Scientia Agricultura Sinica ›› 2026, Vol. 59 ›› Issue (20): 4547-4569.doi: 10.3864/j.issn.0578-1752.2026.20.009

• HORTICULTURE • Previous Articles     Next Articles

Research Progress and Prospect of Medicinal Citrus Application

LIU ZeYang1,2,3(), LIANG YaNing1,2,3(), CHEN Qi1,2,3, TAN MengQi1,2,3, ZHANG HuiXian1,2,3, YUAN ZiYu1,2,3, YANG Yong4, ZHANG Fei1, XU Qiang1, DENG XiuXin1, CHEN JiaJing1,2,3(), XU Juan1,2,3()   

  1. 1 National Key Laboratory for Germplasm Innovation and Utilization of Horticultural Crops/College of Horticulture and Forestry, Huazhong Agricultural University, Wuhan 430070
    2 Hubei Hongshan Laboratory, Wuhan 430070
    3 Sensory Evaluation and Quality Inspection Center for Horticultural Products, Huazhong Agricultural University, Wuhan 430070
    4 People's Government of Qianjiang City, Hubei Province, Qianjiang 433100, Hubei
  • Received:2026-03-08 Accepted:2026-07-21 Online:2026-10-16 Published:2026-10-21
  • Contact: CHEN JiaJing, XU Juan

Abstract:

In addition to fresh consumption, juicing, and essential oil extraction, citrus is also an important botanical source in traditional Chinese medicine. With a history of medicinal use spanning over two millennia, their therapeutic effects are attributed to diverse bioactive compounds, including flavonoids, volatile components, alkaloids, coumarins, limonoids, and polysaccharides, which collectively contribute to antioxidant, anti-inflammatory, and anticancer activities. However, the composition and levels of these active components are influenced by multiple factors, such as germplasm, environment, developmental stage, and tissue type, resulting in considerable variation in efficacy among different genotypes, origins, and harvest periods. Despite widespread recognition of its medicinal and health benefits, research remains limited in several key areas, including the accurate identification of botanical origins, systematic characterization of bioactive components, establishment of official quality evaluation standards, and exploration of novel germplasm resources. This review systematically examined the medicinal citrus germplasm resources, medicinal tissues, and their primary functional components, focusing on the material basis of efficacy and fundamental evaluation indicators. Future research prospects were also proposed concerning quality assessment system improvement, accurate germplasm identification, novel resource exploitation and standardized personalized medicinal application. Collectively, this review provides a theoretical foundation for improving the quality control of medicinal citrus, promoting the discovery and utilization of novel germplasms, and facilitating the development of industry-wide regulatory standards.

Key words: medicinal citrus, source plant, bioactive constituent, comprehensive evaluation, germplasm exploration and innovation

Fig. 1

Source plants, processed medicinal materials, major bioactive components, and representative Chinese patent medicines of medicinal citrus A: Schematic classification of medicinal citrus source plants recorded in the Chinese pharmacopoeia; B: Illustrative diagram of medicinal citrus germplasm resources; C: Processed traditional Chinese medicinal materials; D: Structural formulae of major bioactive components; E: Representative Chinese patent medicines; F: Phylogenetic relationships of the four major categories of source plants used medicinally"

Table 1

Summary of original plants, medicinal parts and Chinese patent medicines of medicinal citrus in the Chinese Pharmacopoeia"

