Project's information

Project's title Study on iridoids extraction procedures and iridoid derivatives transformation from Dolichandrone spathacea to prepare antihyperglycemic production
Project’s code VAST04.03/19-20
Research hosting institution Institute of Chemistry
Project leader’s name Dr. Tran Thi Phuong Thao
Project duration 01/01/2019 - 31/12/2021
Project’s budget 600 million VND
Classify Excellent
Goal and objectives of the project

- To investigate iridoids extraction procedures from Dolichandrone spathacea in high yields.
- To investigate iridoid derivatives transformation procedure.
- To produce the antihyperglycemic iridoid production from Dolichandrone spathacea.

Main results

Scientific research results:
- From Dolichandrone spathacea collected in Thua Thien Hue province: 9 compounds were purified and elucidated, of which two iridoids were isolated in large scale for synthetic transformation.
- From Dolichandrone spathacea collected in Soc Trang province: 4 iridoids  were isolated and elucidated, of which 2 main iridoids were also identified in the samples from Thua Thien Hue province.
- 10 iridoid derivatives were semi-synthesized from 4 isolated iridoids, five of them are new derivatives.
- Evaluation of α-glucosidase inhibition of 14 isolated and synthesized iridoids. Five of them possessed significant activity, of which nemoroside was the best active compound with an IC50 of 0.05 µM (5700 times better than acarbose-IC50 285 µM).
- Evaluation of  α-glucosidase inhibition of iridoid production (IC50 = 114.09 ± 2 µM).
- Evaluation of acute toxicity of D. spathacea production. The result showed that the production was non-toxic in mice (oral intake, maximum dose 10 g production/kg of mice).
- Establishing the baseline standard of iridoid production from D. spathacea, quantifying the total content of iridoids. The results showed that the contents of two main iridoids are 2.09 and 3.13% in the production.
- Screening virtually the structures of 15 iridoids on the molecular docking to investigate the structure-activity relationships. The theoretical calculation was compatible with experimental results.
- Publishing 1 article in RSC Advances (RSC Advance, 11, 35765-35782, 2021) and 1 article in Vietnam Journal of Chemistry (2021, 59 (6), 943-920).
Application results:
- The iridoid extraction procedure in laboratory scale was achieved.
- The synthesized procedures of 7 iridoid derivatives were achieved
- The procedure to prepare antihyperglycemic iridoid production of 100 gram/scale was established.
- Preparation of 224 g antihyperglycemic iridoid production.

Novelty and actuality and scientific meaningfulness of the results

- The chemical constituents of the fruits of D. spathacea was studied for the first time.
- 3 compounds were isolated for the first time from D. spathacea and 5 new iridoid derivatives were synthesized.
- The first study on α-glucosidase inhibitory activity of the isolated and synthesized iridoids.
- The first study on the structure-activity relationships of 15 iridoids based on the molecular docking.

Products of the project

- Scientific papers in referred journals (list): 2 scientific articles (RSC Advances and Vietnam Journal of Chemistry).
- Patents (list):
- Technological products (describe in details: technical characteristics, place):
+ The iridoids extraction procedure in lab scale.
+ The synthesized procedure of 7 iridoid derivatives.
+ The procedure for preparation of antihyperglycemic iridoid production in 100 gram/scale.
+ 224 g antihyperglycemic iridoid production.
+ The in vitro anti-hyperglycemic activity of the isolated and synthesized iridoids.
+ The spectroscopic data of 21 isolated or synthesized compounds (MS, NMR, IR,…).
+ The anti-hyperglycemic activity of iridoid production.
+ The baseline standard of iridoid production (including the report of baseline standard establishment, the acute toxicity data and main iridoids quantification).

Recommendations Study on antihyperglycemic mechanism of the production for futher application as functional food, supporting for treatment of diabetic diseases.
Images of project
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