Pilot Study of a Herbal Formulation Composed of Bidens pilosa for Constipation in Humans

ABSTRACT The gut microbiota and their metabolites are associated with constipation and other gastrointestinal diseases. Dietary phytochemicals are crucial factors shaping gut microbiota. Here, we conducted a first‐in‐human trial of the herbal formulation BP, composed of a Bidens pilosa extract and excipient, in volunteers with constipation. Data from the Bristol Stool Form Scale, Cleveland Clinic Constipation Score, and the Quality of Life Scale for Patients with Constipation indicated that BP improved constipation and quality of life in patients with constipation. Metagenomic data showed that BP increased the abundance of bacterial genera with beneficial potential and decreased the abundance of those with harmful potential in the stools of most volunteers. To dissect the clinical mechanism of BP, loperamide‐treated mice were used to tease out its anti‐constipation mechanism. Mouse data demonstrated that BP improved loperamide‐induced constipation and modulated the gut microbiota. Mechanistically, BP at ≥ 0.5 μg/mL promoted probiotics, including Bifidobacterium and Lactobacillus , and at 800 μg/ml or higher, it inhibited pathogens, such as Escherichia coli , Salmonella enterica , and Clostridium difficile . Inter‐bacterial antagonism data revealed that probiotics inhibited pathogens. Collectively, BP promoted relief of constipation and modulated the gut microbiota, involving increased levels of probiotics and their metabolites that antagonized pathogenic bacteria.