药材名
Medicinal material name
基原植物
Original plant source
品种群
Cultivar group
入药组织/部位
Medicinal
part or
tissue
含量标准
Content standard
功能与主治
Function and indication
中成药数量
(不完全统计)
Number (Incomplete statistics)
陈皮
Chenpi
橘及其栽培变种
Citrus reticulata and its cultivated varieties
茶枝柑、大红袍、温州蜜柑、福橘
Chachi,
Dahongpao,
Unshiu, Fuju
干燥成熟果皮
Dried ripe pericarp
陈皮:橙皮苷≥3.5%,广陈皮:橙皮苷≥2.0%,川陈皮素和橘皮素≥0.42%
Chenpi: Hesperidin≥3.5%,
Guangchenpi: Hesperidin≥2.0%, Nobiletin and tangeretin≥0.42%
理气健脾,燥湿化痰;用于脘腹胀满,食少吐泻,咳嗽痰多
Regulate qi and strengthen the spleen, dry dampness and transform phlegm. It is indicated for abdominal distension and fullness, poor appetite with vomiting and diarrhea, as well as cough with profuse phlegm
186
青皮
Qingpi
橘及其栽培变种
Citrus reticulata and its cultivated varieties
/ 干燥幼果或
未成熟果实的果皮
Dried pericarp of young or unripe fruits
橙皮苷≥5.0%
Hesperidin≥5.0%
疏肝破气,消积化滞;用于胸胁胀痛,疝气疼痛,乳癖,乳痈,食积气滞,脘腹胀痛
Soothe the liver, break stagnant qi, resolve accumulation, and transform stagnation. Chest and hypochondriac distending pain, hernia pain, breast hyperplasia (mammary nodule), acute mastitis, food accumulation with qi stagnation, and epigastric and abdominal distending pain
33
橘红
Juhong
橘及其栽培变种
Citrus reticulata and its cultivated varieties
大红袍、福橘
Dahongpao,
Fuju
干燥外层果皮
Dried exocarp
橙皮苷≥1.7%
Hesperidin≥1.7%
理气宽中,燥湿化痰;用于咳嗽痰多,食积伤酒,呕恶痞闷
Regulate qi, broaden the middle, dry dampness, and transform phlegm. Cough with profuse sputum, food accumulation due to alcohol abuse, nausea, vomiting, and stuffy oppression
11
橘核
Juhe
橘及其栽培变种
Citrus reticulata and its cultivated varieties
大红袍、福橘
Dahongpao,
Fuju
干燥成熟种子
Dried mature seed
/ 理气,散结,止痛;用于疝气疼痛,睾丸肿痛,乳痛乳癖
Regulate qi, dissipate nodules, and relieve pain. Hernia pain, testicular swelling and pain, breast pain, and breast hyperplasia (mammary nodules)
1
橘叶Juye / / / / / 3
化橘红
Huajuhong
化州柚或柚
Citrus grandis Tomentosa or Citrus grandis
/ 未成熟或近成熟的
干燥外层果皮
Dried immature or nearly ripe fruit exocarp
柚皮苷≥3.5%
Naringin≥3.5%
理气宽中,燥湿化痰;用于咳嗽痰多,食积伤酒,呕恶痞闷
Regulate qi, broaden the middle, dry dampness, and transform phlegm. Cough with profuse sputum, food accumulation due to alcohol abuse, nausea, vomiting, and stuffy oppression
12
枳实
Zhishi
酸橙及其栽培
变种或甜橙
Citrus aurantium and its cultivated varieties, or Citrus sinensis
黄皮、代代花、
朱栾、塘橙
Huangpi, Daidai,
Chuluan, Tangcheng
干燥幼果
Dried young fruit
辛弗林≥0.3%
Synephrine≥0.3%
破气消积,化痰散痞;用于积滞内停,痞满胀痛,泻痢后重,大便不通,痰滞气阻,胸痹,结胸,脏器下垂
Break stagnant qi, eliminate accumulation, transform phlegm, and dissipate stuffiness. Internal accumulation of undigested food and qi stagnation, stuffiness and distending pain, tenesmus in dysentery, constipation, phlegm stagnation with qi blockage, chest impediment (thoracic obstruction), chest binding (fullness and pain in the chest), and visceral ptosis
47
枳壳
Zhiqiao
酸橙及其
栽培变种
Citrus aurantium and its cultivated varieties
黄皮、代代花、
朱栾、塘橙
Huangpi,
Daidai,
Chuluan, Tangcheng
干燥未成熟果实
Dried immature fruit
柚皮苷≥4.0%
新橙皮苷≥3.0%
Naringin≥4.0%
Neohesperidin≥3.0%
理气宽中,行滞消胀;用于胸胁气滞,胀满疼痛,食积不化,痰饮内停,脏器下垂
Regulate qi, broaden the middle, unblock stagnation, and relieve distension. Qi stagnation in the chest and hypochondrium, distension and pain, food accumulation with indigestion, internal retention of phlegm-fluid, and visceral ptosis
79
香橼
Xiangyuan
枸橼或香圆
Citrus medica or Citrus wilsonii
/ 干燥成熟果实
Dried ripe fruit
香圆:柚皮苷≥2.5%
枸橼未作具体指标要求
Xiangyuan: Naringin≥2.5%
Citron: No specific requirement.
疏肝理气,宽中,化痰;用于肝胃气滞,胸胁胀痛,脘腹痞满,呕吐噫气,痰多咳嗽
Soothe the liver, regulate qi, broaden the middle, and transform phlegm. Qi stagnation of the liver and stomach, chest and hypochondriac distending pain, epigastric and abdominal stuffiness, vomiting and eructation, and profuse cough with sputum
6
佛手
Foshou
佛手
C. medica var. sarcodactylis
/ 干燥果实
Dried fruit
橙皮苷≥0.03%
Hesperidin≥0.03%
疏肝理气,和胃止痛,燥湿化痰;用于肝胃气滞,胸胁胀痛,胃脘痞满,食少呕吐,咳嗽痰多
Soothe the liver, regulate qi, harmonize the stomach, relieve pain, dry dampness, and transform phlegm. Qi stagnation of the liver and stomach, chest and hypochondriac distending pain, epigastric stuffiness, poor appetite, vomiting, and cough with profuse sputum
10

