocytes ; drug effects ; Liver ; drug effects ; Mice ; Oxidative Stress ; Random Allocation

The present study was designed to further investigate the C steroidal glycosides in Cynanchum plants. Two new steroidal glycosides based on a 13, 14:14, 15-disecopregnane-type aglycone, komaroside P (1) and komaroside Q (2), together with three known compounds (3-5) were isolated from the whole herbs of Cynanchum komarovii. The aglycones of compounds 1 and 2 were two new disecopregnane. Their structures were elucidated on the basis of 1D, 2D NMR spectroscopic data and acid hydrolysis. All the compounds (1-5) showed potent inhibitory activities against human leukemia cell lines (HL-60) with IC values ranging from 16.6 to 26.3 μmol·L, compared to the positive control 5-fluorouracil (6.4 μmol·L).
Cell Survival ; drug effects ; Cynanchum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Glycosides ; chemistry ; isolation & purification ; pharmacology ; HL-60 Cells ; Humans ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Steroids ; chemistry ; isolation & purification ; pharmacology

Cynanchum is one of the most important genera in Asclepiadaceae family, which has long been known for its therapeutic effects. In this genus, 16 species are of high medicinal value. The extracts of the root and/or rhizome parts have been applied in traditional Chinese medicines (TCM) for the prevention and treatment of various illnesses for centuries. C21 steroids, as the typical constituents of Cynanchum species, possess a variety of structures and pharmacological activities. This review summarizes the comprehensive information on phytochemistry and pharmacology of C21 steroid constituents from Cynanchum plants, based on reports published between 2007 and 2015. Our aim is to provide a rationale for their therapeutic application, and to discuss the future trends in research and development of these compounds. A total of 172 newly identified compounds are reviewed according to their structural classifications. Their in vitro and in vivo pharmacological studies are also reviewed and discussed, focusing on antitumor, antidepressant, antifungal, antitaging, Na(+)/K(+)-ATPase inhibitory, appetite suppressing and antiviral activities. Future research efforts should concentrate on in vitro and in vivo biological studies and structure activity relationship of various C21 steroid constituents.
Animals ; Cynanchum ; chemistry ; Humans ; Molecular Structure ; Plant Extracts ; chemistry ; pharmacology ; Steroids ; chemistry ; pharmacology

Eleven C21 steroids were isolated from chloroform extract of roots of Cynanchum otophyllumby silica gel, MCI, ODS columns, and semi-preparative HPLC. Their structures were determined by spectroscopic data analysis as otophylloside B(1), caudatin-3-O-beta-D-cymaropyranosyl-(1-->4)-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (2), caudatin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (3), caudatin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-digitoxopyranosyl-(1-->4)-beta-D-cymaropyranoside (4), otophylloside O (5), gagamine-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (6), sinomarinoside B (7), mucronatosides C (8), wallicoside J (9), stephanoside H (10), and qinyangshengenin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-digitoxopyranoside (11). Among them, compounds 2-3, and 6-11 were separated from the roots of this plant for the first time.
Cynanchum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Plant Roots ; chemistry ; Steroids ; chemistry ; isolation & purification

OBJECTIVETo study anti-HIV activity and mechanism of Cynanchum otophyllum glucan sulfate in vitro.

METHODAnti-HIV-1 activity was detected with syncytial formation assay and quantitative P24 enzyme-linked immunosorbent assay (ELISA); cytotoxicity was tested with MTT colorimetric assay. Antiviral mechanism was investigated by fusion inhibition, time of addition and pre-treatment experiments.

RESULTThe 50% inhibition concentrations (IC50) of PS20 for HIV-1(IIIB), HIV-1(Ada-M), and HIV-1(Bal), were 0.26, 0.46, 0.90 micromol x L(-1), respectively. Studies on antiviral mechanism of PS20 showed that target molecule may be viral envelope protein.

CONCLUSIONThe results suggested that PS20 had high anti-HIV activity and was worth to be studied further.

Anti-HIV Agents ; pharmacology ; Cell Fusion ; Cell Line ; Cell Proliferation ; drug effects ; Cynanchum ; chemistry ; Glucans ; isolation & purification ; pharmacology ; HIV-1 ; drug effects ; Humans ; Inhibitory Concentration 50 ; Plant Extracts ; pharmacology ; Plant Roots ; chemistry ; metabolism ; Viral Envelope Proteins ; drug effects

OBJECTIVETo evaluate the inhibitive effect of C-21 steroidal glycosides from the root of Cynanchum auriculatum (CGB) on rat glioma C6 cells.

