Baogongteng A
Baogongteng A and Baogongteng C are the major toxic chemical compounds of the Erycibe species. Baogongteng A analogs as effective muscarinic agonists or antagonists in clinical use.Baogongteng A is a new tropane alkaloid used for treating glaucoma, synthetic baogongteng A also shows myotic activities in rabbits, but the potency is half of that of the natural product.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Bioorg Med Chem. 2008 Dec 15;16(24):10251-6.
The absolute configuration plays an important role in muscarinic activity of BGT-A and its analogs.[Pubmed:
19013075]
METHODS AND RESULTS:
Both enantiomers of 2, 3, and 4, three bioactive analogs of muscarinic agonist BGT-A were prepared respectively and underwent functional studies and radioreceptor binding assays. 6S enantiomers of 2, 3, and 4 showed obvious muscarinic activity, while 6R ones elicited little muscarinic activity by functional studies. Besides, the affinity of 6S enantiomers of 2, 3, and 4 was greatly larger than that of their 6R enantiomers respectively. All these pharmacological results indicated the 6S configuration was beneficial for the active BGT-A analogs to bind with the muscarinic receptors. The finding was in good agreement with our previous SAR study to BGT-A and its active analogs by computational approach.
CONCLUSIONS:
The understanding to the relationship between muscarinic activity and absolute configuration will provide the basis for successive screening of BGT-A analogs as effective muscarinic agonists or antagonists in clinical use.
Regul. Toxicol. Pharm. 2014, 70(1):349-56
Toxicology and the chemical foundation of plants of Erycibe.[Pubmed:
25073109]
Erycibe is a relatively small genus in the family Convolvulaceae with over 10 identified species. Some Erycibe plant species are purportedly toxic at high doses. However, few toxicology studies have been conducted on those species.
METHODS AND RESULTS:
In this study, the toxicity of 40% ethanolic extracts of Erycibeobtusifolia, Erycibeschmidtii, and Erycibeellipptimba was evaluated. E. ellipptimba has been reported to be more toxic due to containing larger amounts of Baogongteng C, an alkaloid with known toxicity. Thus, E. ellipptimba was chosen for further toxicology study here. An HPLC-MS method was developed to identify the main components and determine the percentages of Baogongteng C in total alkaloid of E. ellipptimba (EWA). The toxicity of total alkaloid and Baogongteng C was evaluated and compared.
CONCLUSIONS:
The results indicated that Baogongteng A and Baogongteng C are the major toxic chemical compounds of the Erycibe species tested. The results also suggest EWA is cholinergic. Finally, in a subacute toxicity study of EWA, alterations observed with high dosage suggest that the liver and kidney could be the target organs of toxicity.
Yao Xue Xue Bao. 1998 Nov;33(11):832-5.
The preparation and bioactivities of chiral analogs of baogongteng A.[Pubmed:
12016943]
Eight chiral analogs of Baogongteng A were prepared from (+/-)-3 alpha-hydroxy-6 beta-acetoxytropane by chemical resolution.
METHODS AND RESULTS:
In myotic or mydriatic tests in rabbits, (-)-3 alpha-paramethyl benzenesulfonyloxy-6 beta-acetoxytropane showed cholinergic activities, while (+)-3 alpha-benzoyloxy-6 beta-acetoxytropane and (+)-3 alpha-parachloro benzoyloxy-6 beta-acetoxytropane showed anticholinergic activities.
Bioorg Med Chem Lett. 2005 Nov 1;15(21):4814-8.
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists.[Pubmed:
16153841]
Baogongteng A (BGT-A), a naturally occurring tropane muscarinic agonist isolated from Chinese medicinal plant, exhibits a bioactive effect different from those of many tropane alkaloids that are muscarinic antagonists.
METHODS AND RESULTS:
A series of racemic derivatives of BGT-A was synthesized to study the structure-activity relationships (SAR). To explore further the SAR in this series and to ultimately design muscarinic agonists for drug development, a Comparative Molecular Field Analysis (CoMFA) was performed. The values of the leave-one-out cross-validated correlation coefficient q2 and the conventional correlation coefficient r2 for the model are 0.613 and 0.965, respectively.
CONCLUSIONS:
The regression analysis of the data indicated that the steric effect of N-substituted group on tropane of analyzed compounds critically affected the agonistic activity to muscarinic receptors.
Yao Xue Xue Bao. 1989;24(2):105-9.
Studies on synthesis of baogongteng A--a new myotic agent.[Pubmed:
2801130]
Baogongteng A, isolated from Erycibe obtusifolia Benth., is a new tropane alkaloid used for treating glaucoma.
METHODS AND RESULTS:
Using synthetic 6 beta-acetoxy-tropinone as starting material, racemic Baogongteng A(8) was synthesized. Synthetic Baogongteng A also shows myotic activities in rabbits, but the potency is half of that of the natural product.