Fig. 2

Schematic diagram of the classification of reported and potential metabolites, pharmacodynamic components, and functional exploration in medicinal citrus The key parameters used to evaluate the physiological activities depicted in the figure are presented below: Anti-inflammatory activity was evidenced by the downregulation of pro-inflammatory cytokines (TNF-α, IL-6) and the concomitant upregulation of the anti-inflammatory cytokine IL-4. Antioxidant activity is reflected by the upregulation of the antioxidant enzyme SOD (superoxide dismutase) activity and GSH (glutathione) levels, alongside the downregulation of oxidative damage products MDA (malondialdehyde) and ROS (reactive oxygen species). Pro-apoptotic activity (particularly targeting cancer cells) is characterized by the upregulation of the pro-apoptotic protein Bax and the death receptor ligand FasL. In the figure, the arrow “↑” indicates upregulation or improvement of an indicator, while “↓” indicates downregulation or reduction"

Table 2

Potential pharmacodynamic components and their pharmacological activities in medicinal citrus"

序号
No.
潜在药效成分
Potential active constituent
化学分类
Chemical classification
药理作用
Pharmacological action
实验模型
Experimental model
参考文献
Reference
1 柚皮素
Naringenin
类黄酮
Flavonoids
抗氧化、降血糖血脂、抗肥胖、抗糖尿病、抗炎、抗器官毒性
Antioxidant, hypoglycemic and lipid-lowering, anti-obesity, antidiabetic, anti-inflammatory, and anti-organ toxicity
大鼠、小鼠
Rat, mouse
[14]
2 圣草酚Eriodictyol 抗炎、保护神经系统Anti-inflammatory and neuroprotective 大鼠Rat [15]
3 芹菜素
Apigenin
抗氧化、抗炎、抗癌、降血糖血脂、延缓衰老、减轻焦虑
Antioxidant, anti-inflammatory, anticancer, hypoglycemic and lipid-lowering, anti-aging, and anxiolytic
细胞、大鼠、小鼠
Cell, rat, mouse
[16-18]
4 木犀草素Luteolin 抗炎Anti-inflammatory 小鼠Mouse [19]
5 香叶木素Diosmetin 抗炎Anti-inflammatory 小鼠Mouse [20]
6 四甲氧基木犀草素
Tetramethoxyluteolin
调节免疫
Immunomodulatory
细胞
Cell
[21]
7 香蜂草苷Didymin 保护肝脏Hepatoprotective 小鼠Mouse [22]
8 芸香柚皮苷Narirutin 抗癌、神经保护Anticancer and neuroprotective 大鼠Rat [23-24]
9 地奥司明
Diosmin
抗炎、抗氧化、抗糖尿病、抗癌、保护肝脏、保护神经系统、保护视网膜 Anti-inflammatory, antioxidant, antidiabetic, anticancer, hepatoprotective, neuroprotective, and retinoprotective 大鼠、小鼠
Rat, mouse
[25]
10 野漆树苷
Rhoifolin
抗糖尿病、抗癌、抗氧化、抗炎
Antidiabetic, anticancer, antioxidant, anti-inflammatory
小鼠、大鼠
Mouse, rat
[26-27]
11 甜橙黄酮
Sinensetin
抗炎、降血糖血脂、抗肥胖
Anti-inflammatory, hypoglycemic and lipid-lowering, anti-obesity
大鼠、小鼠
Rat, mouse
[28-29]
12 异甜橙黄酮
Isosinensetin
抗氧化、抗癌
Antioxidant, anticancer
小鼠、细胞
Mouse, cell
[30-31]
13 芹菜素三甲醚
Apigenin trimethyl ether
治疗房颤
Treatment of atrial fibrillation
小鼠
Mouse
[32]
14 异欧前胡素
Isoimperatorin
香豆素类
Coumarins
抑制肿瘤血管生成、预防糖尿病、预防和治疗甲型流感病毒
Inhibit tumor angiogenesis, prevent diabetes, prevent and treat influenza A virus
细胞
Cell
[33-34]
15 佛手柑内酯Bergapten 抗炎、抗衰老Anti-inflammatory, anti-aging 细胞Cell [35]
16 花椒毒酚Xanthotoxol 抗炎Anti-inflammatory 细胞Cell [36]
17 伞形酮Umbelliferone 抗炎Anti-inflammatory 小鼠Mouse [37]
18 异橙皮内酯Isomeranzin 抗炎Anti-inflammatory 细胞Cell [38]
19 橙皮油素
Auraptene
抗癌、抗抑郁、预防心肌梗死、调节免疫、改善人体认知障碍
Anticancer, antidepressant, prevent myocardial infarction, immunomodulatory, improve cognitive impairment in humans
细胞、小鼠、大鼠、人体 Cell, mouse, rat, human [39-41]
20 异茴芹素
Isopimpinellin
抗癌、抑制肿瘤血管生成
Anticancer, inhibit tumor angiogenesis
小鼠、细胞、斑马鱼 Mouse, cell, zebrafish [42]
21 马尔敏Marmin 促进脂肪细胞凋亡、降脂Promote adipocyte apoptosis, lipid-lowering 细胞Cell [43]