METHODSC6 cells were treated with CGB for 24, 48,72 h at concentration of 30, 60, 120 mg/L, respectively. MTT assay was used for evaluating cell viability; fluorescence-activated cell sorting analysis after Annexin V/propidium iodide staining or single propidium iodide staining was used to test cell apoptosis and cell cycle.

RESULTSCGB at 30, 60, 120 mg/L concentration-dependently decreased C6 cell viability (P<0.001). CGB at 60 and 120 mg/L induced C6 cell apoptosis and cell cycle arrest. The fraction of G0/G1 cells was increased (P<0.05) and that of S phase cells was decreased (P<0.01).

CONCLUSIONCGB can inhibit the growth of rat glioma C6 cells, and induce apoptosis and G0/G1 cell cycle arrest.

Animals ; Apoptosis ; drug effects ; Cell Cycle ; drug effects ; Cell Line, Tumor ; Cynanchum ; chemistry ; Glioma ; pathology ; Monosaccharides ; pharmacology ; Rats ; Steroids ; pharmacology

OBJECTIVETo study the optimizal hydrolysis process for C21 steroidal glycoside of Bai Shou Wu by acetic acid.

METHODThe effects of acetic acid concentration, reaction temperature and reaction time had been investigated using orthogonal design and the contents of kidjoranin 3-O-beta-digitoxopyranoside, caudatin, kidjoranin 3-O-alpha-L-diginopyranosyl-(1 --> 4)-beta-cymaropyranoside and caudatin 3-O-beta-cymaropyranoside as response indexs were determined by the high performance liquid chromatography.

RESULTThe factors influencing acetic extraction efficiency were as follows: A > B > C (A. reaction temperature; B. reaction time; C. acetic acid concentration). The optimal hydrolysis condition obtained was: refluxing for 6 hours with 5.0% dilute CH3COOH solution at 100 degrees C.

CONCLUSIONThe content of antitumor active ingredients under the optimum hydrolysis condition is raised obviously and has a great part in studying this antitumor drug.

Acetates ; pharmacology ; Cynanchum ; chemistry ; metabolism ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Glycosides ; analysis ; chemistry ; metabolism ; Hydrolysis ; drug effects ; Temperature ; Time Factors

High performance liquid chromatography coupled with on-line electrospray tandem mass spectrometry (HPLC/ESI-MS/MS) was used to identify C21 steroidal glycosides in the roots of Cynanchum atratum. The structures of C21 steroidal glycosides were deduced from mass fragments features in positive and negative mode. The constituents of C. atratum were separated and detected. 7 compounds were identified by comparing their ESI-MS/MS data with the reference compounds and 2 compounds were inferred solely by the ESI-MS/MS data. The method is sensitive, and provides good separation and rapid qualitative characterization of C21 steroidal glycosides in the roots of C. atratum.
Chromatography, High Pressure Liquid ; Cynanchum ; chemistry ; Glycosides ; analysis ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; Steroids ; chemistry ; Tandem Mass Spectrometry

OBJECTIVETo investigate the effect of general glycosides from Cynanchun auriculatum of Jiangsu on liver fibrosis of rats.

METHODSeventy-two Wistar rats were randomly divided into normal group, model group, BSW three doses treated group and hydrocortisone treated group. CCl4 (50%, 2 mL x kg(-1)) was orally administraeated twice a week for 8 weeks. The liver and spleen indices were observed. The level of serum GPT, GOT, and HA, PCIII and the level of SOD, HyP, MDA in liver homogenates was also measured. The histopathologic change in hepatic of rats was examined.

RESULTThe elevation of serum GPT, GOT, HA, PCIll, MDA and HyP and the content of liver homogenates were attanuated remarkably by BSW treatment. BSW groups also increased the level of SOD of liver homogenates, and make the fibrotic liver better.

CONCLUSIONThe general glycosides in C. auriculatum of jiangsu province have an anti-hepatic fibrosis ettect on CCl4-induced fibrosis rats, the mechanisms might be associated with its anti-oxidative action.

Animals ; China ; Cynanchum ; chemistry ; Drug Evaluation, Preclinical ; Drugs, Chinese Herbal ; administration & dosage ; Glycosides ; administration & dosage ; Liver ; drug effects ; pathology ; Liver Cirrhosis ; drug therapy ; pathology ; Male ; Random Allocation ; Rats ; Rats, Wistar