In this study, we analyzed the mechanism and the process of fungal-induced agarwood formation in Aquilaria sinensis and studied the functional changes in the xylem structure after the process. The microscopic structure of the white zone, transition zone, agarwood zone, and decay zone of 12-and 18-months of inoculation A. sinensis xylem was studied. The distribution of nuclei, starch grains, soluble sugars, sesquiterpenes, fungal propagules, and mycelium in xylem tissues was investigated by histochemical analysis. The results show that the process of agarwood formation was accompanied by apoptosis of parenchyma cells such as interxylary phloem, xylem rays, and axial parenchyma. Regular changes in the conversion of starch grains to soluble sugars, the production of sesquiterpenoids, and other characteristic components of agarwood in various types of parenchyma cells were also observed. The material transformation was concentrated in the interxylary phloem, providing a structural and material basis for the formation of agarwood. It is the core part of the production of sesquiterpenoids and other characteristic products of agarwood. Compared with the A. sinensis inoculated for 12 months, the xylem of the A. sinensis inoculated for 18 months was more vigorous. There were no significant differences between the 12 and 18 months of inoculation in terms of sugars and agarwood characteristic products. In production, harvesting after 12 months of inoculation can improve harvesting efficiency.

Continuous innovation in artificially-induced agarwood technology is increasing the amount of agarwood and substantially alleviating shortages. Agarwood is widely utilized in perfumes and fragrances; however, it is unclear whether the overall pharmacological activity of induced agarwood can replace wild agarwood for medicinal use. In this study, the volatile components, total chromone content, and the differences in the overall activities of wild agarwood and induced agarwood, including the antioxidant, anti-acetylcholinesterase, and anti-glucosidase activity were all determined. The results indicated that both induced and wild agarwood’s chemical makeup contains sesquiterpenes and 2-(2-phenylethyl)chromones. The total chromone content in generated agarwood can reach 82.96% of that in wild agarwood. Induced agarwood scavenged 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS⁺) radicals and inhibited acetylcholinesterase activity and α-glucosidase activity with IC₅₀ values of 0.1873 mg/mL, 0.0602 mg/mL, 0.0493 mg/mL, and 0.2119 mg/mL, respectively, reaching 80.89%, 93.52%, 93.52%, and 69.47% of that of wild agarwood, respectively. Accordingly, the results distinguished that induced agarwood has the potential to replace wild agarwood in future for use in medicine because it has a similar chemical makeup to wild agarwood and has comparable antioxidant, anti-acetylcholinesterase, and anti-glucosidase capabilities.

Agarwood is a highly economically important medicinal herb with widespread uses; however, the difference between the biological activities of artificial and wild agarwood is unclear. In this study, the alcohol-soluble extracts of agarwood produced by fungi and natural agarwood were used to determine the differences between the overall biological activities. The antioxidant ability (the clearance rates of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS⁺) radicals, and total reducing power), anti-acetylcholinesterase, and anti-α-glucosidase activity were determined by ultraviolet-visible spectrophotometry. The results indicated that with 2 mg/mL alcohol-soluble extracts, the scavenging DPPH radical rates of the artificial agarwood samples were 93.74–102.31% of that of the wild agarwood, and the ABTS⁺ radical clearance rates of the artificial agarwood samples were 75.38–95.52% of that of the natural agarwood. With 3.5 mg/mL alcohol-soluble extracts, the artificial agarwood samples had a total reducing power of 63.07–80.29% of that of the wild agarwood. With 4 mg/mL alcohol-soluble extract, the acetylcholinesterase activity inhibition rates of the artificial agarwood samples were 102.56–109.16% of that of the wild agarwood. With 1 mg/mL alcohol soluble extracts, the α-glucosidase effect inhibitions rates of the artificial agarwood samples were 68.32–100.39% of that of the wild agarwood.