22 欧前胡素Imperatorin 减轻心肌损伤Reduce myocardial injury 小鼠Mouse [44]
23 滨蒿内酯Scoparone 保护肝脏Hepatoprotective 小鼠Mouse [45]
24 丁香酚
Eugenol
苯丙素类
Phenylpropanoids
抗氧化、抗癌、抗糖尿病、抗肥胖、心血管保护、抗炎、镇痛、保护神经系统
Antioxidant, anticancer, antidiabetic, anti-obesity, cardiovascular protection, anti-inflammatory, analgesic, neuroprotective
小鼠、大鼠、斑马鱼
Mouse, rat, zebrafish
[46]
25 邻百里香酚Thymol 抗癌Anticancer 小鼠Mouse [47]
26 茴香脑Anethole 保护神经系统Neuroprotective 小鼠Mouse [48]
27 对香豆酸
p-Coumaric acid
抗氧化、抗炎、抑制肿瘤血管生成
Antioxidant, anti-inflammatory, inhibit tumor angiogenesis
小鼠、大鼠
Mouse, rat
[49-50]
28 2-蒈烯2-Carene 单萜
Monoterpene
抗癌Anticancer 大鼠Rat [51]
29 β-月桂烯
β-Myrcene
抗氧化、抗衰老、抗炎、抗癌
Antioxidant, anti-aging, anti-inflammatory, anticancer
大鼠、细胞
Rat, cell
[52-53]
30 d-柠檬烯d-Limonene 抗抑郁Antidepressant 小鼠Mouse [54]
31 3-蒈烯3-Carene 促进睡眠Promote sleep 小鼠Mouse [55]
32 橙花醛Neral 抗炎Anti-inflammatory 细胞Cell [56]
33 柠檬醛Citral 抗炎Anti-inflammatory 细胞Cell [56]
34 α-松油醇
α-Terpineol
抗炎、抗氧化、抗癌
Anti-inflammatory, antioxidant, anticancer
大鼠、细胞
Rat, cell
[57]
35 (R)-芳樟醇 (R)-Linalool 抗氧化、保护神经系统Antioxidant, neuroprotective 细胞Cell [58]
36 香叶醇
Geraniol
抗氧化、保护神经、抗炎
Antioxidant, neuroprotective, anti-inflammatory
大鼠、小鼠
Rat, mouse
[59-60]
37 松油烯-4-醇Terpinen-4-ol 抗氧化Antioxidant 细胞Cell [61]
38 氧化芳樟醇 Linalool oxide 抗焦虑Anxiolytic 小鼠Mouse [62]
39 橙花叔醇
Nerolidol
倍半萜
Sesquiterpene
抗氧化、抗人体溃疡病、抗癌
Antioxidant, anti-ulcer, anticancer
大鼠、细胞
Rat, cell
[63-64]
40 β-石竹烯
β-Caryophyllene
抗炎、抗氧化、抗癌、保护心肌、降血糖血脂
Anti-inflammatory, antioxidant, anticancer, cardioprotective, hypoglycemic and lipid-lowering
大鼠、细胞、小鼠
Rat, cell, mouse
[65]
41 α-蛇麻烯α-Humulene 抗炎Anti-inflammatory 小鼠Mouse [66]
42 δ-杜松烯δ-Cadinene 抑制癌细胞增殖、诱导凋亡Inhibit cancer cell proliferation, induce apoptosis 细胞Cell [67]
43 氧化石竹烯
Caryophyllene oxide
抑制癌细胞增殖、诱导凋亡
Inhibit cancer cell proliferation, induce apoptosis
细胞
Cell
[68]
44 奥巴叩酮
Obacunone
三萜
Triterpene
预防肥胖和高血糖、抑制癌细胞增殖和抗癌
Prevent obesity and hyperglycemia, inhibit cancer cell proliferation and anticancer
小鼠、细胞
Mouse, cell
[69-70]
45 柠檬苦素
Limonin
抗癌、抗炎、镇痛、抗菌抗病毒、抗氧化、保护肝脏
Anticancer, anti-inflammatory, analgesic, antibacterial and antiviral, antioxidant, hepatoprotective
小鼠、细胞
Mouse, cell
[71-73]
46 诺米林
Nomilin
抗抑郁、预防骨骼异常发育疾病、延长寿命
Antidepressant, prevent abnormal bone development diseases, prolong lifespan
小鼠
Mouse
[74-75]
47 木栓酮Friedelin 抑制癌细胞增殖Inhibit cancer cell proliferation 细胞Cell [76]
48 叶黄素
Lutein
四萜
Tetraterpene
改善人体认知障碍、改善视力、抑制动脉粥样硬化
Improve cognitive impairment in humans, improve vision, inhibit atherosclerosis
人体
Human
[77-78]
49 玉米黄质Zeaxanthin 改善人体认知障碍Improve cognitive impairment in humans 人体Human [79]
50 新叶黄素Neoxanthin 抗癌、抗氧化、抗肥胖Anticancer, antioxidant, anti-obesity 细胞Cell [80]
51 番茄红素
Lycopene
抗癌、降血糖、抗炎、保护肝脏
Anticancer, hypoglycemic, anti-inflammatory, hepatoprotective
细胞、人体
Cell, human
[81]
52 β-胡萝卜素β-Carotene 抗炎Anti-inflammatory 细胞Cell [82]
53 N-甲基酪胺
N-Methyltyramine
生物碱
Alkaloid
促进营养消化、减肥、治疗胃肠道疾病
Promote nutrient digestion, weight loss, treat gastrointestinal diseases
大鼠、小鼠
Rat, mouse
[83-84]
54 水苏碱
Stachydrine
抗纤维化、抗癌、抗炎、心血管保护
Antifibrotic, anticancer, anti-inflammatory, cardiovascular protection
大鼠、细胞
Rat, cell
[85]
55 8-羟基喹啉
8-Hydroxyquinoline
抗癌
Anticancer
细胞
Cell
[86]
56 β-谷甾醇
β-Sitosterol
甾醇类
Sterols
抗癌、抗糖尿病
Anticancer, antidiabetic
小鼠、大鼠
Mouse, rat
[87-88]
57 腐胺
Putrescine
多胺类Polyamines 抗抑郁
Antidepressant
小鼠
Mouse
[89]

Fig. 3

Schematic summary of the effects of medicinal plant parts, harvest timing, and geographic authenticity on the bioactive components of medicinal citrus A: Structure of citrus fruit tissues; B: General trends in metabolite content during fruit maturation across citrus varieties; C: Tissue-specific metabolic profiles of citrus varieties; D: Characteristic germplasms of regionally authentic medicinal citrus. The fruit structure (from inner to outer) comprises: seeds, juice sacs, segment membrane (enclosing juice sacs, shown in black dashed frame), the white layer (albedo, indicated by the white circle), the yellow layer (flavedo, indicated by the orange circle) and the pericarp consists of both flavedo and albedo. Arrows “↑” denote upregulation or increase, while arrows “↓” indicate downregulation or decrease"

Fig. 4

The primary and prospective evaluation index system and methodology for medicinal citrus Commonly used evaluation indicators mainly include bioactive components specified in the Chinese Pharmacopoeia and those reported in the latest research. Basic safety indicators cover the contents of heavy metals and pesticides, microbial contamination, as well as the impact of interactions between the human body and drugs. Important potential indicators involve growth environment, drug stability, and production and processing methods. Multi-omics evaluation indicators include metabolomics evaluation, genomics evaluation, and transcriptomics evaluation"

Fig. 5

Novel citrus germplasms with potential for medicinal use as new botanical origins A1-A6 represent different germplasms of the wrinkled skin citrus series, B1-B6 represent the fragrant citrus category[133], C1-C2 represent the sour citrus category, D1-D2 represent the citron and lemon category, and E1-E2 represent the kumquat category, each germplasm from F to K represents a separate category"

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